Literature for peptidase S09.003: dipeptidyl-peptidase IV (eukaryote)

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates Pharma

(Topics flags: S Structure, A Assay, T Target, P Specificity, K Knockout, E Expression, V Review, M Mutation, I Inhibitor, L Localization. To select only the references relevant to a single topic, click the link above. See explanation.)

2026

Aeimlapa,R., Panmanee,J., Teerapornpuntakit,J., Wongdee,K., Thongbunchoo,J., Panupinthu,N., Svasti,S., Apaijai,N., Sa-Nguanmoo,P., Chattipakorn,S., Chattipakorn,N. and Charoenphandhu,N.
Vildagliptin and Omarigliptin Differentially Bind to DPP-4 Homodimers and Modulate Osteoclast-Mediated Bone Resorption
Compr Physiol (2026) 16, e70103-e70103. PubMed Europe PubMed DOI PMC EPMC I

2025

Aguilera-Flores,C., Valencia-Morales,M.D.P., Lopez,T., Moreno-Contreras,J., Lentz,A., Espinoza,M.A., DuBois,R.M., Lopez,S. and Arias,C.F.
Functional characterization of DPP4 and FcRn as receptor and coreceptor for classical human astroviruses in Caco-2 cells
PLoS Pathog (2025) 21, e1013316-e1013316. PubMed Europe PubMed DOI PMC EPMC
Arrahman,A., Luthfianeu Edsyah,N., Thiofani,T., Sakinatun Khalidah,H., Fauziah,L., Widyasintia,A., Benson,B., Tanu Putra,K. and Hayun,H.
Synthesis and Bioactivity Investigation of Novel 2-(2-[(Dialkylamino) Methyl] Quinazolin-4-one-3-yl Methyl) Benzonitrile Derivatives as Dipeptidyl Peptidase-4 Inhibitory Agent
Iran J Pharm Res (2025) 24, e145406-e145406. PubMed Europe PubMed DOI PMC EPMC
Catanzaro,N.J., Wu,Z., Fan,C., Jefferson,V., Abdelgadir,A., Schafer,A., Yount,B.L., Bjorkman,P.J., Baric,R. and Letko,M.
ACE2 from Pipistrellus abramus bats is a receptor for HKU5 coronaviruses
Nat Commun (2025) 16, 4932-4932. PubMed Europe PubMed DOI PMC EPMC
Dastjerdi,H.F., Naderi,N., Garmabdari,A., Nematpour,M., Ebrahimi,M., Hosseinpoor,S., Saberinasab,F., Sheikholislam,Z., Hosseini,O., Rezaee,E. and Tabatabai,S.A.
Design, Synthesis and Antidiabetic Activity of Novel Pyrrole-3-Carboximidamide Derivatives as Dipeptidyl Peptidase-4 Inhibitors
Arch Pharm (Weinheim) (2025) 358, e70077-e70077. PubMed Europe PubMed DOI I
de Souza Gama,F., Ferreira,M., Segretti,N.D., Damiao,M.C.F.C., Guimaraes,C.R.W., Mascarello,A. and Azevedo,H.
Design, Optimization, and Biological Evaluation of First-in-Class Triple Inhibitors of SGLT1, SGLT2, and DPP4 for Type 2 Diabetes Mellitus
J Med Chem (2025) 68, 26121-26174. PubMed Europe PubMed DOI
Dutta,R., Khatun,S., Ghosh,P., Dey,P.K., Gayen,S. and Amin,S.A.
Exploring DPP-4: Implications in diverse diseases and structural insights for novel inhibitor design
Bioorg Chem (2025) 165, 108947-108947. PubMed Europe PubMed DOI
Faucher,F.F., Lovell,S., Bertolini,M., Blazkova,K., Cosco,E.D., Bogyo,M. and Barniol-Xicota,M.
Macrocyclic phage display for identification of selective protease substrates
bioRxiv (2025) PubMed Europe PubMed DOI PMC EPMC
Guan,X., Yu,X.Y. and Zhang,L.
A breakthrough in NSCLC therapy: targeted protein degradation of CD26 via PROTACs
EBioMedicine (2025) 123, 106082-106082. PubMed Europe PubMed DOI
Huang,Y., Wu,J., Zhang,X., Zhang,S., Wu,S. and Bao,W.
Dipeptidyl peptidase 4 is a cofactor for porcine epidemic diarrhea virus infection
Vet Microbiol (2025) 301, 110370-110370. PubMed Europe PubMed DOI
Kobayashi,K., Fujita,K., Kojima,R., Hino,R., Urano,Y. and Sato,M.
Rapid imaging of pulmonary metastasis from colorectal cancer with a red fluorescence probe targeting puromycin-sensitive aminopeptidase and dipeptidyl peptidase IV
Sci Rep (2025) 15, 43930-43930. PubMed Europe PubMed DOI PMC EPMC
Kumaragurubaran,N., Yun,H.P., Zinovicius,A., Huang,S.T., Arul,P., Lin,H.Y., Min-Shin,O. and Morkvenaite-Vilkonciene,I.
Development of an activity-based ratiometric electrochemical substrate for measuring circulating dipeptidyl peptidase-IV/CD26 in whole blood samples
Biosens Bioelectron (2025) 283, 117538-117538. PubMed Europe PubMed DOI
Li,Y., Zhang,L., Zhang,Q., Zhang,Y., Pan,S., Zhao,H. and Zhang,L.
HSPB1 suppresses oxLDL-induced vascular smooth muscle cell ferroptosis by inhibiting DPP4
Arch Biochem Biophys (2025) 768, 110400-110400. PubMed Europe PubMed DOI K
Madel Alfajaro,M., Keeler,E.L., Li,N., Catanzaro,N.J., Teng,I.T., Zhao,Z., Grunst,M.W., Yount,B., Schafer,A., Wang,D., Kim,A.S., Synowiec,A., Pena-Hernandez,M.A., Zepeda,S., Arinola,R., Kaur,R., Menasche,B.L., Wei,J., Russell,G.A., Huck,J., Song,J., Ring,A., Iwasaki,A., Jangra,R.K., Lee,S., Martinez,D.R., Mothes,W., Uchil,P.D., Doench,J.G., Spaulding,A.B., Baric,R.S., Serebryannyy,L., Tsybovsky,Y., Zhou,T., Douek,D.C. and Wilen,C.B.
HKU5 bat merbecoviruses engage bat and mink ACE2 as entry receptors
Nat Commun (2025) 16, 6822-6822. PubMed Europe PubMed DOI PMC EPMC
Martins,F.L., Ribeiro-Silva,J.C., de Jesus,E.F., Nistala,R. and Girardi,A.C.C.
Unique Role of Proximal Tubule Dipeptidyl Peptidase 4 on Blood Pressure, Renal Sodium Handling, and Na(+)/H(+) Exchanger Isoform 3 Phosphorylation
Acta Physiol (Oxf) (2025) 241, e70127-e70127. PubMed Europe PubMed DOI PMC EPMC
Shen,C., Oh,H.R., Park,Y.R., Oh,S. and Park,J.H.
Soluble DPP4 promotes hepatocyte lipid accumulation via SOX2-SCD1 signaling and counteracts DPP4 inhibition
Biochem Biophys Res Commun (2025) 756, 151521-151521. PubMed Europe PubMed DOI K
Shieh,T.M., Lin,N.C., Shen,Y.W., Lan,W.C. and Shih,Y.H.
Epithelium-derived exosomal dipeptidyl peptidase-4 involved in arecoline-induced oral submucous fibrosis
Biochim Biophys Acta Mol Basis Dis (2025) , 167683-167683. PubMed Europe PubMed DOI
Sun,L., Ma,Y., Geng,C., Gao,X., Li,X., Ru,Q., Zhu,S. and Zhang,P.
DPP4, a potential tumor biomarker, and tumor therapeutic target: review
Mol Biol Rep (2025) 52, 126-126. PubMed Europe PubMed DOI
Trivedi,A. and Gudipati,R.K.
The Caenorhabditis elegans DPF-3 and human DPP4 have tripeptidyl peptidase activity
FEBS Lett (2025) PubMed Europe PubMed DOI
Turalic,A., Osmanovic,A., Podlipnik,C., Omeragic,E., Spirtovic-Halilovic,S. and Dedibegovic,J.
Aminopeptidase and carboxypeptidase activity of DPP-4 on the example of peptides LPQNIPPL and LPbeta(3)hQNIPPL
J Mol Graph Model (2025) 142, 109173-109173. PubMed Europe PubMed DOI
Wang,X., Chen,L., Qiu,J., Wang,K., Xi,P., Cheng,X., He,Z. and Jiang,H.
Dipeptidyl Peptidase 4 Mediated Caspase-8 Affects Cognitive Impairment in Mice With Alzheimer's Disease
FASEB J (2025) 39, e71264-e71264. PubMed Europe PubMed DOI
Zhang,G., Liu,B., Qiao,D., Gao,S., Zhu,X., Huang,J., He,W., Gao,R., Zhang,L., Wang,J., Huang,Y. and Gong,Q.
PROTAC-mediated structure-function disruption of CD26: a therapeutic strategy for driver-negative non-small cell lung cancer
EBioMedicine (2025) 122, 106026-106026. PubMed Europe PubMed DOI PMC EPMC
Zhang,Y., Tan,R., Wu,L., Zhao,D., Zhong,C., Luo,C., Chung,J.Y., Tang,P.M. and Yu,C.
Epithelial DPP4 promotes Ang II-driven renal fibrosis by targeting ACE2 activity in the renin-angiotensin system
Int J Biol Sci (2025) 21, 3901-3916. PubMed Europe PubMed DOI PMC EPMC
Zhou,Y., Matsumura,T., Saito,S., Yagi,Y., Yoshinaga,T., Takeshita,M., Fukuda,K., Senokuchi,T., Motoshima,H., Kondo,T., Hatano,R., Ohnuma,K., Morimoto,C., Araki,E. and Kubota,N.
Hematopoietic dipeptidyl peptidase-4 deficiency promotes M2 macrophage polarization and attenuates atherosclerosis
Biochem Biophys Res Commun (2025) 794, 153037-153037. PubMed Europe PubMed DOI

2024

Bayanati,M., Ismail Mahboubi Rabbani,M., Sirous Kabiri,S., Mir,B., Rezaee,E. and Tabatabai,S.A.
Dipeptidyl Peptidase-4 Inhibitors: A Systematic Review of Structure-Activity Relationship Studies
Iran J Pharm Res (2024) 23, e151581-e151581. PubMed Europe PubMed DOI PMC EPMC V
Chayah,M., Luque-Gonzalez,A., Gomez-Perez,V., Salagre,D., Al-Shdaifat,A., Campos,J.M., Conejo-Garcia,A. and Agil,A.
Synthesis and Anti-Diabetic Activity of an 8-Purine Derivative as a Novel DPP-4 Inhibitor in Obese Diabetic Zucker Rats
Drug Des Devel Ther (2024) 18, 1133-1141. PubMed Europe PubMed DOI PMC EPMC I
Chen,J., Ji,H., Luo,J., Zhang,D. and Liu,S.
Two novel angiotensin-converting enzyme (ACE) and dipeptidyl peptidase IV (DPP-IV) inhibiting peptides from tilapia (Oreochromis mossambicus) skin and their molecular docking mechanism
J Food Sci (2024) 89, 3603-3617. PubMed Europe PubMed DOI I
Cui,C., Cao,F., Kong,I.I., Wu,Q., Li,F., Li,H. and Liu,D.
A model-informed approach to accelerate the clinical development of cofrogliptin (HSK7653), a novel ultralong-acting dipeptidyl peptidase-4 inhibitor
Diabetes Obes Metab (2024) 26, 592-601. PubMed Europe PubMed DOI I
Gheonea,T.C., Surlin,P., Nicolae,F.M., Gheorghe,D.N., Popescu,D.M. and Rogoveanu,I.
Dipeptidyl-Peptidase-4 and Glucagon-like-Peptide-1, a Link in the Connection between Periodontitis and Diabetes Mellitus-What Do We Know So Far?-A Scoping Review
J Clin Med (2024) 13 PubMed Europe PubMed DOI PMC EPMC
Gnoth,K., Bar,J.W., Rosche,F., Rahfeld,J.U. and Demuth,H.U.
Contribution of amino acids in the active site of dipeptidyl peptidase 4 to the catalytic action of the enzyme
PLoS ONE (2024) 19, e0289239-e0289239. PubMed Europe PubMed DOI PMC EPMC
Guo,X., Feng,H., Cai,L., Zheng,J. and Li,Y.
DPP-IV as a potential candidate in anti-obesity and obesity-related diseases treatment
Biomed Pharmacother (2024) 180, 117464-117464. PubMed Europe PubMed DOI
Ingle,H., Molleston,J.M., Hall,P.D., Bui,D., Wang,L., Foster,L., Antia,A., Ding,S., Lee,S., Fremont,D.H. and Baldridge,M.T.
The neonatal Fc receptor and DPP4 are human astrovirus receptors
Nat Microbiol (2024) 9, 3321-3331. PubMed Europe PubMed DOI PMC EPMC
Janin,Y.L.
On the origins of SARS-CoV-2 main protease inhibitors
RSC Med Chem (2024) 15, 81-118. PubMed Europe PubMed DOI PMC EPMC V I
Li,X., Zhang,Z., Jiang,W., Ju,Y., Guo,W. and Huang,Z.
Dipeptidyl Peptidase 4 (DPP4) Exacerbates Osteoarthritis Progression in an Enzyme-Independent Manner
Adv Sci (Weinh) (2024) , e2410525-e2410525. PubMed Europe PubMed DOI
Liu,M., Zeng,J., Zhang,W., Lei,J., Li,S., Zhou,J., Cheng,D. and He,L.
Fabrication of a Near-Infrared-Emissive Probe for Detecting Dipeptidyl Peptidase 4 in the Liver of Diabetic Mice and Clinical Serum
Anal Chem (2024) PubMed Europe PubMed DOI
Liu,Y., Zhao,W., Jiang,Y., Xing,S. and Li,W.
Study on the Mechanism of Interaction between Dipeptidyl Peptidase 4 and Inhibitory Peptides Based on Gaussian Accelerated Molecular Dynamic Simulation
Int J Mol Sci (2024) 25 PubMed Europe PubMed DOI PMC EPMC
Lu,P., Dai,S.M., Zhou,H., Wang,F., Dong,W.R. and Jiang,J.H.
Xanthene-based near-infrared chromophores for high-contrast fluorescence and photoacoustic imaging of dipeptidyl peptidase 4
Chem Sci (2024) 15, 2221-2228. PubMed Europe PubMed DOI PMC EPMC
Masyita,A., Firdayani,F., Listiana,S. and Besari,A.Y.
Emodin derivatives as novel potent DPP-4 inhibitors: Design, synthesis, and in vitro evaluation
Biochem Biophys Res Commun (2024) 735, 150867-150867. PubMed Europe PubMed DOI I
Nag,S., Mandal,S., Mukherjee,O., Majumdar,T., Mukhopadhyay,S. and Kundu,R.
Vildagliptin inhibits high fat and fetuin-A mediated DPP-4 expression, intracellular lipid accumulation and improves insulin secretory defects in pancreatic beta cells
Biochim Biophys Acta Mol Basis Dis (2024) 1870, 167047-167047. PubMed Europe PubMed DOI K I
Phan,H.A.T., Chang,Y., Eaton,S.A. and Petersson,E.J.
Thioamide-based fluorescent sensors for dipeptidyl peptidase 4
Chem Commun (Camb) (2024) PubMed Europe PubMed DOI PMC EPMC
Shamim,S., Alam,O., Jha,M., Nazar,S., Mathur,V., Ali,S., Iliyas,A., Chandra,K., Jamil Ahmed,S.M.A., Naim,M.J. and Parveen,B.
Triazole scaffold-based DPP-IV Inhibitors for the management of Type-II Diabetes Mellitus: Insight into Molecular Docking and SAR
Curr Top Med Chem (2024) PubMed Europe PubMed DOI V I
Shao,S., Zhang,N., Specht,G.P., You,S., Song,L., Fu,Q., Huang,D., You,H., Shu,J., Domissy,A., Li,S., Nguyen-Tran,V., Joseph,S.B., Chatterjee,A.K., Chen,J.J., Schultz,P.G. and Bollong,M.J.
Pharmacological expansion of type 2 alveolar epithelial cells promotes regenerative lower airway repair
Proc Natl Acad Sci U S A (2024) 121, e2400077121-e2400077121. PubMed Europe PubMed DOI PMC EPMC
Sivaraman,S.A. and Sabareesh,V.
An Update on Dipeptidyl Peptidase-IV Inhibiting Peptides
Curr Protein Pept Sci (2024) 25, 267-285. PubMed Europe PubMed DOI V
Vorstandlechner,V. and Mildner,M.
Much More Than Just Diabetes: The Pivotal Role of Dipeptidyl-Peptidase 4 in Skin Fibrosis
J Invest Dermatol (2024) 144, 2341-2343. PubMed Europe PubMed DOI
Zhang,J., Zhu,Y.D., Li,C.Q., Fan,Y.M., Huo,H., Sun,C.G., Zhou,J., Sun,L., Qian,X.K. and Zou,L.W.
A sensitive fluorescence assay of serum dipeptidyl peptidase IV activity to predict the suitability of its inhibitors in patients with type 2 diabetes mellitus
J Pharm Biomed Anal (2024) 249, 116382-116382. PubMed Europe PubMed DOI
Zhang,M., He,S., Han,C., Wu,Y., Cui,J., Feng,L., Huo,X., Li,D., Chen,Q., Ma,X. and Wang,C.
High-Throughput Screening of DPPIV Inhibitors Antagonizing GLP-1 Degradation Using an Enzymatic Activated Fluorescent Probe
Anal Chem (2024) PubMed Europe PubMed DOI
Zhang,M., Yue,X., Xu,S., Piao,J., Zhao,L., Shu,S., Kuzuya,M., Li,P., Hong,L., Kim,W., Liu,B. and Cheng,X.W.
Dipeptidyl peptidase-4 disturbs adipocyte differentiation via the negative regulation of the glucagon-like peptide-1/adiponectin-cathepsin K axis in mice under chronic stress conditions
FASEB J (2024) 38, e23684-e23684. PubMed Europe PubMed DOI

2023

Cambier,S., Beretta,F., Portner,N., Metzemaekers,M., de Carvalho,A.C., Martens,E., Kaes,J., Aelbrecht,C., Jacobs,C., Van Mol,P., Wauters,E., Meersseman,P., Hermans,G., Marques,R.E., Vanaudenaerde,B., Vos,R., Wauters,J., Gouwy,M. and Proost,P.
Proteolytic inactivation of CXCL12 in the lungs and circulation of COVID-19 patients
Cell Mol Life Sci (2023) 80, 234-234. PubMed Europe PubMed DOI I
Castle,A.R., Kang,S.G., Eskandari-Sedighi,G., Wohlgemuth,S., Nguyen,M.A., Drucker,D.J., Mulvihill,E.E. and Westaway,D.
Beta-endoproteolysis of the cellular prion protein by dipeptidyl peptidase-4 and fibroblast activation protein
Proc Natl Acad Sci U S A (2023) 120, e2209815120-e2209815120. PubMed Europe PubMed DOI PMC EPMC
Chen,Y.H., Zhang,X., Chou,C.H., Hsueh,M.F., Attarian,D., Li,Y.J. and Kraus,V.B.
Association of Dipeptidylpeptidase 4 (CD26) With Chondrocyte Senescence and Radiographic Progression in Knee Osteoarthritis
Arthritis Rheumatol (2023) 75, 1120-1131. PubMed Europe PubMed DOI
Fadzeyeva,E., Locatelli,C.A.A., Trzaskalski,N.A., Nguyen,M.A., Capozzi,M.E., Vulesevic,B., Morrow,N.M., Ghorbani,P., Hanson,A.A., Lorenzen-Schmidt,I., Doyle,M.A., Seymour,R., Varin,E.M., Fullerton,M.D., Campbell,J.E. and Mulvihill,E.E.
Pancreas-derived DPP4 is not essential for glucose homeostasis under metabolic stress
iScience (2023) 26, 106748-106748. PubMed Europe PubMed DOI PMC EPMC
Gonzatti,M.B., Junior,J.E.M., Rocha,A.J., de Oliveira,J.S., Evangelista,A.J.J., Fonseca,F.M.P., Ceccatto,V.M., de Oliveira,A.C. and da Cruz Freire,J.E.
Mechanism of molecular interaction of sitagliptin with human DPP(4) enzyme - New Insights
Adv Med Sci (2023) 68, 402-408. PubMed Europe PubMed DOI I
Guan,C., Luo,J., Li,S., Tan,Z.L., Wang,Y., Chen,H., Yamamoto,N., Zhang,C., Lu,Y., Chen,J. and Xing,X.H.
Exploration of DPP-IV Inhibitory Peptide Design Rules Assisted by the Deep Learning Pipeline That Identifies the Restriction Enzyme Cutting Site
ACS Omega (2023) 8, 39662-39672. PubMed Europe PubMed DOI PMC EPMC
Li,J., Ma,M., Li,J., Xu,L., Song,D., Ma,P. and Fei,Q.
Visualizing Dipeptidyl Peptidase-IV with an Advanced Non-pi-Conjugated Fluorescent Probe for Early Thyroid Disease Diagnosis
Anal Chem (2023) 95, 17577-17585. PubMed Europe PubMed DOI
Li,Q., Deng,X., Xu,Y.J. and Dong,L.
Development of Long-Acting Dipeptidyl Peptidase-4 Inhibitors: Structural Evolution and Long-Acting Determinants
J Med Chem (2023) 66, 11593-11631. PubMed Europe PubMed DOI
Prajapati,N., Sharma,D., Ashok Bidve,P., Chouhan,D., Allani,M., Kumar Patel,S., Ghosh Chowdhury,M., Shard,A. and Tiwari,V.
Glucose regulation by newly synthesized boronic acid functionalized molecules as dipeptidyl peptidase IV inhibitor: a potential compound for therapeutic intervention in hyperglycaemia
J Biomol Struct Dyn (2023) , 1-13. PubMed Europe PubMed DOI
Yue,L., Chen,F., Liu,X., Wu,C., Wang,J., Lai,J. and Zhu,H.
miR-23b-3p Ameliorates LPS-Induced Pulmonary Fibrosis by Inhibiting EndMT via DPP4 Inhibition
Mol Biotechnol (2023) PubMed Europe PubMed DOI

2022

Alves,E.S., Tonet-Furioso,A.C., Alves,V.P., Moraes,C.F., Perez,D.I.V., Bastos,I.M.D., Cordova,C. and Nobrega,O.T.
A haplotype in the dipeptidyl peptidase 4 gene impacts glycemic-related traits of Brazilian older adults
Braz J Med Biol Res (2022) 55, e12148-e12148. PubMed Europe PubMed DOI PMC EPMC
Benramdane,S., De Loose,J., Beyens,O., Van Rymenant,Y., Vliegen,G., Augustyns,K., De Winter,H., De Meester,I. and Van der Veken,P.
Vildagliptin-Derived Dipeptidyl Peptidase 9 (DPP9) Inhibitors: Identification of a DPP8/9-Specific Lead
ChemMedChem (2022) 17, e202200097-e202200097. PubMed Europe PubMed DOI I
Bernstein,H.G., Keilhoff,G., Dobrowolny,H. and Steiner,J.
The many facets of CD26/dipeptidyl peptidase 4 and its inhibitors in disorders of the CNS - a critical overview
Rev Neurosci (2022) 34, 1-24. PubMed Europe PubMed DOI V
Bhargave,A., Devi,K., Ahmad,I., Yadav,A. and Gupta,R.
Genetic variation in DPP-IV gene linked to predisposition of T2DM: A case control study
J Diabetes Metab Disord (2022) 21, 1709-1716. PubMed Europe PubMed DOI PMC EPMC
Huang,J., Liu,X., Wei,Y., Li,X., Gao,S., Dong,L., Rao,X. and Zhong,J.
Emerging Role of Dipeptidyl Peptidase-4 in Autoimmune Disease
Front Immunol (2022) 13, 830863-830863. PubMed Europe PubMed DOI PMC EPMC V
Maslov,I.O., Zinevich,T.V., Kirichenko,O.G., Trukhan,M.V., Shorshnev,S.V., Tuaeva,N.O., Gureev,M.A., Dahlen,A.D., Porozov,Y.B., Schioth,H.B. and Trukhan,V.M.
Design, Synthesis and Biological Evaluation of Neogliptin, a Novel 2-Azabicyclo[2.2.1]heptane-Based Inhibitor of Dipeptidyl Peptidase-4 (DPP-4)
Pharmaceuticals (Basel) (2022) 15 PubMed Europe PubMed DOI PMC EPMC I
Masui,S., Yonezawa,A., Yokoyama,K., Iwamoto,N., Shimada,T., Onishi,A., Onizawa,H., Fujii,T., Murakami,K., Murata,K., Tanaka,M., Nakagawa,S., Hira,D., Itohara,K., Imai,S., Nakagawa,T., Hayakari,M., Matsuda,S., Morinobu,A., Terada,T. and Matsubara,K.
N-terminus of Etanercept is Proteolytically Processed by Dipeptidyl Peptidase-4
Pharm Res (2022) 39, 2541-2554. PubMed Europe PubMed DOI
Pan,J., Zhang,Q., Zhang,C., Yang,W., Liu,H., Lv,Z., Liu,J. and Jiao,Z.
Inhibition of Dipeptidyl Peptidase-4 by Flavonoids: Structure-Activity Relationship, Kinetics and Interaction Mechanism
Front Nutr (2022) 9, 892426-892426. PubMed Europe PubMed DOI PMC EPMC I
Sebastian-Martin,A., Sanchez,B.G., Mora-Rodriguez,J.M., Bort,A. and Diaz-Laviada,I.
Role of Dipeptidyl Peptidase-4 (DPP4) on COVID-19 Physiopathology
Biomedicines (2022) 10 PubMed Europe PubMed DOI PMC EPMC V
Shatizadeh Malekshahi,S., Yavarian,J. and Shafiei-Jandaghi,N.Z.
Usage of peptidases by SARS-CoV-2 and several human coronaviruses as receptors: A mysterious story
Biotechnol Appl Biochem (2022) 69, 124-128. PubMed Europe PubMed DOI
Yang,Q., Fu,B., Luo,D., Wang,H., Cao,H., Chen,X., Tian,L. and Yu,X.
The Multiple Biological Functions of Dipeptidyl Peptidase-4 in Bone Metabolism
Front Endocrinol (Lausanne) (2022) 13, 856954-856954. PubMed Europe PubMed DOI PMC EPMC V

2021

Alkin,N., Dunaevsky,Y., Elpidina,E., Beljakova,G., Tereshchenkova,V., Filippova,I. and Belozersky,M.
Proline-Specific Fungal Peptidases: Genomic Analysis and Identification of Secreted DPP4 in Alkaliphilic and Alkalitolerant Fungi
J Fungi (Basel) (2021) 7 PubMed Europe PubMed DOI PMC EPMC
Arshia, Fayyaz,S., Shaikh,M., Khan,K.M. and Choudhary,M.I.
Anti-glycemic potential of benzophenone thio/semicarbazone derivatives: synthesis, enzyme inhibition and ligand docking studies
J Biomol Struct Dyn (2021) , 1-12. PubMed Europe PubMed DOI I
Bardaweel,S.K., Hajjo,R. and Sabbah,D.A.
Sitagliptin: a potential drug for the treatment of COVID-19?
Acta Pharm (2021) 71, 175-184. PubMed Europe PubMed DOI I
Beumer,J., Geurts,M.H., Lamers,M.M., Puschhof,J., Zhang,J., van der Vaart,J., Mykytyn,A.Z., Breugem,T.I., Riesebosch,S., Schipper,D., van den Doel,P.B., de Lau,W., Pleguezuelos-Manzano,C., Busslinger,G., Haagmans,B.L. and Clevers,H.
A CRISPR/Cas9 genetically engineered organoid biobank reveals essential host factors for coronaviruses
Nat Commun (2021) 12, 5498-5498. PubMed Europe PubMed DOI PMC EPMC
Cameron,K., Rozano,L., Falasca,M. and Mancera,R.L.
Does the SARS-CoV-2 Spike Protein Receptor Binding Domain Interact Effectively with the DPP4 (CD26) Receptor? A Molecular Docking Study
Int J Mol Sci (2021) 22 PubMed Europe PubMed DOI PMC EPMC
Cao,W., Chen,X., Chin,Y., Zheng,J., Lim,P.E., Xue,C. and Tang,Q.
Identification of curcumin as a potential alpha-glucosidase and dipeptidyl-peptidase 4 inhibitor: Molecular docking study, in vitro and in vivo biological evaluation
J Food Biochem (2021) , e13686-e13686. PubMed Europe PubMed DOI I
Choudhary,S., Sreenivasulu,K., Mitra,P., Misra,S. and Sharma,P.
Role of Genetic Variants and Gene Expression in the Susceptibility and Severity of COVID-19
Ann Lab Med (2021) 41, 129-138. PubMed Europe PubMed DOI PMC EPMC
Francis,P. and Chakraborty,K.
Clathriketal, a new tricyclic spiroketal compound from marine sponge Clathria prolifera attenuates serine exopeptidase dipeptidyl peptidase-IV
Nat Prod Res (2021) , 1-9. PubMed Europe PubMed DOI I
Fuh,M.T., Tseng,C.C., Li,S.M., Tsai,S.E., Chuang,T.J., Lu,C.H., Yang,Y.C., Tsai,H.J. and Wong,F.F.
Design, synthesis and biological evaluation of glycolamide, glycinamide, and beta-amino carbonyl 1,2,4-triazole derivatives as DPP-4 inhibitors
Bioorg Chem (2021) 114, 105049-105049. PubMed Europe PubMed DOI
Gurgel Penaforte-Saboia,J., Couri,C.E.B., Vasconcelos Albuquerque,N., Lauanna Lima Silva,V., Bitar da Cunha Olegario,N., Oliveira Fernandes,V. and Montenegro Junior,R.M.
Emerging Roles of Dipeptidyl Peptidase-4 Inhibitors in Delaying the Progression of Type 1 Diabetes Mellitus
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Herz,C.T., Brix,J.M., Ludvik,B., Schernthaner,G. and Schernthaner,G.H.
Decrease of dipeptidyl peptidase 4 activity is associated with weight loss after bariatric surgery
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Hu,X., Chen,S., Xie,C., Li,Z., Wu,Z. and You,Z.
DPP4 gene silencing inhibits proliferation and epithelial-mesenchymal transition of papillary thyroid carcinoma cells through suppression of the MAPK pathway
J Endocrinol Invest (2021) PubMed Europe PubMed DOI K
Iwanaga,T. and Nio-Kobayashi,J.
Cellular expression of CD26/dipeptidyl peptidase IV
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Lau,S.K.P., Fan,R.Y.Y., Zhu,L., Li,K.S.M., Wong,A.C.P., Luk,H.K.H., Wong,E.Y.M., Lam,C.S.F., Lo,G.C.S., Fung,J., He,Z., Fok,F.C.H., Au-Yeung,R.K.H., Zhang,L., Kok,K.H., Yuen,K.Y. and Woo,P.C.Y.
Isolation of MERS-related coronavirus from lesser bamboo bats that uses DPP4 and infects human-DPP4-transgenic mice
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Li,T.T., Peng,C., Wang,J.Q., Xu,Z.J., Su,M.B., Li,J., Zhu,W.L. and Li,J.Y.
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Love,K.M. and Liu,Z.
DPP4 Activity, Hyperinsulinemia and Atherosclerosis
J Clin Endocrinol Metab (2021) PubMed Europe PubMed DOI V
Lugowska,A., Baydakova,G., Ilyushkina,A., Zakharova,E., Mierzewska,H., Szymanska,K., Wierzba,J., Kubalska,J., Graban,A., Kmiec,T., Perkowska-Sumila,B., Tylki-Szymanska,A. and Bednarska-Makaruk,M.
Elevated Dipeptidyl Peptidase IV (DPP-IV) Activity in Plasma from Patients with Various Lysosomal Diseases
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Ngetich,E., Lapolla,P., Chandrashekar,A., Handa,A. and Lee,R.
The role of dipeptidyl peptidase-IV in abdominal aortic aneurysm pathogenesis: A systematic review
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Pan,K., Ohnuma,K., Morimoto,C. and Dang,N.H.
CD26/Dipeptidyl Peptidase IV and Its Multiple Biological Functions
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Scheen,A.J.
DPP-4 inhibition and COVID-19: From initial concerns to recent expectations
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Schmiedl,A., Wagener,I., Jungen,M., von Horsten,S. and Stephan,M.
Lung development and immune status under chronic LPS exposure in rat pups with and without CD26/DPP4 deficiency
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Singh,A.K., Yadav,D., Sharma,N. and Jin,J.O.
Dipeptidyl Peptidase (DPP)-IV Inhibitors with Antioxidant Potential Isolated from Natural Sources: A Novel Approach for the Management of Diabetes
Pharmaceuticals (Basel) (2021) 14 PubMed Europe PubMed DOI PMC EPMC V
Tomovic,K., Ilic,B.S. and Smelcerovic,A.
Structure-Activity Relationship Analysis of Cocrystallized Gliptin-like Pyrrolidine, Trifluorophenyl, and Pyrimidine-2,4-Dione Dipeptidyl Peptidase-4 Inhibitors
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Torrecillas-Baena,B., Galvez-Moreno,M.A., Quesada-Gomez,J.M., Dorado,G. and Casado-Diaz,A.
Influence of Dipeptidyl Peptidase-4 (DPP4) on Mesenchymal Stem-Cell (MSC) Biology: Implications for Regenerative Medicine - Review
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Vorstandlechner,V., Laggner,M., Copic,D., Klas,K., Direder,M., Chen,Y., Golabi,B., Haslik,W., Radtke,C., Tschachler,E., Hotzenecker,K., Ankersmit,H.J. and Mildner,M.
The serine proteases dipeptidyl-peptidase 4 and urokinase are key molecules in human and mouse scar formation
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Wang,J., Zhang,L., Qu,Y., Yang,Y., Cao,T., Cao,Y., Iqbal,A., Qin,W. and Liu,Y.
Long-Wavelength Ratiometric Fluorescent Probe for the Early Diagnosis of Diabetes
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Yang,X., Zhu,Y., Shi,Q., Zhao,X., Huang,Y., Yao,F., Zhang,Y. and Wang,Z.
Dipeptidyl peptidase IV is required for endometrial carcinoma cell proliferation and tumorigenesis via the IL-6/STAT3 pathway
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Yoshihara,M., Mizutani,S., Kato,Y., Matsumoto,K., Mizutani,E., Mizutani,H., Fujimoto,H., Osuka,S. and Kajiyama,H.
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The Roles of Dipeptidyl Peptidase 4 (DPP4) and DPP4 Inhibitors in Different Lung Diseases: New Evidence
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2020

Abdel Motaal,A., Salem,H.H., Almaghaslah,D., Alsayari,A., Bin Muhsinah,A., Alfaifi,M.Y., Elbehairi,S.E.I., Shati,A.A. and El-Askary,H.
Flavonol Glycosides: In Vitro Inhibition of DPPIV, Aldose Reductase and Combating Oxidative Stress are Potential Mechanisms for Mediating the Antidiabetic Activity of Cleome droserifolia
Molecules (2020) 25 PubMed Europe PubMed DOI PMC EPMC I
Ahmad,I., Arifianti,A.E., Sakti,A.S., Saputri,F.C. and Mun'im,A.
Simultaneous Natural Deep Eutectic Solvent-Based Ultrasonic-Assisted Extraction of Bioactive Compounds of Cinnamon Bark and Sappan Wood as a Dipeptidyl Peptidase IV Inhibitor
Molecules (2020) 25 PubMed Europe PubMed DOI I
Alsamghan,A.S., Alwabli,A.S., Abadi,M., Alsaleem,S.A., Anbari,D.M., Alomari,A.S., Alzahrani,O., Alam,Q. and Tarique,M.
From sequence analysis of DPP-4 to molecular docking based searching of its inhibitors
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Araki,M., Kanegawa,N., Iwata,H., Sagae,Y., Ito,K., Masuda,K. and Okuno,Y.
Hydrophobic interactions at subsite S1' of human dipeptidyl peptidase IV contribute significantly to the inhibitory effect of tripeptides
Heliyon (2020) 6, e04227-e04227. PubMed Europe PubMed DOI PMC EPMC
Asiabi,P., Dolmans,M.M., Ambroise,J., Camboni,A. and Amorim,C.A.
In vitro differentiation of theca cells from ovarian cells isolated from postmenopausal women
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Baggio,L.L., Varin,E.M., Koehler,J.A., Cao,X., Lokhnygina,Y., Stevens,S.R., Holman,R.R. and Drucker,D.J.
Plasma levels of DPP4 activity and sDPP4 are dissociated from inflammation in mice and humans
Nat Commun (2020) 11, 3766-3766. PubMed Europe PubMed DOI I
Balazki,P., Schaller,S., Eissing,T. and Lehr,T.
A Physiologically-Based Quantitative Systems Pharmacology Model of the Incretin Hormones GLP-1 and GIP and the DPP4 Inhibitor Sitagliptin
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Barchetta,I., Ceccarelli,V., Cimini,F.A., Barone,E., Sentinelli,F., Coluzzi,M., Chiappetta,C., Bertoccini,L., Tramutola,A., Labbadia,G., Di Cristofano,C., Silecchia,G., Leonetti,F. and Cavallo,M.G.
Circulating dipeptidyl peptidase-4 is independently associated with the presence and severity of NAFLD/NASH in individuals with and without obesity and metabolic disease
J Endocrinol Invest (2020) PubMed Europe PubMed DOI
Bindu,B., Vijayalakshmi,S. and Manikandan,A.
Synthesis and discovery of triazolo-pyridazine-6-yl-substituted piperazines as effective anti-diabetic drugs; evaluated over dipeptidyl peptidase-4 inhibition mechanism and insulinotropic activities
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Carr,R.D. and Solomon,A.
Inhibitors of dipeptidyl peptidase-4 as therapeutic agents for individuals with type 2 diabetes: a 25-year journey
Diabet Med (2020) PubMed Europe PubMed DOI I
Charoenkwan,P., Kanthawong,S., Nantasenamat,C., Hasan,M.M. and Shoombuatong,W.
iDPPIV-SCM: A Sequence-Based Predictor for Identifying and Analyzing Dipeptidyl Peptidase IV (DPP-IV) Inhibitory Peptides Using a Scoring Card Method
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Chen,L., Zhang,X., Zhang,L. and Zheng,D.
Effect of Saxagliptin, a Dipeptidyl Peptidase 4 Inhibitor, on Non-Alcoholic Fatty Liver Disease
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Deacon,C.F.
Dipeptidyl peptidase 4 inhibitors in the treatment of type 2 diabetes mellitus
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Devarakonda,C.K.V., Meredith,E., Ghosh,M. and Shapiro,L.H.
Coronavirus Receptors as Immune Modulators
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Du,H., Wang,D.W. and Chen,C.
The potential effects of DPP-4 inhibitors on cardiovascular system in COVID-19 patients
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Du,J., Fu,L., Ji,F., Wang,C., Liu,S. and Qiu,X.
FosB recruits KAT5 to potentiate the growth and metastasis of papillary thyroid cancer in a DPP4-dependent manner
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Dunaevsky,Y.E., Tereshchenkova,V.F., Oppert,B., Belozersky,M.A., Filippova,I.Y. and Elpidina,E.N.
Human proline specific peptidases: a comprehensive analysis
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Franco,R., Lillo,A., Rivas-Santisteban,R., Rodriguez-Perez,A.I., Reyes-Resina,I., Labandeira-Garcia,J.L. and Navarro,G.
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Gomaa,S.H., Abaza,M.M., Elattar,H.A., Amin,G.A. and Elshahawy,D.M.
Soluble cluster of differentiation 26/soluble dipeptidyl peptidase-4 and glypican-3 are promising serum biomarkers for the early detection of Hepatitis C virus related hepatocellular carcinoma in Egyptians
Arab J Gastroenterol (2020) PubMed Europe PubMed DOI
Guan,G.Y., Wei,N., Song,T., Zhao,C., Sun,Y., Pan,R.X., Zhang,L.L., Xu,Y.Y., Dai,Y.M. and Han,H.
miR-448-3p alleviates diabetic vascular dysfunction by inhibiting endothelial-mesenchymal transition through DPP-4 dysregulation
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Guo,X., Mu,S., Li,J., Zhang,Y., Liu,X., Zhang,H. and Gao,H.
Fabrication of a water-soluble near-infrared fluorescent probe for selective detection and imaging of dipeptidyl peptidase IV in biological systems
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Gupta,A., Narkowicz,C.K., Al-Aubaidy,H.A., Jelinek,H.F., Nichols,D.S., Burgess,J.R. and Jacobson,G.A.
Phytosterol supplements do not inhibit dipeptidyl peptidase-4
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Jiang,S., Wu,X., Wang,Y., Zou,J. and Zhao,X.
The potential DPP-4 inhibitors from Xiao-Ke-An improve the glucolipid metabolism via the activation of AKT/GSK-3beta pathway
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Khalaf,R.A., Masalha,D. and Sabbah,D.
DPP-IV Inhibitory phenanthridines: ligand, structure-based design, and synthesis
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Khalaf,R.A., Jarad,H.A., Al-Qirim,T. and Sabbah,D.
Synthesis, Biological Evaluation, and QPLD Studies of Piperazine Derivatives as Potential DPP-IV Inhibitors
Med Chem (2020) PubMed Europe PubMed DOI I
Kim,J., Yang,Y.L., Jeong,Y. and Jang,Y.S.
Conjugation of Human beta-Defensin 2 to Spike Protein Receptor-Binding Domain Induces Antigen-Specific Protective Immunity against Middle East Respiratory Syndrome Coronavirus Infection in Human Dipeptidyl Peptidase 4 Transgenic Mice
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Kluess,H.A.
Dipeptidyl peptidase IV as a muscle myokine
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Lettau,M., Dietz,M., Vollmers,S., Armbrust,F., Peters,C., Dang,T.M., Chitadze,G., Kabelitz,D. and Janssen,O.
Degranulation of human cytotoxic lymphocytes is a major source of proteolytically active soluble CD26/DPP4
Cell Mol Life Sci (2020) 77, 751-764. PubMed Europe PubMed DOI
Maremanda,K.P., Sundar,I.K., Li,D. and Rahman,I.
Age-dependent assessment of genes involved in cellular senescence, telomere and mitochondrial pathways in human lung tissue of smokers, COPD and IPF: Associations with SARS-CoV-2 COVID-19 ACE2-TMPRSS2-Furin-DPP4 axis
Res Sq (2020) PubMed Europe PubMed DOI PMC EPMC
Melo,F.J., Pinto-Lopes,P., Estevinho,M.M. and Magro,F.
The Role of Dipeptidyl Peptidase 4 as a Therapeutic Target and Serum Biomarker in Inflammatory Bowel Disease: A Systematic Review
Inflamm Bowel Dis (2020) PubMed Europe PubMed DOI V
Mendez,L.R., Arrebola,Y., Valdes-Tresanco,M.E., Diaz-Guevara,L., Bergado,G., Sanchez,B., Charli,J.L. and Alonso,I.P.
Bestatin and bacitracin inhibit porcine kidney cortex dipeptidyl peptidase IV activity and reduce human melanoma MeWo cell viability
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Moffitt,L.R., Bilandzic,M., Wilson,A.L., Chen,Y., Gorrell,M.D., Oehler,M.K., Plebanski,M. and Stephens,A.N.
Hypoxia Regulates DPP4 Expression, Proteolytic Inactivation, and Shedding from Ovarian Cancer Cells
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Mozafari,N., Azadi,S., Mehdi-Alamdarlou,S., Ashrafi,H. and Azadi,A.
Inflammation: A bridge between diabetes and COVID-19, and possible management with sitagliptin
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Nicotera,R., Casarella,A., Longhitano,E., Bolignano,D., Andreucci,M., De Sarro,G., Cernaro,V., Russo,E. and Coppolino,G.
Antiproteinuric effect of DPP-IV inhibitors in diabetic and non-diabetic kidney diseases
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Pantaleao,S.Q., Philot,E.A., de Oliveira Almeida,M., Lima,A.N., de Sairre,M.I., Scott,A.L. and Honorio,K.M.
Integrated protocol to design potential inhibitors of dipeptidyl peptidase-4 (DPP-4)
Curr Top Med Chem (2020) 20, 209-226. PubMed Europe PubMed DOI I
Patel,P.M., Jones,V.A., Kridin,K. and Amber,K.T.
The role of Dipeptidyl Peptidase-4 in cutaneous disease
Exp Dermatol (2020) PubMed Europe PubMed DOI V
Raha,A.A., Chakraborty,S., Henderson,J., Mukaetova-Ladinska,E., Zaman,S., Trowsdale,J. and Raha-Chowdhury,R.
Investigation of CD26, a potential SARS-CoV-2 receptor, as a biomarker of age and pathology
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Roncati,L. and Lusenti,B.
The <<moonlighting protein>> able to explain the Th1 immune lockdown in severe COVID-19
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Senapati,S., Kumar,S., Singh,A.K., Banerjee,P. and Bhagavatula,S.
Assessment of risk conferred by coding and regulatory variations of TMPRSS2 and CD26 in susceptibility to SARS-CoV-2 infection in human
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DPP4 inhibition: preventing SARS-CoV-2 infection and/or progression of COVID-19?
Diabetes Metab Res Rev (2020) 36, e3330-e3330. PubMed Europe PubMed DOI
Sun,Z.G., Li,Z.N. and Zhu,H.L.
The Research Progress of DPP-4 Inhibitors
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Tomovic,K., Ilic,B.S., Smelcerovic,Z., Miljkovic,M., Yancheva,D., Kojic,M., Mavrova,A.T., Kocic,G. and Smelcerovic,A.
Benzimidazole-based dual dipeptidyl peptidase-4 and xanthine oxidase inhibitors
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Valencia,I., Peiro,C., Lorenzo,O., Sanchez-Ferrer,C.F., Eckel,J. and Romacho,T.
DPP4 and ACE2 in Diabetes and COVID-19: Therapeutic Targets for Cardiovascular Complications?
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Wicik,Z., Eyileten,C., Jakubik,D., Simoes,S.N., Martins,D.C., Jr., Pavao,R., Siller-Matula,J.M. and Postula,M.
ACE2 Interaction Networks in COVID-19: A Physiological Framework for Prediction of Outcome in Patients with Cardiovascular Risk Factors
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Wong,C.K.H., Man,K.K.C., Chan,E.W.Y., Wu,T., Tse,E.T.Y., Wong,I.C.K. and Lam,C.L.K.
DPP4i, thiazolidinediones, or insulin and risks of cancer in patients with type 2 diabetes mellitus on metformin-sulfonylurea dual therapy with inadequate control
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Xi,C.R., Di Fazio,A., Nadvi,N.A., Patel,K., Xiang,M.S.W., Zhang,H.E., Deshpande,C., Low,J.K.K., Wang,X.T., Chen,Y., McMillan,C.L.D., Isaacs,A., Osborne,B., Vieira de Ribeiro,A.J., McCaughan,G.W., Mackay,J.P., Church,W.B. and Gorrell,M.D.
A Novel Purification Procedure for Active Recombinant Human DPP4 and the Inability of DPP4 to Bind SARS-CoV-2
Molecules (2020) 25 PubMed Europe PubMed DOI PMC EPMC
Yamamoto,K., Ohnishi,S., Mizushima,T., Kodaira,J., Ono,M., Hatanaka,Y., Hatanaka,K.C., Kuriki,Y., Kamiya,M., Ehira,N., Shinada,K., Takahashi,H., Shimizu,Y., Urano,Y. and Sakamoto,N.
Detection of early adenocarcinoma of the esophagogastric junction by spraying an enzyme-activatable fluorescent probe targeting dipeptidyl peptidase-IV
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Yip,H.K., Lee,M.S., Li,Y.C., Shao,P.L., Chiang,J.Y., Sung,P.H., Yang,C.H. and Chen,K.H.
Dipeptidyl Peptidase-4 deficiency effectively protects the brain and neurological function in rodent after acute Hemorrhagic Stroke
Int J Biol Sci (2020) 16, 3116-3132. PubMed Europe PubMed DOI PMC EPMC
Yoon,H., Cho,S.H., Seo,Y.R., Yu,K.S., Park,S.S. and Song,M.J.
Optimization and validation of a fluorogenic dipeptidyl peptidase 4 enzymatic assay in human plasma
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Zeng,S., Dou,W., Li,M., Zhou,Y., Guo,J., Zhao,N., Huang,H., Zhou,Q., Hu,W., Ma,Y., Zhao,X. and Xie,H.
Discovery of an Orally Active and Long-Acting DPP-IV Inhibitor through Property-Based Optimization with an in Silico Biotransformation Prediction Tool
ChemMedChem (2020) 15, 1608-1617. PubMed Europe PubMed DOI I
Zhao,Y., Zou,J., Song,Y., Peng,J., Wang,Y. and Bi,Y.
A novel label-free fluorescence assay for dipeptidyl peptidase 4 activity detection based on supramolecular self-assembly
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2019

Ahren,B.
DPP-4 Inhibition and the path to clinical proof
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Critical role of dipeptidyl peptidase IV: a therapeutic target for diabetes and cancer
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Deng,X., Wang,N., Meng,L., Zhou,S., Huang,J., Xing,J., He,L., Jiang,W. and Li,Q.
Optimization of the benzamide fragment targeting the S2' site leads to potent dipeptidyl peptidase-IV inhibitors
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Rapid detection of DPP-IV activity in porcine serum: a fluorospectrometric assay
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Elmansi,A.M., Awad,M.E., Eisa,N.H., Kondrikov,D., Hussein,K.A., Aguilar-Perez,A., Herberg,S., Periyasamy-Thandavan,S., Fulzele,S., Hamrick,M.W., McGee-Lawrence,M.E., Isales,C.M., Volkman,B.F. and Hill,W.D.
What doesn't kill you makes you stranger: dipeptidyl peptidase-4 (CD26) proteolysis differentially modulates the activity of many peptide hormones and cytokines generating novel cryptic bioactive ligands
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Gou,Z.P., Wang,Z.L., Liang,X.F., Zheng,L., Wang,Y. and Feng,P.
Single-dose escalation study of yogliptin in healthy Chinese volunteers
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Gupta,S. and Sen,U.
More than just an enzyme: dipeptidyl peptidase-4 (DPP-4) and its association with diabetic kidney remodelling
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Hollande,C., Boussier,J., Ziai,J., Nozawa,T., Bondet,V., Phung,W., Lu,B., Duffy,D., Paradis,V., Mallet,V., Eberl,G., Sandoval,W., Schartner,J.M., Pol,S., Barreira da Silva,R. and Albert,M.L.
Inhibition of the dipeptidyl peptidase DPP4 (CD26) reveals IL-33-dependent eosinophil-mediated control of tumor growth
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Huang,F., Ning,M., Wang,K., Liu,J., Guan,W., Leng,Y. and Shen,J.
Discovery of highly polar beta-homophenylalanine derivatives as nonsystemic intestine-targeted dipeptidyl peptidase IV inhibitors
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Kong,F., Pang,X., Zhao,J., Deng,P., Zheng,M., Zhong,D. and Chen,X.
Hydrolytic metabolism of cyanopyrrolidine DPP-4 inhibitors mediated by dipeptidyl peptidases
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Lu,Y., Lu,P., Wang,Y., Fang,X., Wu,J. and Wang,X.
A novel dipeptidyl peptidase IV inhibitory tea peptide improves pancreatic beta-cell function and reduces alpha-cell proliferation in streptozotocin-induced diabetic mice
Int J Mol Sci (2019) 20 PubMed Europe PubMed DOI I
Mishra,A., Cross,M., Hofmann,A., Coster,M.J., Karim,A. and Sattar,A.
Identification of a novel scaffold for inhibition of dipeptidyl peptidase-4
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Mohanty,I.R., Borde,M., Kumar C,S. and Maheshwari,U.
Dipeptidyl peptidase IV inhibitory activity of Terminalia arjuna attributes to its cardioprotective effects in experimental diabetes: in silico, in vitro and in vivo analyses
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Nieto-Fontarigo,J.J., Gonzalez-Barcala,F.J., San Jose,E., Arias,P., Nogueira,M. and Salgado,F.J.
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Red fluorescence probe targeted to dipeptidylpeptidase-IV for highly sensitive detection of esophageal cancer
Bioconjug Chem (2019) 30, 1055-1060. PubMed Europe PubMed DOI L
Sesti,G., Avogaro,A., Belcastro,S., Bonora,B.M., Croci,M., Daniele,G., Dauriz,M., Dotta,F., Formichi,C., Frontoni,S., Invitti,C., Orsi,E., Picconi,F., Resi,V., Bonora,E. and Purrello,F.
Ten years of experience with DPP-4 inhibitors for the treatment of type 2 diabetes mellitus
Acta Diabetol (2019) 56, 605-617. PubMed Europe PubMed DOI I
Sharma,S., Srivastava,S., Shrivastava,A., Malik,R., Almalki,F., Saifullah,K., Alam,M.M., Shaqiquzzaman,M., Ali,S. and Akhter,M.
Mining of potential dipeptidyl peptidase-IV inhibitors as anti-diabetic agents using integrated in silico approaches
J Biomol Struct Dyn (2019) , 1-13. PubMed Europe PubMed DOI I
Syam,Y.M., El-Karim,S.S.A., Nasr,T., Elseginy,S.A., Anwar,M.M., Kamel,M.M. and Ali,H.F.
Design, synthesis and biological evaluation of spiro cyclohexane-1,2-quinazoline derivatives as potent dipeptidyl peptidase IV inhibitors
Mini Rev Med Chem (2019) 19, 250-269. PubMed Europe PubMed DOI I
Tomovic,K., Ilic,B.S., Miljkovic,M., Dimov,S., Yancheva,D., Kojic,M., Mavrova,A.T., Kocic,G. and Smelcerovic,A.
Benzo[4,5]thieno[2,3-d]pyrimidine phthalimide derivative, one of the rare noncompetitive inhibitors of dipeptidyl peptidase-4
Arch Pharm (Weinheim) (2019) , e1900238-e1900238. PubMed Europe PubMed DOI I
Varin,E.M., Mulvihill,E.E., Beaudry,J.L., Pujadas,G., Fuchs,S., Tanti,J.F., Fazio,S., Kaur,K., Cao,X., Baggio,L.L., Matthews,D., Campbell,J.E. and Drucker,D.J.
Circulating levels of soluble dipeptidyl peptidase-4 are dissociated from inflammation and induced by enzymatic DPP4 inhibition
Cell Metab (2019) 29, 320-334. PubMed Europe PubMed DOI
Yang,F., Takagaki,Y., Yoshitomi,Y., Ikeda,T., Li,J., Kitada,M., Kumagai,A., Kawakita,E., Shi,S., Kanasaki,K. and Koya,D.
Inhibition of dipeptidyl peptidase-4 accelerates epithelial-mesenchymal transition and breast cancer metastasis via the CXCL12/CXCR4/mTOR axis
Cancer Res (2019) 79, 735-746. PubMed Europe PubMed DOI I
Yazbeck,R., Jaenisch,S., Squire,M., Abbott,C.A., Parkinson-Lawrence,E., Brooks,D.A. and Butler,R.N.
Development of a (13)C stable isotope assay for dipeptidyl peptidase-4 enzyme activity a new breath test for dipeptidyl peptidase activity
Sci Rep (2019) 9, 4906-4906. PubMed Europe PubMed DOI PMC EPMC A
Zhao,X., Zhang,K., Daniel,P., Wisbrun,N., Fuchs,H. and Fan,H.
Delayed allogeneic skin graft rejection in CD26-deficient mice
Cell Mol Immunol (2019) 16, 557-567. PubMed Europe PubMed DOI K

2018

Abd El-Karim,S.S., Anwar,M.M., Syam,Y.M., Nael,M.A., Ali,H.F. and Motaleb,M.A.
Rational design and synthesis of new tetralin-sulfonamide derivatives as potent anti-diabetics and DPP-4 inhibitors: 2D & 3D QSAR, in vivo radiolabeling and bio distribution studies
Bioorg Chem (2018) 81, 481-493. PubMed Europe PubMed DOI I
Casrouge,A., Sauer,A.V., Barreira da Silva,R., Tejera-Alhambra,M., Sanchez-Ramon,S., ICAReB, Cancrini,C., Ingersoll,M.A., Aiuti,A. and Albert,M.L.
Lymphocytes are a major source of circulating soluble dipeptidyl peptidase 4
Clin Exp Immunol (2018) 194, 166-179. PubMed Europe PubMed DOI
Cheng,A.C., Doherty,E.M., Johnstone,S., DiMauro,E.F., Dao,J., Luthra,A., Ye,J., Tang,J., Nixey,T., Min,X., Tagari,P., Miranda,L.P. and Wang,Z.
Structure-guided discovery of dual-recognition chemibodies
Sci Rep (2018) 8, 7570-7570. PubMed Europe PubMed DOI PMC EPMC
Deacon,C.F.
A review of dipeptidyl peptidase-4 inhibitors. Hot topics from randomized controlled trials
Diabetes Obes Metab (2018) 20 Suppl 1, 34-46. PubMed Europe PubMed DOI I
Deacon,C.F.
Peptide degradation and the role of DPP-4 inhibitors in the treatment of type 2 diabetes
Peptides (2018) 100, 150-157. PubMed Europe PubMed DOI I
Fan,C., Wu,X., Liu,Q., Li,Q., Liu,S., Lu,J., Yang,Y., Cao,Y., Huang,W., Liang,C., Ying,T., Jiang,S. and Wang,Y.
A human DPP4-knockin mouse's susceptibility to infection by authentic and pseudotyped MERS-CoV
Viruses (2018) 10 PubMed Europe PubMed DOI
Gupta,A., Jacobson,G.A., Burgess,J.R., Jelinek,H.F., Nichols,D.S., Narkowicz,C.K. and Al-Aubaidy,H.A.
Citrus bioflavonoids dipeptidyl peptidase-4 inhibition compared with gliptin antidiabetic medications
Biochem Biophys Res Commun (2018) 503, 21-25. PubMed Europe PubMed DOI I
Kalhotra,P., Chittepu,V.C.S.R., Osorio-Revilla,G. and Gallardo-Velazquez,T.
Structure(-)activity relationship and molecular docking of natural product library reveal chrysin as a novel dipeptidyl peptidase-4 (DPP-4) inhibitor: an integrated in silico and in vitro study
Molecules (2018) 23 PubMed Europe PubMed DOI I
Kato,E., Kawakami,K. and Kawabata,J.
Macrocarpal C isolated from Eucalyptus globulus inhibits dipeptidyl peptidase 4 in an aggregated form
J Enzyme Inhib Med Chem (2018) 33, 106-109. PubMed Europe PubMed DOI I
Khalaf,R.A., Sabbah,D., Al-Shalabi,E., Al-Sheikh,I., Albadawi,G. and Abu Sheikha,G.
Synthesis, structural characterization and docking studies of sulfamoyl-phenyl acid esters as dipeptidyl peptidase-IV inhibitors
Curr Comput Aided Drug Des (2018) 14, 142-151. PubMed Europe PubMed DOI I
Kuranov,S.O., Tsypysheva,I.P., Khvostov,M.V., Zainullina,L.F., Borisevich,S.S., Vakhitova,Y.V., Luzina,O.A. and Salakhutdinov,N.F.
Synthesis and evaluation of camphor and cytisine-based cyanopyrrolidines as DPP-IV inhibitors for the treatment of type 2 diabetes mellitus
Bioorg Med Chem (2018) 26, 4402-4409. PubMed Europe PubMed DOI I
Li,N., Wang,L.J., Jiang,B., Li,X.Q., Guo,C.L., Guo,S.J. and Shi,D.Y.
Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus
Eur J Med Chem (2018) 151, 145-157. PubMed Europe PubMed DOI I
Li,N., Wang,L.J., Jiang,B., Guo,S.J., Li,X.Q., Chen,X.C., Luo,J., Li,C., Wang,Y. and Shi,D.Y.
Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors
Bioorg Med Chem Lett (2018) 28, 2131-2135. PubMed Europe PubMed DOI I
Liu,T., Ning,J., Wang,B., Dong,B., Li,S., Tian,X., Yu,Z., Peng,Y., Wang,C., Zhao,X., Huo,X., Sun,C., Cui,J., Feng,L. and Ma,X.
Activatable near-infrared fluorescent probe for dipeptidyl peptidase IV and its bioimaging applications in living cells and animals
Anal Chem (2018) 90, 3965-3973. PubMed Europe PubMed DOI L
Luippold,G., Mark,M., Klein,T., Amann,K. and Daniel,C.
Differences in kidney-specific DPP-4 inhibition by linagliptin and sitagliptin
Diabetes Res Clin Pract (2018) 143, 199-203. PubMed Europe PubMed DOI I
Ohnuma,K., Hatano,R., Komiya,E., Otsuka,H., Itoh,T., Iwao,N., Kaneko,Y., Yamada,T., Dang,N.H. and Morimoto,C.
A novel role for CD26/dipeptidyl peptidase IV as a therapeutic target
Front Biosci (Landmark Ed) (2018) 23, 1754-1779. PubMed Europe PubMed T
Ojeda-Montes,M.J., Gimeno,A., Tomas-Hernandez,S., Cereto-Massague,A., Beltran-Debon,R., Valls,C., Mulero,M., Pujadas,G. and Garcia-Vallve,S.
Activity and selectivity cliffs for DPP-IV inhibitors: lessons we can learn from SAR studies and their application to virtual screening
Med Res Rev (2018) 38, 1874-1915. PubMed Europe PubMed DOI S I
Olivares,M., Schuppel,V., Hassan,A.M., Beaumont,M., Neyrinck,A.M., Bindels,L.B., Benitez-Paez,A., Sanz,Y., Haller,D., Holzer,P. and Delzenne,N.M.
The potential role of the dipeptidyl peptidase-4-like activity from the gut microbiota on the host health
Front Microbiol (2018) 9, 1900-1900. PubMed Europe PubMed DOI PMC EPMC
Pantaleao,S.Q., Philot,E.A., de Resende-Lara,P.T., Lima,A.N., Perahia,D., Miteva,M.A., Scott,A.L. and Honorio,K.M.
Structural dynamics of DPP-4 and its influence on the projection of bioactive ligands
Molecules (2018) 23 PubMed Europe PubMed DOI
Park,D.S., Kim,K., Jang,M. and Choi,S.C.
Role of dipeptidyl peptidase-4 as a potentiator of activin/nodal signaling pathway
BMB Rep (2018) 51, 636-641. PubMed Europe PubMed
Patil,R.B., Barbosa,E.G., Sangshetti,J.N., Zambre,V.P. and Sawant,S.D.
Structural insights of dipeptidyl peptidase-IV inhibitors through molecular dynamics-guided receptor-dependent 4D-QSAR studies
Mol Divers (2018) 22, 575-583. PubMed Europe PubMed DOI I
Rohilla,A., Gupta,T., Pathak,A., Akhtar,M.J., Haider,M.R., Haider,K. and Shahar Yar,M.
Emergence of promising novel DPP-4 inhibitory heterocycles as anti-diabetic agents: a review
Arch Pharm (Weinheim) (2018) , e1800127-e1800127. PubMed Europe PubMed DOI I
Salaga,M., Binienda,A., Draczkowski,P., Kosson,P., Kordek,R., Jozwiak,K. and Fichna,J.
Novel peptide inhibitor of dipeptidyl peptidase IV (Tyr-Pro-D-Ala-NH2) with anti-inflammatory activity in the mouse models of colitis
Peptides (2018) 108, 34-45. PubMed Europe PubMed DOI I
Svarcbahs,R., Julku,U.H., Norrbacka,S. and Myohanen,T.T.
Removal of prolyl oligopeptidase reduces alpha-synuclein toxicity in cells and in vivo
Sci Rep (2018) 8, 1552-1552. PubMed Europe PubMed DOI K
Turdu,G., Gao,H., Jiang,Y. and Kabas,M.
Plant dipeptidyl peptidase-IV inhibitors as antidiabetic agents: a brief review
Future Med Chem (2018) 10, 1229-1239. PubMed Europe PubMed DOI I
Wang,X., Zheng,P., Huang,G., Yang,L. and Zhou,Z.
Dipeptidyl peptidase-4(DPP-4) inhibitors: promising new agents for autoimmune diabetes
Clin Exp Med (2018) 18, 473-480. PubMed Europe PubMed DOI I
Xing,J., Gong,Q., Zhang,R., Sun,S., Zou,R. and Wu,A.
A novel non-enzymatic hydrolytic probe for dipeptidyl peptidase IV specific recognition and imaging
Chem Commun (Camb) (2018) 54, 8773-8776. PubMed Europe PubMed DOI A
Yang,L., Han,W., Luo,Y., Hu,X., Xu,Y., Li,H., Hu,C., Huang,D., Ma,J., Yang,Y., Chen,Q., Li,Y., Zhang,J., Xia,H., Chen,Z., Wang,H., Ran,D. and Yang,J.
Adapentpronitrile, a new dipeptidyl peptidase-IV inhibitor, ameliorates diabetic neuronal injury through inhibiting mitochondria-related oxidative stress and apoptosis
Front Cell Neurosci (2018) 12, 214-214. PubMed Europe PubMed DOI PMC EPMC I

2017

Akoumianakis,I. and Antoniades,C.
Dipeptidyl peptidase IV inhibitors as novel regulators of vascular disease
Vascul Pharmacol (2017) 96-98, 1-4. PubMed Europe PubMed DOI T
Aldewachi,H.S., Woodroofe,N., Turega,S. and Gardiner,P.H.E.
Optimization of gold nanoparticle-based real-time colorimetric assay of dipeptidyl peptidase IV activity
Talanta (2017) 169, 13-19. PubMed Europe PubMed DOI A
Ali,Z., Akhtar,M.J., Haider,M.R., Khan,A.A., Siddiqui,A.A. and Yar,M.S.
Design and synthesis of quinazoline-3,4-(4H)-diamine endowed with thiazoline moiety as new class for DPP-4 and DPPH inhibitor
Bioorg Chem (2017) 71, 181-191. PubMed Europe PubMed DOI I
Angevin,E., Isambert,N., Trillet-Lenoir,V., You,B., Alexandre,J., Zalcman,G., Vielh,P., Farace,F., Valleix,F., Podoll,T., Kuramochi,Y., Miyashita,I., Hosono,O., Dang,N.H., Ohnuma,K., Yamada,T., Kaneko,Y. and Morimoto,C.
First-in-human phase 1 of YS110, a monoclonal antibody directed against CD26 in advanced CD26-expressing cancers
Br J Cancer (2017) 116, 1126-1134. PubMed Europe PubMed DOI
Antonyan,A., Schlenzig,D., Schilling,S., Naumann,M., Sharoyan,S., Mardanyan,S. and Demuth,H.U.
Concerted action of dipeptidyl peptidase IV and glutaminyl cyclase results in formation of pyroglutamate-modified amyloid peptides in vitro
Neurochem Int (2017) 113, 112-119. PubMed Europe PubMed DOI
Bohm,A., Wagner,R., Machicao,F., Holst,J.J., Gallwitz,B., Stefan,N., Fritsche,A., Haring,H.U. and Staiger,H.
DPP4 gene variation affects GLP-1 secretion, insulin secretion, and glucose tolerance in humans with high body adiposity
PLoS ONE (2017) 12, e0181880-e0181880. PubMed Europe PubMed DOI M
Chandra,S., Pandey,J., Tamrakar,A.K. and Siddiqi,M.I.
SVMDLF: a novel R-based web application for prediction of dipeptidyl peptidase 4 inhibitors
Chem Biol Drug Des (2017) 90, 1173-1183. PubMed Europe PubMed DOI I
Deng,X., Han,L., Zhou,J., Zhang,H. and Li,Q.
Discovery of triazole-based uracil derivatives bearing amide moieties as novel dipeptidyl peptidase-IV inhibitors
Bioorg Chem (2017) 75, 357-367. PubMed Europe PubMed DOI I
Herlihy,S.E., Tang,Y., Phillips,J.E. and Gomer,R.H.
Functional similarities between the Dictyostelium protein AprA and the human protein dipeptidyl-peptidase IV
Protein Sci (2017) 26, 578-585. PubMed Europe PubMed DOI
Huan,Y., Jiang,Q., Li,G., Bai,G., Zhou,T., Liu,S., Li,C., Liu,Q., Sun,S., Yang,M., Guo,N., Wang,X., Wang,S., Liu,Y., Wang,G., Huang,H. and Shen,Z.
The dual DPP4 inhibitor and GPR119 agonist HBK001 regulates glycemic control and beta cell function ex and in vivo
Sci Rep (2017) 7, 4351-4351. PubMed Europe PubMed DOI PMC EPMC I
Jackson,E.K.
Context-dependent effects of dipeptidyl peptidase 4 inhibitors
Curr Opin Nephrol Hypertens (2017) 26, 83-90. PubMed Europe PubMed DOI I
Jain,M.R., Joharapurkar,A.A., Kshirsagar,S.G., Patel,V.J., Bahekar,R.H., Patel,H.V., Jadav,P.A., Patel,P.R. and Desai,R.C.
ZY15557 a novel long acting inhibitor of dipeptidyl peptidase-4 for the treatment of Type 2 diabetes mellitus
Br J Pharmacol (2017) 174, 2346-2357. PubMed Europe PubMed DOI I
Janssens,R., Mortier,A., Boff,D., Ruytinx,P., Gouwy,M., Vantilt,B., Larsen,O., Daugvilaite,V., Rosenkilde,M.M., Parmentier,M., Noppen,S., Liekens,S., Van Damme,J., Struyf,S., Teixeira,M.M., Amaral,F.A. and Proost,P.
Truncation of CXCL12 by CD26 reduces its CXC chemokine receptor 4- and atypical chemokine receptor 3-dependent activity on endothelial cells and lymphocytes
Biochem Pharmacol (2017) 132, 92-101. PubMed Europe PubMed DOI
Kim,K.M., Noh,J.H., Bodogai,M., Martindale,J.L., Yang,X., Indig,F.E., Basu,S.K., Ohnuma,K., Morimoto,C., Johnson,P.F., Biragyn,A., Abdelmohsen,K. and Gorospe,M.
Identification of senescent cell surface targetable protein DPP4
Genes Dev (2017) 31, 1529-1534. PubMed Europe PubMed DOI
Lei,Y., Hu,L., Yang,G., Piao,L., Jin,M. and Cheng,X.
Dipeptidyl peptidase-IV inhibition for the treatment of cardiovascular disease - recent insights focusing on angiogenesis and neovascularization
Circ J (2017) 81, 770-776. PubMed Europe PubMed DOI I
Maezaki,H., Tawada,M., Yamashita,T., Banno,Y., Miyamoto,Y., Yamamoto,Y., Ikedo,K., Kosaka,T., Tsubotani,S., Tani,A., Asakawa,T., Suzuki,N. and Oi,S.
Design of potent dipeptidyl peptidase IV (DPP-4) inhibitors by employing a strategy to form a salt bridge with Lys554
Bioorg Med Chem Lett (2017) 27, 3565-3571. PubMed Europe PubMed DOI I
Ogawa,F., Takeda,M., Miyanaga,K., Tani,K., Yamazawa,R., Ito,K., Tarui,A., Sato,K. and Omote,M.
Development of a fluorogenic small substrate for dipeptidyl peptidase-4
Beilstein J Org Chem (2017) 13, 2690-2697. PubMed Europe PubMed DOI PMC EPMC A
Patel,B.D., Bhadada,S.V. and Ghate,M.D.
Design, synthesis and anti-diabetic activity of triazolotriazine derivatives as dipeptidyl peptidase-4 (DPP-4) inhibitors
Bioorg Chem (2017) 72, 345-358. PubMed Europe PubMed DOI I
Rozano,L., Abdullah Zawawi,M.R., Ahmad,M.A. and Jaganath,I.B.
Computational analysis of Gynura bicolor bioactive compounds as dipeptidyl peptidase-IV inhibitor
Adv Bioinformatics (2017) 2017, 5124165-5124165. PubMed Europe PubMed DOI PMC EPMC I
Salaga,M., Mokrowiecka,A., Zielinska,M., Malecka-Panas,E., Kordek,R., Kamysz,E. and Fichna,J.
New peptide inhibitor of dipeptidyl peptidase IV, EMDB-1 extends the half-life of GLP-2 and attenuates colitis in mice after topical administration
J Pharmacol Exp Ther (2017) 363, 92-103. PubMed Europe PubMed DOI I
Sato,A. and Ogita,H.
Pathophysiological implications of dipeptidyl peptidases
Curr Protein Pept Sci (2017) 18, 843-849. PubMed Europe PubMed DOI
Sharma,M.C., Jain,S. and Sharma,R.
In silico screening for identification of pyrrolidine derivatives dipeptidyl peptidase-IV inhibitors using COMFA, CoMSIA, HQSAR and docking studies
In Silico Pharmacol (2017) 5, 13-13. PubMed Europe PubMed DOI PMC EPMC I
Uchida,T., Wakasugi,M., Kitamura,T., Yamamoto,T., Asakura,M., Fujiwara,R., Itoh,T., Fujii,H. and Hirono,S.
Exploration of DPP-IV inhibitors with a novel scaffold by multistep in silico screening
J Mol Graph Model (2017) 79, 254-263. PubMed Europe PubMed DOI I
Wang,Z., Jiang,J., Hu,P. and Zhao,Q.
Development and validation of a UPLC-MS/MS method for simultaneous determination of fotagliptin and its two major metabolites in human plasma and urine
Bioanalysis (2017) 9, 381-393. PubMed Europe PubMed I
Zou,L.W., Wang,P., Qian,X.K., Feng,L., Yu,Y., Wang,D.D., Jin,Q., Hou,J., Liu,Z.H., Ge,G.B. and Yang,L.
A highly specific ratiometric two-photon fluorescent probe to detect dipeptidyl peptidase IV in plasma and living systems
Biosens Bioelectron (2017) 90, 283-289. PubMed Europe PubMed DOI A

2016

An update on the 'gliptins'
Drug Ther Bull (2016) 54, 138-141. PubMed Europe PubMed DOI V I
Akinboye,E.S., Brennen,W.N., Rosen,D.M., Bakare,O. and Denmeade,S.R.
Iterative design of emetine-based prodrug targeting fibroblast activation protein (FAP) and dipeptidyl peptidase IV DPPIV using a tandem enzymatic activation strategy
Prostate (2016) 76, 703-714. PubMed Europe PubMed DOI
Amini,Z., Fatemi,M.H. and Gharaghani,S.
Hybrid docking-QSAR studies of DPP-IV inhibition activities of a series of aminomethyl-piperidones
Comput Biol Chem (2016) 64, 335-345. PubMed Europe PubMed DOI I
Arulmozhiraja,S., Matsuo,N., Ishitsubo,E., Okazaki,S., Shimano,H. and Tokiwa,H.
Comparative binding analysis of dipeptidyl peptidase IV (DPP-4) with antidiabetic drugs - an ab initio fragment molecular orbital study
PLoS ONE (2016) 11, e0166275-e0166275. PubMed Europe PubMed DOI I
Cox,J.M., Chu,H.D., Kuethe,J.T., Gao,Y.D., Scapin,G., Eiermann,G., He,H., Li,X., Lyons,K.A., Metzger,J., Petrov,A., Wu,J.K., Xu,S., Sinha-Roy,R., Weber,A.E. and Biftu,T.
The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors
Bioorg Med Chem Lett (2016) 26, 2622-2626. PubMed Europe PubMed DOI I
de Almeida Salles,T., Zogbi,C., de Lima,T.M., de Godoi Carneiro,C., Garcez,A.T., Barbeiro,H.V., Antonio,E.L., Dos Santos,L., da Costa Pereira,A., Tucci,P.J., de Paula Faria,D., Soriano,F.G. and Girardi,A.C.
The contributions of dipeptidyl peptidase IV to inflammation in heart failure
Am J Physiol Heart Circ Physiol (2016) 310, H1760-H1772. PubMed Europe PubMed DOI I
Deacon,C.F. and Lebovitz,H.E.
Comparative review of dipeptidyl peptidase-4 inhibitors and sulphonylureas
Diabetes Obes Metab (2016) 18, 333-347. PubMed Europe PubMed DOI I
Decalf,J., Tarbell,K.V., Casrouge,A., Price,J.D., Linder,G., Mottez,E., Sultanik,P., Mallet,V., Pol,S., Duffy,D. and Albert,M.L.
Inhibition of DPP4 activity in humans establishes its in vivo role in CXCL10 post-translational modification: prospective placebo-controlled clinical studies
EMBO Mol Med (2016) 8, 679-683. PubMed Europe PubMed DOI I
Glorie,L., D'Haese,P.C. and Verhulst,A.
Boning up on DPP4, DPP4 substrates, and DPP4-adipokine interactions: logical reasoning and known facts about bone related effects of DPP4 inhibitors
Bone (2016) 92, 37-49. PubMed Europe PubMed DOI V
Gonzalez,R. and Unniappan,S.
Mass spectrometry-assisted confirmation of the inability of dipeptidyl peptidase-4 to cleave goldfish peptide YY(1-36) and the lack of anorexigenic effects of peptide YY(3-36) in goldfish (Carassius auratus)
Fish Physiol Biochem (2016) 42, 831-844. PubMed Europe PubMed DOI
Grimshaw,C.E., Jennings,A., Kamran,R., Ueno,H., Nishigaki,N., Kosaka,T., Tani,A., Sano,H., Kinugawa,Y., Koumura,E., Shi,L. and Takeuchi,K.
Trelagliptin (SYR-472, Zafatek), novel once-weekly treatment for type 2 diabetes, inhibits dipeptidyl peptidase-4 (DPP-4) via a non-covalent mechanism
PLoS ONE (2016) 11, e0157509-e0157509. PubMed Europe PubMed DOI I
Ikeda,J., Kimoto,N., Kitayama,T. and Kunori,S.
Cardiac DPP-4 inhibition by saxagliptin ameliorates isoproterenol-induced myocardial remodeling and cardiac diastolic dysfunction in rats
J Pharmacol Sci (2016) 132, 65-70. PubMed Europe PubMed DOI I
Kato,E., Uenishi,Y., Inagaki,Y., Kurokawa,M. and Kawabata,J.
Isolation of rugosin A, B and related compounds as dipeptidyl peptidase-IV inhibitors from rose bud extract powder
Biosci Biotechnol Biochem (2016) 80, 2087-2092. PubMed Europe PubMed DOI I
Li,S., Xu,H., Cui,S., Wu,F., Zhang,Y., Su,M., Gong,Y., Qiu,S., Jiao,Q., Qin,C., Shan,J., Zhang,M., Wang,J., Yin,Q., Xu,M., Liu,X., Wang,R., Zhu,L., Li,J., Xu,Y., Jiang,H., Zhao,Z., Li,J. and Li,H.
Discovery and rational design of natural-product-derived 2-phenyl-3,4-dihydro-2h-benzo[f]chromen-3-amine analogs as novel and potent dipeptidyl peptidase 4 (DPP-4) inhibitors for the treatment of type 2 diabetes
J Med Chem (2016) 59, 6772-6790. PubMed Europe PubMed DOI I
Nojima,H., Kanou,K., Terashi,G., Takeda-Shitaka,M., Inoue,G., Atsuda,K., Itoh,C., Iguchi,C. and Matsubara,H.
Comprehensive analysis of the co-structures of dipeptidyl peptidase IV and its inhibitor
BMC Struct Biol (2016) 16, 11-11. PubMed Europe PubMed DOI PMC EPMC S I
Onoyama,H., Kamiya,M., Kuriki,Y., Komatsu,T., Abe,H., Tsuji,Y., Yagi,K., Yamagata,Y., Aikou,S., Nishida,M., Mori,K., Yamashita,H., Fujishiro,M., Nomura,S., Shimizu,N., Fukayama,M., Koike,K., Urano,Y. and Seto,Y.
Rapid and sensitive detection of early esophageal squamous cell carcinoma with fluorescence probe targeting dipeptidylpeptidase IV
Sci Rep (2016) 6, 26399-26399. PubMed Europe PubMed DOI PMC EPMC L
Pissarnitski,D.A., Zhao,Z., Cole,D., Wu,W.L., Domalski,M., Clader,J.W., Scapin,G., Voigt,J., Soriano,A., Kelly,T., Powles,M.A., Yao,Z. and Burnett,D.A.
Scaffold-hopping from xanthines to tricyclic guanines: a case study of dipeptidyl peptidase 4 (DPP4) inhibitors
Bioorg Med Chem (2016) 24, 5534-5545. PubMed Europe PubMed DOI I
Ran,Y., Pei,H., Shao,M. and Chen,L.
Synthesis, biological evaluation, and molecular docking of (R)-2-((8-(3-aminopiperidin-1-yl)-3-methyl-7-(3-methylbut-2-en-1-yl)-26-dioxo-2367-tetrahydro-1H-purin-1-yl)methyl)benzonitrile as dipeptidyl peptidase IV inhibitors
Chem Biol Drug Des (2016) 87, 290-295. PubMed Europe PubMed DOI I
Remm,F., Franz,W.M. and Brenner,C.
Gliptins and their target dipeptidyl peptidase 4: implications for the treatment of vascular disease
Eur Heart J Cardiovasc Pharmacother (2016) 2, 185-193. PubMed Europe PubMed DOI I
Schnapp,G., Klein,T., Hoevels,Y., Bakker,R.A. and Nar,H.
Comparative analysis of binding kinetics and thermodynamics of dipeptidyl peptidase-4 inhibitors and their relationship to structure
J Med Chem (2016) 59, 7466-7477. PubMed Europe PubMed DOI I
Shi,S., Kanasaki,K. and Koya,D.
Linagliptin but not Sitagliptin inhibited transforming growth factor-beta2-induced endothelial DPP-4 activity and the endothelial-mesenchymal transition
Biochem Biophys Res Commun (2016) 471, 184-190. PubMed Europe PubMed DOI I
Suman,R.K., Mohanty,I.R., Maheshwari,U., Borde,M.K. and Deshmukh,Y.A.
Natural dipeptidyl peptidase-IV inhibitor mangiferin mitigates diabetes- and metabolic syndrome-induced changes in experimental rats
Diabetes Metab Syndr Obes (2016) 9, 261-272. PubMed Europe PubMed DOI PMC EPMC
van Doremalen,N., Miazgowicz,K.L. and Munster,V.J.
Mapping the specific amino acid residues that make hamster DPP4 functional as a receptor for Middle East Respiratory Syndrome coronavirus
J Virol (2016) 90, 5499-5502. PubMed Europe PubMed DOI
Wagner,L., Klemann,C., Stephan,M. and von Horsten,S.
Unravelling the immunological roles of dipeptidyl peptidase 4 (DPP4) activity and/or structure homologue (DASH) proteins
Clin Exp Immunol (2016) 184, 265-283. PubMed Europe PubMed DOI
Wagner,L., Kaestner,F., Wolf,R., Stiller,H., Heiser,U., Manhart,S., Hoffmann,T., Rahfeld,J.U., Demuth,H.U., Rothermundt,M. and von Horsten,S.
Identifying neuropeptide Y (NPY) as the main stress-related substrate of dipeptidyl peptidase 4 (DPP4) in blood circulation
Neuropeptides (2016) 57, 21-34. PubMed Europe PubMed DOI
Wang,Y., Wu,X., Cheng,Y. and Zhao,X.
A fluorescent switchable AIE probe for selective imaging of dipeptidyl peptidase-4 in vitro and in vivo and its application in screening DPP-4 inhibitors
Chem Commun (Camb) (2016) 52, 3478-3481. PubMed Europe PubMed DOI L
Wong,P.F., Gall,M.G., Bachovchin,W.W., McCaughan,G.W., Keane,F.M. and Gorrell,M.D.
Neuropeptide Y is a physiological substrate of fibroblast activation protein: enzyme kinetics in blood plasma and expression of Y2R and Y5R in human liver cirrhosis and hepatocellular carcinoma
Peptides (2016) 75, 80-95. PubMed Europe PubMed DOI
Wu,W.L., Hao,J., Domalski,M., Burnett,D.A., Pissarnitski,D., Zhao,Z., Stamford,A., Scapin,G., Gao,Y.D., Soriano,A., Kelly,T.M., Yao,Z., Powles,M.A., Chen,S., Mei,H. and Hwa,J.
Discovery of novel tricyclic heterocycles as potent and selective DPP-4 inhibitors for the treatment of type 2 diabetes
ACS Med Chem Lett (2016) 7, 498-501. PubMed Europe PubMed DOI PMC EPMC I
Zhong,J., Kankanala,S. and Rajagopalan,S.
Dipeptidyl peptidase-4 inhibition: insights from the bench and recent clinical studies
Curr Opin Lipidol (2016) 27, 484-492. PubMed Europe PubMed DOI I

2015

Asakura,M., Fujii,H., Atsuda,K., Itoh,T. and Fujiwara,R.
Dipeptidyl peptidase-4 greatly contributes to the hydrolysis of vildagliptin in human liver
Drug Metab Dispos (2015) 43, 477-484. PubMed Europe PubMed DOI I
Barreira da Silva,R., Laird,M.E., Yatim,N., Fiette,L., Ingersoll,M.A. and Albert,M.L.
Dipeptidylpeptidase 4 inhibition enhances lymphocyte trafficking, improving both naturally occurring tumor immunity and immunotherapy
Nat Immunol (2015) 16, 850-858. PubMed Europe PubMed DOI I
Block,H., Maertens,B., Spriestersbach,A., Kubicek,J. and Schafer,F.
Proteolytic affinity tag cleavage
Methods Enzymol (2015) 559, 71-97. PubMed Europe PubMed DOI
Costante,R., Stefanucci,A., Carradori,S., Novellino,E. and Mollica,A.
DPP-4 inhibitors: a patent review (2012 - 2014)
Expert Opin Ther Pat (2015) 25, 209-236. PubMed Europe PubMed DOI V I
Gao,Y., Zhang,Y., Zhu,J., Li,B., Li,Z., Zhu,W., Shi,J., Jia,Q. and Li,Y.
Recent progress in natural products as DPP-4 inhibitors
Future Med Chem (2015) 7, 1079-1089. PubMed Europe PubMed DOI I
Gilibili,R.R., Bhamidipati,R.K., Mullangi,R. and Srinivas,N.R.
Retrospective and prospective human intravenous and oral pharmacokinetic projection of dipeptidyl peptidase-IV inhibitors using simple allometric principles - case studies of ABT-279, ABT-341, alogliptin, carmegliptin, sitagliptin and vildagliptin
J Pharm Pharm Sci (2015) 18, 434-448. PubMed Europe PubMed I
Jain,M.R., Joharapurkar,A.A., Bahekar,R.H., Patel,H., Jadav,P., Kshirsagar,S.G., Patel,V.J., Patel,K.N., Ramanathan,V.K., Patel,P.R. and Desai,R.C.
Pharmacological characterization of ZYDPLA1, a novel long-acting dipeptidyl peptidase-4 inhibitor
J Diabetes (2015) 7, 708-717. PubMed Europe PubMed DOI I
Jiang,T., Zhou,Y., Chen,Z., Sun,P., Zhu,J., Zhang,Q., Wang,Z., Shao,Q., Jiang,X., Li,B., Chen,K., Jiang,H., Wang,H., Zhu,W. and Shen,J.
Design, synthesis, and pharmacological evaluation of fused beta-homophenylalanine derivatives as potent DPP-4 inhibitors
ACS Med Chem Lett (2015) 6, 602-606. PubMed Europe PubMed DOI PMC EPMC I
Jiang,T., Zhou,Y., Zhu,J., Chen,Z., Sun,P., Zhang,Q., Wang,Z., Shao,Q., Jiang,X., Li,B., Wang,H., Zhu,W. and Shen,J.
Design, synthesis, and pharmacological evaluation of highly potent and selective dipeptidyl peptidase-4 inhibitors
Arch Pharm (Weinheim) (2015) 348, 399-407. PubMed Europe PubMed DOI I
Kushwaha,R.N., Srivastava,R., Mishra,A., Rawat,A.K., Srivastava,A.K., Haq,W. and Katti,S.B.
Design, synthesis, biological screening, and molecular docking studies of piperazine-derived constrained inhibitors of DPP-IV for the treatment of type 2 diabetes
Chem Biol Drug Des (2015) 85, 439-446. PubMed Europe PubMed DOI I
Lacroix,I.M. and Li-Chan,E.C.
Comparison of the susceptibility of porcine and human dipeptidyl-peptidase IV to inhibition by protein-derived peptides
Peptides (2015) 69, 19-25. PubMed Europe PubMed DOI I
Lan,V.T.T., Ito,K., Ohno,M., Motoyama,T., Ito,S. and Kawarasaki,Y.
Analyzing a dipeptide library to identify human dipeptidyl peptidase IV inhibitor
Food Chem (2015) 175, 66-73. PubMed Europe PubMed DOI I
McKeage,K.
Trelagliptin: first global approval
Drugs (2015) 75, 1161-1164. PubMed Europe PubMed DOI I
Mo,D.W., Dong,S., Sun,H., Chen,J.S., Pang,J.X., Xi,B.M. and Chen,W.H.
Synthesis and potent inhibitory activities of carboxybenzyl-substituted 8-(3-(R)-aminopiperidin-1-yl)-7-(2-chloro/cyanobenzyl)-3-methyl-3,7-dihydro-purine-2,6-diones as dipeptidyl peptidase IV (DPP-IV) inhibitors
Bioorg Med Chem Lett (2015) 25, 1872-1875. PubMed Europe PubMed DOI I
Morikawa,T., Ninomiya,K., Akaki,J., Kakihara,N., Kuramoto,H., Matsumoto,Y., Hayakawa,T., Muraoka,O., Wang,L.B., Wu,L.J., Nakamura,S., Yoshikawa,M. and Matsuda,H.
Dipeptidyl peptidase-IV inhibitory activity of dimeric dihydrochalcone glycosides from flowers of Helichrysum arenarium
J Nat Med (2015) 69, 494-506. PubMed Europe PubMed DOI I
Ohno,M., Ito,K., Lan,V.T., Kusubata,M., Tometsuka,C., Koyama,Y.I., Motoyama,T., Ito,S. and Kawarasaki,Y.
Synergistic inhibition of human dipeptidyl peptidase IV by combinations of peptides
Peptides (2015) 69, 115-117. PubMed Europe PubMed DOI I
Panchapakesan,U. and Pollock,C.
The role of dipeptidyl peptidase-4 inhibitors in diabetic kidney disease
Front Immunol (2015) 6, 443-443. PubMed Europe PubMed DOI PMC EPMC I
Patel,B.D. and Ghate,M.D.
3D-QSAR studies of dipeptidyl peptidase-4 inhibitors using various alignment methods
Med Chem Res (2015) 24, 1060-1069. DOI I
Patil,S., Sharma,R. and Abhishek,A.
Comparative study to predict dipeptidyl peptidase IV inhibitory activity of beta-amino amide scaffold
Indian J Pharm Sci (2015) 77, 142-150. PubMed Europe PubMed PMC EPMC I
Ran,Y., Pei,H., Xie,C., Ma,L., Wu,Y., Lei,K., Shao,M., Tang,M., Xiang,M., Peng,A., Wei,Y. and Chen,L.
Scaffold-based design of xanthine as highly potent inhibitors of DPP-IV for improving glucose homeostasis in DIO mice
Mol Divers (2015) 19, 333-346. PubMed Europe PubMed DOI I
Ren,H., Zhuo,X., Su,H., Li,X., Tang,H., Jin,Y., Zhao,Q. and Wang,S.
Synthesis and evaluation of novel xanthone derivatives as potent dipeptidyl peptidase-4 inhibitors
Asian J Chem (2015) 27, 2079-2081. DOI I
Salles,T.A., Santos,L.D., Barauna,V.G. and Girardi,A.C.
Potential role of dipeptidyl peptidase IV in the pathophysiology of heart failure
Int J Mol Sci (2015) 16, 4226-4249. PubMed Europe PubMed DOI
Scheen,A.J.
A review of gliptins for 2014
Expert Opin Pharmacother (2015) 16, 43-62. PubMed Europe PubMed DOI V I
Schwehm,C., Li,J., Song,H., Hu,X., Kellam,B. and Stocks,M.J.
Synthesis of new DPP-4 inhibitors based on a novel tricyclic scaffold
ACS Med Chem Lett (2015) 6, 324-328. PubMed Europe PubMed DOI PMC EPMC I
Shoombuatong,W., Prachayasittikul,V., Anuwongcharoen,N., Songtawee,N., Monnor,T., Prachayasittikul,S., Prachayasittikul,V. and Nantasenamat,C.
Navigating the chemical space of dipeptidyl peptidase-4 inhibitors
Drug Des Devel Ther (2015) 9, 4515-4549. PubMed Europe PubMed DOI PMC EPMC I
Smelcerovic,A., Miljkovic,F., Kolarevic,A., Lazarevic,J., Djordjevic,A., Kocic,G. and Anderluh,M.
An overview of recent dipeptidyl peptidase-IV inhibitors: linking their structure and physico-chemical properties with SAR, pharmacokinetics and toxicity
Curr Top Med Chem (2015) 15, 2342-2372. PubMed Europe PubMed V I
Srivastava,J.K., Dubey,P., Singh,S., Bhat,H.R., Kumawat,M.K. and Singh,U.P.
Discovery of novel 1,3,5-triazine-thiazolidine-2,4-diones as dipeptidyl peptidase-4 inhibitors with antibacterial activity targeting the S1 pocket for the treatment of type 2 diabetes
RSC Adv (2015) 5, 14095-14102. DOI I
Velazquez,S., De Castro,S., Diez-Torrubia,A., Balzarini,J. and Camarasa,M.J.
Dipeptidyl-peptidase IV (DPP IV/CD26)-activated prodrugs: a successful strategy for improving water solubility and oral bioavailability
Curr Med Chem (2015) 22, 1041-1054. PubMed Europe PubMed
Verma,S.K., Sharma,S.K. and Thareja,S.
Docking study of novel pyrrolidine derivatives as potential dipeptidyl peptidase-IV (DPP-IV) inhibitors
Lett Drug Des Discov (2015) 12, 284-291. I
Watanabe,Y.S., Yasuda,Y., Kojima,Y., Okada,S., Motoyama,T., Takahashi,R. and Oka,M.
Anagliptin, a potent dipeptidyl peptidase IV inhibitor: its single-crystal structure and enzyme interactions
J Enzyme Inhib Med Chem (2015) 30, 981-988. PubMed Europe PubMed DOI S I
Zhang,J., Liu,Y., Lv,J., Cao,Y. and Li,G.
Dipeptidyl peptidase-IV activity assay and inhibitor screening using a gold nanoparticle-modified gold electrode with an immobilized enzyme substrate
Mikrochim Acta (2015) 182, 281-288. DOI A
Zhong,J. and Rajagopalan,S.
Dipeptidyl peptidase-4 regulation of SDF-1/CXCR4 axis: implications for cardiovascular disease
Front Immunol (2015) 6, 477-477. PubMed Europe PubMed DOI PMC EPMC V
Zhong,J., Maiseyeu,A., Davis,S.N. and Rajagopalan,S.
DPP4 in cardiometabolic disease: recent insights from the laboratory and clinical trials of DPP4 inhibition
Circ Res (2015) 116, 1491-1504. PubMed Europe PubMed DOI PMC EPMC I

2014

Al-Balas,Q.A., Sowaileh,M.F., Hassan,M.A., Qandil,A.M., Alzoubi,K.H., Mhaidat,N.M., Almaaytah,A.M. and Khabour,O.F.
Novel N-substituted aminobenzamide scaffold derivatives targeting the dipeptidyl peptidase-IV enzyme
Drug Des Devel Ther (2014) 8, 129-163. PubMed Europe PubMed DOI PMC EPMC I
Arrebola,Y.M., Gomez,H., Valiente,P.A., Chavez,M.D.L.A. and Pascual,I.
Dipeptidyl peptidase IV and its implication in cancer
Biotecnol Apl (2014) 31, 93-110.
Biftu,T., Sinha-Roy,R., Chen,P., Qian,X., Feng,D., Kuethe,J.T., Scapin,G., Gao,Y.D., Yan,Y., Krueger,D., Bak,A., Eiermann,G., He,J., Cox,J., Hicks,J., Lyons,K., He,H., Salituro,G., Tong,S., Patel,S., Doss,G., Petrov,A., Wu,J., Xu,S.S., Sewall,C., Zhang,X., Zhang,B., Thornberry,N.A. and Weber,A.E.
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes
J Med Chem (2014) 57, 3205-3212. PubMed Europe PubMed DOI I
Chakraborty,C., Hsu,M.J. and Agoramoorthy,G.
Understanding the molecular dynamics of type-2 diabetes drug target DPP-4 and its interaction with sitagliptin and inhibitor diprotin-A
Cell Biochem Biophys (2014) 70, 907-922. PubMed Europe PubMed DOI I
Chua,S., Lee,F.Y., Tsai,T.H., Sheu,J.J., Leu,S., Sun,C.K., Chen,Y.L., Chang,H.W., Chai,H.T., Liu,C.F., Lu,H.I. and Yip,H.K.
Inhibition of dipeptidyl peptidase-IV enzyme activity protects against myocardial ischemia-reperfusion injury in rats
J Transl Med (2014) 12, 357-357. PubMed Europe PubMed DOI I
Dahan,A., Wolk,O., Yang,P., Mittal,S., Wu,Z., Landowski,C.P. and Amidon,G.L.
Dipeptidyl peptidase IV as a potential target for selective prodrug activation and chemotherapeutic action in cancers
Mol Pharm (2014) 11, 4385-4394. PubMed Europe PubMed DOI
Fujimoto,N., Ohnuma,K., Aoe,K., Hosono,O., Yamada,T., Kishimoto,T. and Morimoto,C.
Clinical significance of soluble CD26 in malignant pleural mesothelioma
PLoS ONE (2014) 9, e115647-e115647. PubMed Europe PubMed DOI PMC EPMC
Hatanaka,T., Kawakami,K. and Uraji,M.
Inhibitory effect of collagen-derived tripeptides on dipeptidylpeptidase-IV activity
J Enzyme Inhib Med Chem (2014) 29, 823-828. PubMed Europe PubMed DOI I
Inagaki,N., Onouchi,H., Sano,H., Funao,N., Kuroda,S. and Kaku,K.
SYR-472, a novel once-weekly dipeptidyl peptidase-4 (DPP-4) inhibitor, in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial
Lancet Diabetes Endocrinol (2014) 2, 125-132. PubMed Europe PubMed DOI I
Janardhan,S. and Sastry,G.N.
Dipeptidyl peptidase IV inhibitors: a new paradigm in type 2 diabetes treatment
Curr Drug Targets (2014) 15, 600-621. PubMed Europe PubMed DOI I
Ji,X., Su,M., Wang,J., Deng,G., Deng,S., Li,Z., Tang,C., Li,J., Li,J., Zhao,L., Jiang,H. and Liu,H.
Design, synthesis and biological evaluation of hetero-aromatic moieties substituted pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors
Eur J Med Chem (2014) 75, 111-122. PubMed Europe PubMed DOI I
Ji,X., Xia,C., Wang,J., Su,M., Zhang,L., Dong,T., Li,Z., Wan,X., Li,J., Li,J., Zhao,L., Gao,Z., Jiang,H. and Liu,H.
Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors
Eur J Med Chem (2014) 86, 242-256. PubMed Europe PubMed DOI I
Juillerat-Jeanneret,L.
Dipeptidyl peptidase IV and its inhibitors: therapeutics for type 2 diabetes and what else?
J Med Chem (2014) 57, 2197-2212. PubMed Europe PubMed DOI I
Kim,N.H., Yu,T. and Lee,D.H.
The nonglycemic actions of dipeptidyl peptidase-4 inhibitors
Biomed Res Int (2014) 2014, 368703-368703. PubMed Europe PubMed DOI PMC EPMC I
Kim,Y., Kim,U., Kim,I.S., Lee,S.H., Lee,J., Kim,D.H. and Yoo,H.H.
Absorption, distribution, metabolism and excretion of gemigliptin, a novel dipeptidyl peptidase IV inhibitor, in rats
Xenobiotica (2014) 44, 627-634. PubMed Europe PubMed DOI I
Ku,H.C. and Su,M.J.
DPP4 Deficiency preserved cardiac function in abdominal aortic banding rats
PLoS ONE (2014) 9, e85634-e85634. PubMed Europe PubMed DOI PMC EPMC K
Kushwaha,R.N., Haq,W. and Katti,S.B.
Sixteen-years of clinically relevant dipeptidyl peptidase-IV (DPP-IV) inhibitors for treatment of type-2 diabetes: a perspective
Curr Med Chem (2014) 21, 4013-4045. PubMed Europe PubMed I
Liu,M., Sun,X. and Zhao,X.
Investigating the contributions of residues to dipeptidyl peptidase-IV inhibitor binding by molecular dynamics simulation
Lett Drug Des Discov (2014) 11, 886-893. I
Marier,J.-F., Mouksassi,M.-S., Gosselin,N.H. and Li,J.
Population pharmacokinetic analysis of dutogliptin, a selective dipeptidyl peptidase-4 inhibitor
Clin Pharmacol Drug Dev (2014) 3, 297-304. PubMed Europe PubMed DOI I
Mohandas,R., Sautina,L., Beem,E., Schuler,A., Chan,W.Y., Domsic,J., McKenna,R., Johnson,R.J. and Segal,M.S.
Uric acid inhibition of dipeptidyl peptidase IV in vitro is dependent on the intracellular formation of triuret
Exp Cell Res (2014) 326, 136-142. PubMed Europe PubMed DOI I
Mulvihill,E.E. and Drucker,D.J.
Pharmacology, physiology, and mechanisms of action of dipeptidyl peptidase-4 inhibitors
Endocr Rev (2014) 35, 992-1019. PubMed Europe PubMed DOI I
Namoto,K., Sirockin,F., Ostermann,N., Gessier,F., Flohr,S., Sedrani,R., Gerhartz,B., Trappe,J., Hassiepen,U., Duttaroy,A., Ferreira,S., Sutton,J.M., Clark,D.E., Fenton,G., Beswick,M. and Baeschlin,D.K.
Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV
Bioorg Med Chem Lett (2014) 24, 731-736. PubMed Europe PubMed DOI I
Nedosugova,L.V., Petunina,N.A. and Galstyan,K.O.
Initial investigation of efficacy and safety of a new dipeptidyl peptidase-4 inhibitor, gosogliptin, for type 2 diabetes in Russia
Diabetes Mellitus (2014) 2014, 81-86. DOI I
Nongonierma,A.B. and FitzGerald,R.J.
An in silico model to predict the potential of dietary proteins as sources of dipeptidyl peptidase IV (DPP-IV) inhibitory peptides
Food Chem (2014) 165, 489-498. PubMed Europe PubMed DOI I
Patil,S. and Sharma,R.
3D QSAR study and designing of novel prolinenitriles derivatives as dipeptidyl peptidase IV inhibitor
Curr Trends Biotechnol Pharm (2014) 8, 254-263. I
Peng,C.H., Yang,Y.S., Chan,K.C., Wang,C.J., Chen,M.L. and Huang,C.N.
Hibiscus sabdariffa polyphenols alleviate insulin resistance and renal epithelial to mesenchymal transition: a novel action mechanism mediated by type 4 dipeptidyl peptidase
J Agric Food Chem (2014) 62, 9736-9743. PubMed Europe PubMed DOI I
Rizzo,M.R., Barbieri,M., Boccardi,V., Angellotti,E., Marfella,R. and Paolisso,G.
Dipeptidyl peptidase-4 inhibitors have protective effect on cognitive impairment in aged diabetic patients with mild cognitive impairment
J Gerontol A Biol Sci Med Sci (2014) 69, 1122-1131. PubMed Europe PubMed DOI I
Rohrborn,D., Eckel,J. and Sell,H.
Shedding of dipeptidyl peptidase 4 is mediated by metalloproteases and up-regulated by hypoxia in human adipocytes and smooth muscle cells
FEBS Lett (2014) 588, 3870-3877. PubMed Europe PubMed DOI
Sawant,S.D., Nerkar,A.G., Velapure,A.V. and Pawar,N.D.
Design, synthesis, QSAR studies and in vitro evaluation of novel triazolopiperazine based B-Amino amides as dipeptidyl peptidase-IV (DPP-IV) inhibitors: Part-I
Int J Pharmcy Pharm Sci (2014) 6, 760-765. I
Shu,C., Ge,H., Song,M., Chen,J.H., Zhou,H., Qi,Q., Wang,F., Ma,X., Yang,X., Zhang,G., Ding,Y., Zhou,D., Peng,P., Shih,C.K., Xu,J. and Wu,F.
Discovery of imigliptin, a novel selective DPP-4 inhibitor for the treatment of type 2 diabetes
ACS Med Chem Lett (2014) 5, 921-926. PubMed Europe PubMed DOI PMC EPMC I
Singh,A.K.
Dipeptidyl peptidase-4 inhibitors: novel mechanism of actions
Indian J Endocrinol Metab (2014) 18, 753-759. PubMed Europe PubMed DOI PMC EPMC I
Song,W., Wang,Y., Wang,N., Wang,D., Guo,J., Fu,L. and Shi,X.
Identification of residues on human receptor DPP4 critical for MERS-CoV binding and entry
Virology (2014) 471-473, 49-53. PubMed Europe PubMed DOI
Tanwar,O., Deora,G.S., Tanwar,L., Kumar,G., Janardhan,S., Alam,M.M., Shaquiquzzaman,M. and Akhter,M.
Novel hydrazine derivatives as selective DPP-IV inhibitors: findings from virtual screening and validation through molecular dynamics simulations
J Mol Model (2014) 20, 2118-2118. PubMed Europe PubMed DOI I
Tanwar,O., Tanwar,L., Shaquiquzzaman,M., Alam,M.M. and Akhter,M.
Structure based virtual screening of MDPI database: discovery of structurally diverse and novel DPP-IV inhibitors
Bioorg Med Chem Lett (2014) 24, 3447-3451. PubMed Europe PubMed DOI I
Ustun-Aytekin,O., Gurhan,I.D., Ohura,K., Imai,T. and Ongen,G.
Monitoring of the effects of transfection with baculovirus on Sf9 cell line and expression of human dipeptidyl peptidase IV
Cytotechnology (2014) 66, 159-168. PubMed Europe PubMed DOI E
Wang,S., Su,M., Wang,J., Li,Z., Zhang,L., Ji,X., Li,J., Li,J. and Liu,H.
(R)-3-Amino-1-((3aS,7aS)-octahydro-1H-indol-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one derivatives as potent inhibitors of dipeptidyl peptidase-4: design, synthesis, biological evaluation, and molecular modeling
Bioorg Med Chem (2014) 22, 6684-6693. PubMed Europe PubMed DOI I
Wang,S.C., Zeng,L.L., Ding,Y.Y., Zeng,S.G., Song,H.R., Hu,W.H. and Xie,H.
[A novel dipeptidyl peptidase IV inhibitors developed through scaffold hopping and drug splicing strategy]
Yao Xue Xue Bao (2014) 49, 61-67. PubMed Europe PubMed I
Wang,Z., Grigo,C., Steinbeck,J., von Horsten,S., Amann,K. and Daniel,C.
Soluble DPP4 originates in part from bone marrow cells and not from the kidney
Peptides (2014) 57, 109-117. PubMed Europe PubMed DOI
Xiao,P.-F., Guo,R., Huang,S.-Q., Cui,H.-J., Ye,S. and Zhang,Z.
Discovery of dipeptidyl peptidase IV (DPP4) inhibitors based on a novel indole scaffold
Chin Chem Lett (2014) 209, 1509-1519. DOI I
Xing,J., Li,Q., Zhang,S., Liu,H., Zhao,L., Cheng,H., Zhang,Y., Zhou,J. and Zhang,H.
Identification of dipeptidyl peptidase IV inhibitors: virtual screening, synthesis and biological evaluation
Chem Biol Drug Des (2014) 84, 364-377. PubMed Europe PubMed DOI I
Yang,L., Yuan,J. and Zhou,Z.
Emerging roles of dipeptidyl peptidase 4 inhibitors: anti-inflammatory and immunomodulatory effect and its application in diabetes mellitus
Can J Diabetes (2014) 38, 473-479. PubMed Europe PubMed DOI I
Zhao,Y., Yang,L. and Zhou,Z.
Dipeptidyl peptidase-4 inhibitors: Multitarget drugs, not only antidiabetes drugs
J Diabetes (2014) 6, 21-29. PubMed Europe PubMed DOI I

2013

Almasri,I.M., Taha,M.O. and Mohammad,M.K.
New leads for DPP IV inhibition: structure-based pharmacophore mapping and virtual screening study
Arch Pharm Res (2013) 36, 1326-1337. PubMed Europe PubMed DOI I
Aroor,A., McKarns,S., Nistala,R., Demarco,V., Gardner,M., Garcia-Touza,M., Whaley-Connell,A. and Sowers,J.R.
DPP-4 inhibitors as therapeutic modulators of immune cell function and associated cardiovascular and renal insulin resistance in obesity and diabetes
Cardiorenal Med (2013) 3, 48-56. PubMed Europe PubMed DOI PMC EPMC I
Ben-Shlomo,S., Zvibel,I., Rabinowich,L., Goldiner,I., Shlomai,A., Santo,E.M., Halpern,Z., Oren,R. and Fishman,S.
Dipeptidyl peptidase 4-deficient rats have improved bile secretory function in high fat diet-induced steatosis
Dig Dis Sci (2013) 58, 172-178. PubMed Europe PubMed DOI K
Biftu,T., Qian,X., Chen,P., Feng,D., Scapin,G., Gao,Y.D., Cox,J., Sinha Roy,R., Eiermann,G., He,H., Lyons,K., Salituro,G., Patel,S., Petrov,A., Xu,F., Xu,S.S., Zhang,B., Caldwell,C., Wu,J.K., Lyons,K. and Weber,A.E.
Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: Profile of clinical candidate (2R,3S,5R)-2- (2,5-difluorophenyl)-5-(4,6-dihydropyrrolo [3,4-c]pyrazol-5-(1H)-yl)tetrahydro-2H-pyran-3-amine (23) [corrected]
Bioorg Med Chem Lett (2013) 23, 5361-5366. PubMed Europe PubMed DOI I
Cahn,A. and Raz,I.
Emerging gliptins for type 2 diabetes
Expert Opin Emerg Drugs (2013) 18, 245-258. PubMed Europe PubMed DOI I
Czechtizky,W., Dedio,J., Desai,B., Dixon,K., Farrant,E., Feng,Q., Morgan,T., Parry,D.M., Ramjee,M.K., Selway,C.N., Schmidt,T., Tarver,G.J. and Wright,A.G.
Integrated synthesis and testing of substituted xanthine based DPP4 inhibitors: application to drug discovery
ACS Med Chem Lett (2013) 4, 768-772. PubMed Europe PubMed DOI PMC EPMC I
Dos Santos,L., Salles,T.A., Arruda-Junior,D.F., Campos,L.C., Pereira,A.C., Barreto,A.L., Antonio,E.L., Mansur,A.J., Tucci,P.J., Krieger,J.E. and Girardi,A.C.
Circulating dipeptidyl peptidase IV activity correlates with cardiac dysfunction in human and experimental heart failure
Circ Heart Fail (2013) 6, 1029-1038. PubMed Europe PubMed DOI
Fan,J., Johnson,M.H., Lila,M.A., Yousef,G. and de Mejia,E.G.
Berry and citrus phenolic compounds inhibit dipeptidyl peptidase IV: implications in diabetes management
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Khalaf,R.A., Sheikha,G.A., Al-Sha'er,M. and Taha,M.
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Kim,S.H., Lee,S.H. and Yim,H.J.
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Liu,Y., Si,M., Tang,L., Shangguan,S., Wu,H., Li,J., Wu,P., Ma,X., Liu,T. and Hu,Y.
Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors
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Lu,G., Hu,Y., Wang,Q., Qi,J., Gao,F., Li,Y., Zhang,Y., Zhang,W., Yuan,Y., Bao,J., Zhang,B., Shi,Y., Yan,J. and Gao,G.F.
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A comparative study of the binding modes of recently launched dipeptidyl peptidase IV inhibitors in the active site
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Nongonierma,A.B. and FitzGerald,R.J.
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Ou,X., O'Leary,H.A. and Broxmeyer,H.E.
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Patel,B. and Ghate,M.
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DPP-4 inhibitors improve cognition and brain mitochondrial function of insulin-resistant rats
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Poplawski,S.E., Lai,J.H., Li,Y., Jin,Z., Liu,Y., Wu,W., Wu,Y., Zhou,Y., Sudmeier,J.L., Sanford,D.G. and Bachovchin,W.W.
Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase
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Sharma,M., Singh,D. and Gupta,M.
Synthesis and evaluation of thiouracil derivatives as dipeptidyl peptidase IV inhibitors
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Sharma,M., Gupta,M., Singh,D., Kumar,M. and Kaur,P.
Synthesis, evaluation and molecular docking of prolyl-fluoropyrrolidine derivatives as dipeptidyl peptidase IV inhibitors
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Sharoyan,S., Antonyan,A., Mardanyan,S., Harutyunyan,H., Movsisyan,N., Hovnanyan,N. and Hovnanyan,K.
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Tang,J., Majeti,J., Sudom,A., Xiong,Y., Lu,M., Liu,Q., Higbee,J., Zhang,Y., Wang,Y., Wang,W., Cao,P., Xia,Z., Johnstone,S., Min,X., Yang,X., Shao,H., Yu,T., Sharkov,N., Walker,N., Tu,H., Shen,W. and Wang,Z.
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Tatosian,D.A., Guo,Y., Schaeffer,A.K., Gaibu,N., Popa,S., Stoch,A., Langdon,R.B. and Kauh,E.A.
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Wang,J., Feng,Y., Ji,X., Deng,G., Leng,Y. and Liu,H.
Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes
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Wang,N., Shi,X., Jiang,L., Zhang,S., Wang,D., Tong,P., Guo,D., Fu,L., Cui,Y., Liu,X., Arledge,K.C., Chen,Y.H., Zhang,L. and Wang,X.
Structure of MERS-CoV spike receptor-binding domain complexed with human receptor DPP4
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Wang,X., Li,Y., Gui,X.-R. and Cheng,X.-C.
Progress in dipeptidyl peptidase-4 and its inhibitors
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The emerging role of dipeptidyl peptidase-4 inhibitors in cardiovascular protection: current position and perspectives
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Xie,H., Zeng,L., Zeng,S., Lu,X., Zhao,X., Zhang,G., Tu,Z., Xu,H., Yang,L., Zhang,X., Wang,S. and Hu,W.
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Zeng,S., Xie,H., Zeng,L.L., Lu,X., Zhao,X., Zhang,G.C., Tu,Z.C., Xu,H.J., Yang,L., Zhang,X.Q. and Hu,W.
Discovery of potent dipeptidyl peptidase IV inhibitors through pharmacophore hybridization and hit-to-lead optimization
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Zhang,L., Su,M., Li,J., Ji,X., Wang,J., Li,Z., Li,J. and Liu,H.
Design, synthesis, structure-activity relationships, and docking studies of 1-(gamma-1,2,3-triazol substituted prolyl)-(S)-3,3-difluoropyrrolidines as a novel series of potent and selective dipeptidyl peptidase-4 inhibitors
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Zhao,G., Kwon,C., Wang,A., Robertson,J.G., Marcinkeviciene,J., Parker,R.A., Kirby,M.S. and Hamann,L.G.
Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors
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Zhong,J., Rao,X. and Rajagopalan,S.
An emerging role of dipeptidyl peptidase 4 (DPP4) beyond glucose control: potential implications in cardiovascular disease
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Zhu,L., Li,Y., Qiu,L., Su,M., Wang,X., Xia,C., Qu,Y., Li,J., Li,J., Xiong,B. and Shen,J.
Design and synthesis of 4-(2,4,5-trifluorophenyl)butane-1,3-diamines as dipeptidyl peptidase IV inhibitors
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2012

Aghili,N., Devaney,J.M., Alderman,L.O., Zukowska,Z., Epstein,S.E. and Burnett,M.S.
Polymorphisms in dipeptidyl peptidase IV gene are associated with the risk of myocardial infarction in patients with atherosclerosis
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Davis,J.A., Kumar,P.S., Singh,S., Surender,A., Roy,S., Khanna,V., Sethi,S., Pal,C., Sharma,L., Benjamin,B., Mittra,S., Sattigeri,J. and Bansal,V.S.
Biological evaluation of RBx-0128, a potent and selective dipeptidyl peptidase-IV inhibitor in type 2 diabetes genetic model
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De,S. and Banerjee,S.
Structure based design of few substituted piperidones as dipeptidyl peptidase inhibitors
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Derosa,G. and Maffioli,P.
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Detel,D., Pugel,E.P., Pucar,L.B., Buljevic,S. and Varljen,J.
Development and resolution of colitis in mice with target deletion of dipeptidyl peptidase IV
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Diez-Torrubia,A., Cabrera,S., Lambeir,A.M., Balzarini,J., Camarasa,M.J. and Velazquez,S.
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Fan,H., Tansi,F.L., Weihofen,W.A., Bottcher,C., Hu,J., Martinez,J., Saenger,W. and Reutter,W.
Molecular mechanism and structural basis of interactions of dipeptidyl peptidase IV with adenosine deaminase and human immunodeficiency virus type-1 transcription transactivator
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Fukuda-Tsuru,S., Anabuki,J., Abe,Y., Yoshida,K. and Ishii,S.
A novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor, teneligliptin, improves postprandial hyperglycemia and dyslipidemia after single and repeated administrations
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Gibbs,J.P., Fredrickson,J., Barbee,T., Correa,I., Smith,B., Lin,S.L. and Gibbs,M.A.
Quantitative model of the relationship between dipeptidyl peptidase-4 (DPP-4) inhibition and response: meta-analysis of alogliptin, saxagliptin, sitagliptin, and vildagliptin efficacy results
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Guasch,L., Sala,E., Ojeda,M.J., Valls,C., Blade,C., Mulero,M., Blay,M., Ardevol,A., Garcia-Vallve,S. and Pujadas,G.
Identification of novel human dipeptidyl peptidase-IV inhibitors of natural origin (part II): in silico prediction in antidiabetic extracts
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Guasch,L., Ojeda,M.J., Gonzalez-Abuin,N., Sala,E., Cereto-Massague,A., Mulero,M., Valls,C., Pinent,M., Ardevol,A., Garcia-Vallve,S. and Pujadas,G.
Identification of novel human dipeptidyl peptidase-IV inhibitors of natural origin (part I): virtual screening and activity assays
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Ikuma,Y., Hochigai,H., Kimura,H., Nunami,N., Kobayashi,T., Uchiyama,K., Furuta,Y., Sakai,M., Horiguchi,M., Masui,Y., Okazaki,K., Sato,Y. and Nakahira,H.
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors
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Jadav,P., Bahekar,R., Shah,S.R., Patel,D., Joharapurkar,A., Shah,K., Bhardwaj,S., Patel,K., Patel,K., Chopade,R., Shaikh,M., Sairam,K.V.V.M. and Jain,M.
Design of peptidomimetic based DPP-IV inhibitors, devoid of CYP liabilities
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Dipeptidyl peptidase-4 inhibitor with beta-amino amide scaffold: synthesis, SAR and biological evaluation
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Lam,B., Zhang,Z., Stafford,J.A., Skene,R.J., Shi,L. and Gwaltney,S.L.
Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors
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Lasserson,D. and Mant,J.
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Li,C., Lu,W., Lu,C., Xiao,W., Shen,X., Huang,J., Liu,G. and Tang,Y.
Identification of diverse dipeptidyl peptidase IV inhibitors via structure-based virtual screening
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Liu,W., Yan,M., Liu,Y., McLeish,K.R., Coleman,W.G., Jr. and Rodgers,G.P.
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Acute and chronic administration of SHR117887, a novel and specific dipeptidyl peptidase-4 inhibitor, improves metabolic control in diabetic rodent models
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Marchetti,C., Di Carlo,A., Facchiano,F., Senatore,C., De Cristofaro,R., Luzi,A., Federici,M., Romani,M., Napolitano,M., Capogrossi,M.C. and Germani,A.
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Matheeussen,V., Lambeir,A.M., Jungraithmayr,W., Gomez,N., Mc Entee,K., Van der Veken,P., Scharpe,S. and De Meester,I.
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Misumi,Y. and Ikehara,Y.
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Nitta,A., Fujii,H., Sakami,S., Satoh,M., Nakaki,J., Satoh,S., Kumagai,H. and Kawai,H.
Novel series of 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides as potent and selective dipeptidyl peptidase IV inhibitors
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Pilla,E., Moller,U., Sauer,G., Mattiroli,F., Melchior,F. and Geiss-Friedlander,R.
A novel SUMO1-specific interacting motif in dipeptidyl peptidase 9 (DPP9) that is important for enzymatic regulation
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Sharma,M., Gupta,M., Singh,D., Kumar,M. and Kaur,P.
Synthesis, evaluation and molecular docking of thiazolopyrimidine derivatives as dipeptidyl peptidase IV inhibitors
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Song,J.S., Lee,K.R., Kwon,H.J., Rhee,S.D., Kim,M.S., Choi,S.H., Lee,S.H., Song,I.S., Ahn,J.H., Ahn,S.H. and Bae,M.A.
Pharmacokinetics and pharmacodynamics of KR-66223, a novel DPP-4 inhibitor
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Wu,D., Jin,F., Lu,W., Zhu,J., Li,C., Wang,W., Tang,Y., Jiang,H., Huang,J., Liu,G. and Li,J.
Synthesis, structure-activity relationship, and pharmacophore modeling studies of pyrazole-3-carbohydrazone derivatives as dipeptidyl peptidase IV inhibitors
Chem Biol Drug Des (2012) 79, 897-906. PubMed Europe PubMed DOI I
Wu,W., Liu,Y., Milo,L.J., Jr., Shu,Y., Zhao,P., Li,Y., Woznica,I., Yu,G., Sanford,D.G., Zhou,Y., Poplawski,S.E., Connolly,B.A., Sudmeier,J.L., Bachovchin,W.W. and Lai,J.H.
4-Substituted boro-proline dipeptides: synthesis, characterization, and dipeptidyl peptidase IV, 8, and 9 activities
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Xie,H., Zeng,L., Zeng,S., Lu,X., Zhang,G., Zhao,X., Cheng,N., Tu,Z., Li,Z., Xu,H., Yang,L., Zhang,X., Huang,M., Zhao,J. and Hu,W.
Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization
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Yoshida,T., Akahoshi,F., Sakashita,H., Sonda,S., Takeuchi,M., Tanaka,Y., Nabeno,M., Kishida,H., Miyaguchi,I. and Hayashi,Y.
Fused bicyclic heteroarylpiperazine-substituted l-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group
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Yoshida,T., Akahoshi,F., Sakashita,H., Kitajima,H., Nakamura,M., Sonda,S., Takeuchi,M., Tanaka,Y., Ueda,N., Sekiguchi,S., Ishige,T., Shima,K., Nabeno,M., Abe,Y., Anabuki,J., Soejima,A., Yoshida,K., Takashina,Y., Ishii,S., Kiuchi,S., Fukuda,S., Tsutsumiuchi,R., Kosaka,K., Murozono,T., Nakamaru,Y., Utsumi,H., Masutomi,N., Kishida,H., Miyaguchi,I. and Hayashi,Y.
Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
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Zhang,X., Wang,J., Su,M., Li,Z., Li,J., Li,J. and Liu,H.
Discovering novel alpha-aminoacyl-containing proline derivatives with potent and selective inhibitory activity against dipeptidyl peptidase IV: design, synthesis, biological evaluation, and molecular modeling
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2011

Ahn,H.J., Kim,K.B., Liu,K.H., Shin,J.G., Ahn,J.H., Kim,M.S., Bae,M.A. and Song,I.S.
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1-((3S,4S)-4-Amino-1-(4-substituted-1,3,5-triazin-2-yl) pyrrolidin-3-yl)-5,5-difluoropiperidin-2-one inhibitors of DPP-4 for the treatment of type 2 diabetes
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Ansorge,S., Nordhoff,K., Bank,U., Heimburg,A., Julius,H., Breyer,D., Thielitz,A., Reinhold,D. and Tager,M.
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Cho,J.M., Jang,H.W., Cheon,H., Jeong,Y.T., Kim,D.H., Lim,Y.M., Choi,S.H., Yang,E.K., Shin,C.Y., Son,M.H., Kim,S.H., Kim,H.J. and Lee,M.S.
A novel dipeptidyl peptidase IV inhibitor DA-1229 ameliorates streptozotocin-induced diabetes by increasing beta-cell replication and neogenesis
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Deng,J., Peng,L., Zhang,G., Lan,X., Li,C., Chen,F., Zhou,Y., Lin,Z., Chen,L., Dai,R., Xu,H., Yang,L., Zhang,X. and Hu,W.
The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes
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Huber,B.C., Brunner,S., Segeth,A., Nathan,P., Fischer,R., Zaruba,M.M., Vallaster,M., Theiss,H.D., David,R., Gerbitz,A. and Franz,W.M.
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Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors
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Kato,N., Oka,M., Murase,T., Yoshida,M., Sakairi,M., Yamashita,S., Yasuda,Y., Yoshikawa,A., Hayashi,Y., Makino,M., Takeda,M., Mirensha,Y. and Kakigami,T.
Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor
Bioorg Med Chem (2011) 19, 7221-7227. PubMed Europe PubMed DOI I
Kidd,S., Bueso-Ramos,C., Jagan,S., Paganessi,L.A., Boggio,L.N., Fung,H.C., Gregory,S.A. and Christopherson,K.W.
In Vivo expansion of the megakaryocyte progenitor cell population in adult CD26-deficient mice
Exp Hematol (2011) 39, 580-590. PubMed Europe PubMed DOI K
Kim,H.J., Kwak,W.Y., Min,J.P., Lee,J.Y., Yoon,T.H., Kim,H.D., Shin,C.Y., Kim,M.K., Choi,S.H., Kim,H.S., Yang,E.K., Cheong,Y.H., Chae,Y.N., Park,K.J., Jang,J.M., Choi,S.J., Son,M.H., Kim,S.H., Yoo,M. and Lee,B.J.
Discovery of DA-1229: A potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes
Bioorg Med Chem Lett (2011) 21, 3809-3812. PubMed Europe PubMed DOI I
Ku,H.C., Chen,W.P. and Su,M.J.
DPP4 deficiency preserves cardiac function via GLP-1 signaling in rats subjected to myocardial ischemia/reperfusion
Naunyn Schmiedebergs Arch Pharmacol (2011) 384, 197-207. PubMed Europe PubMed DOI K
Kuhn-Wache,K., Bar,J.W., Hoffmann,T., Wolf,R., Rahfeld,J.U. and Demuth,H.U.
Selective inhibition of dipeptidyl peptidase 4 by targeting a substrate-specific secondary binding site
Biol Chem (2011) 392, 223-231. PubMed Europe PubMed DOI P I
Li,C., Shen,J., Li,W., Lu,C., Liu,G. and Tang,Y.
Possible ligand release pathway of dipeptidyl peptidase IV investigated by molecular dynamics simulations
Proteins (2011) 79, 1800-1809. PubMed Europe PubMed DOI I
Maezaki,H., Banno,Y., Miyamoto,Y., Moritou,Y., Asakawa,T., Kataoka,O., Takeuchi,K., Suzuki,N., Ikedo,K., Kosaka,T., Sasaki,M., Tsubotani,S., Tani,A., Funami,M., Yamamoto,Y., Tawada,M., Aertgeerts,K., Yano,J. and Oi,S.
Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554
Bioorg Med Chem (2011) 19, 4482-4498. PubMed Europe PubMed DOI I
Matteucci,E. and Giampietro,O.
Dipeptidyl peptidase-4 inhibition: linking chemical properties to clinical safety
Curr Med Chem (2011) 18, 4753-4760. PubMed Europe PubMed DOI I
Mendieta,L., Tarrago,T. and Giralt,E.
Recent patents of dipeptidyl peptidase IV inhibitors
Expert Opin Ther Pat (2011) 21, 1693-1741. PubMed Europe PubMed DOI I
Miyamoto,Y., Banno,Y., Yamashita,T., Fujimoto,T., Oi,S., Moritoh,Y., Asakawa,T., Kataoka,O., Takeuchi,K., Suzuki,N., Ikedo,K., Kosaka,T., Tsubotani,S., Tani,A., Funami,M., Amano,M., Yamamoto,Y., Aertgeerts,K., Yano,J. and Maezaki,H.
Design and synthesis of 3-pyridylacetamide derivatives as dipeptidyl peptidase IV (DPP-4) inhibitors targeting a bidentate interaction with Arg125
Bioorg Med Chem (2011) 19, 172-185. PubMed Europe PubMed DOI I
Miyamoto,Y., Banno,Y., Yamashita,T., Fujimoto,T., Oi,S., Moritoh,Y., Asakawa,T., Kataoka,O., Yashiro,H., Takeuchi,K., Suzuki,N., Ikedo,K., Kosaka,T., Tsubotani,S., Tani,A., Sasaki,M., Funami,M., Amano,M., Yamamoto,Y., Aertgeerts,K., Yano,J. and Maezaki,H.
Discovery of a 3-pyridylacetic acid derivative (TAK-100) as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor
J Med Chem (2011) 54, 831-850. PubMed Europe PubMed DOI I
Motoshima,K., Sugita,K., Hashimoto,Y. and Ishikawa,M.
Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related alpha-glucosidase inhibitors and liver X receptor antagonists
Bioorg Med Chem Lett (2011) 21, 3041-3045. PubMed Europe PubMed DOI I
Murugesan,V., Sethi,N., Prabhakar,Y.S. and Katti,S.B.
CoMFA and CoMSIA of diverse pyrrolidine analogues as dipeptidyl peptidase IV inhibitors: active site requirements
Mol Divers (2011) 15, 457-466. PubMed Europe PubMed DOI I
Nishio,Y., Kimura,H., Sawada,N., Sugaru,E., Horiguchi,M., Ono,M., Furuta,Y., Sakai,M., Masui,Y., Otani,M., Hashizuka,T., Honda,Y., Deguchi,J., Nakagawa,T. and Nakahira,H.
2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): A potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A
Bioorg Med Chem (2011) 19, 5490-5499. PubMed Europe PubMed DOI I
Ohnuma,K., Hosono,O., Dang,N.H. and Morimoto,C.
Dipeptidyl peptidase in autoimmune pathophysiology
Adv Clin Chem (2011) 53, 51-84. PubMed Europe PubMed DOI
Paliwal,S., Seth,D., Yadav,D., Yadav,R. and Paliwal,S.
Development of a robust QSAR model to predict the affinity of pyrrolidine analogs for dipeptidyl peptidase IV (DPP- IV)
J Enzyme Inhib Med Chem (2011) 26, 129-140. PubMed Europe PubMed DOI I
Park,W.S., Kang,S.K., Jun,M.A., Shin,M.S., Kim,K.Y., Rhee,S.D., Bae,M.A., Kim,M.S., Kim,K.R., Kang,N.S., Yoo,S.E., Lee,J.O., Song,D.H., Silinski,P., Schneider,S.E., Ahn,J.H. and Kim,S.S.
Discovery of beta-aminoacyl containing thiazolidine derivatives as potent and selective dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (2011) 21, 1366-1370. PubMed Europe PubMed DOI I
Pascual,I., Gomez,H., Pons,T., Chappe,M., Vargas,M.A., Valdes,G., Lopez,A., Saroyan,A., Charli,J.L. and de Los Angeles Chavez,M.
Effect of divalent cations on the porcine kidney cortex membrane-bound form of dipeptidyl peptidase IV
Int J Biochem Cell Biol (2011) 43, 363-371. PubMed Europe PubMed DOI
Shah,Z., Kampfrath,T., Deiuliis,J.A., Zhong,J., Pineda,C., Ying,Z., Xu,X., Lu,B., Moffatt-Bruce,S., Durairaj,R., Sun,Q., Mihai,G., Maiseyeu,A. and Rajagopalan,S.
Long-term dipeptidyl-peptidase 4 inhibition reduces atherosclerosis and inflammation via effects on monocyte recruitment and chemotaxis
Circulation (2011) 124, 2338-2349. PubMed Europe PubMed DOI I
Shan,Z., Peng,M., Fan,H., Lu,Q., Lu,P., Zhao,C. and Chen,Y.
Discovery of potent dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing substituted [1,2,3]-triazolopiperidines for the treatment of type 2 diabetes
Bioorg Med Chem Lett (2011) 21, 1731-1735. PubMed Europe PubMed DOI I
Singh,S., Roy,S., Sethi,S., Benjamin,B., Sundaram,S., Khanna,V., Kandalkar,S.R., Pal,C., Kant,R., Patra,A.K., Rayasam,G., Mittra,S., Saini,K.S., Paliwal,J., Chugh,A., Ahmed,S., Sattigeri,J., Cliff,I., Ray,A., Bansal,V.S., Bhatnagar,P.K. and Davis,J.A.
RBx-0597, a potent, selective and slow-binding inhibitor of dipeptidyl peptidase-IV for the treatment of type 2 diabetes
Eur J Pharmacol (2011) 652, 157-163. PubMed Europe PubMed DOI I
Tajima,A., Yamamoto,K., Kozakai,A., Okumura-Kitajima,L., Mita,Y., Kitano,K., Jingu,S. and Nakaike,S.
(2S,4S)-4-Fluoro-1-{[(2-hydroxy-1,1-dimethylethyl)amino]acetyl}-pyrrolidine-2-carbonitrile monobenzenesulfonate (TS-021) is a selective and reversible dipeptidyl peptidase IV inhibitor
Eur J Pharmacol (2011) 655, 99-107. PubMed Europe PubMed DOI I
Tang,H.K., Chen,K.C., Liou,G.G., Cheng,S.C., Chien,C.H., Tang,H.Y., Huang,L.H., Chang,H.P., Chou,C.Y. and Chen,X.
Role of a propeller loop in the quaternary structure and enzymatic activity of prolyl dipeptidases DPP-IV and DPP9
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Wagner,L., Wermann,M., Rosche,F., Rahfeld,J.U., Hoffmann,T. and Demuth,H.U.
Isolation of dipeptidyl peptidase IV (DP 4) isoforms from porcine kidney by preparative isoelectric focusing to improve crystallization
Biol Chem (2011) 392, 665-677. PubMed Europe PubMed DOI
Yang,W., Xia,W., Mao,J., Xu,D., Chen,J., Feng,S., Wang,J., Li,H., Theisen,C.F., Petersen,J.M., Thorolfsson,M., Rasmussen,H.B., Junker,F., Boel,E. and Su,J.
High level expression, purification and activation of human dipeptidyl peptidase I from mammalian cells
Protein Expr Purif (2011) 76, 59-64. PubMed Europe PubMed DOI E
Zhang,Z., Wallace,M.B., Feng,J., Stafford,J.A., Skene,R.J., Shi,L., Lee,B., Aertgeerts,K., Jennings,A., Xu,R., Kassel,D.B., Kaldor,S.W., Navre,M., Webb,D.R. and Gwaltney,S.L.
Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV
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2010

Boehringer,M., Fischer,H., Hennig,M., Hunziker,D., Huwyler,J., Kuhn,B., Loeffler,B.M., Luebbers,T., Mattei,P., Narquizian,R., Sebokova,E., Sprecher,U. and Wessel,H.P.
Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (2010) 20, 1106-1108. PubMed Europe PubMed DOI I
Brigance,R.P., Meng,W., Fura,A., Harrity,T., Wang,A., Zahler,R., Kirby,M.S. and Hamann,L.G.
Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes
Bioorg Med Chem Lett (2010) 20, 4395-4398. PubMed Europe PubMed DOI I
Cho,T.P., Gang,L.Z., Long,Y.F., Yang,W., Qian,W., Lei,Z., Jing,L.J., Ying,F., Ke,Y.P., Ying,L. and Jun,F.
Synthesis and biological evaluation of bicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes
Bioorg Med Chem Lett (2010) 20, 3521-3525. PubMed Europe PubMed DOI I
Cho,T.P., Long,Y.F., Gang,L.Z., Yang,W., Jun,L.H., Yuan,S.G., Hong,F.J., Lin,W., Liang,G.D., Lei,Z., Jing,L.J., Shen,G.A., Hong,S.G., Dan,W., Ying,F., Ke,Y.P., Ying,L., Jun,F. and Tai,M.X.
Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes
Bioorg Med Chem Lett (2010) 20, 3565-3568. PubMed Europe PubMed DOI I
Chung,K.M., Cheng,J.H., Suen,C.S., Huang,C.H., Tsai,C.H., Huang,L.H., Chen,Y.R., Wang,A.H., Jiaang,W.T., Hwang,M.J. and Chen,X.
The dimeric transmembrane domain of prolyl dipeptidase DPP-IV contributes to its quaternary structure and enzymatic activities
Protein Sci (2010) 19, 1627-1638. PubMed Europe PubMed DOI
Deacon,C.F. and Holst,J.J.
Linagliptin, a xanthine-based dipeptidyl peptidase-4 inhibitor with an unusual profile for the treatment of type 2 diabetes
Expert Opin Investig Drugs (2010) 19, 133-140. PubMed Europe PubMed DOI I
Furuta,Y., Horiguchi,M., Sugaru,E., Ono-Kishino,M., Otani,M., Sakai,M., Masui,Y., Tsuchida,A., Sato,Y., Takubo,K., Hochigai,H., Kimura,H., Nakahira,H., Nakagawa,T. and Taiji,M.
Chronic administration of DSP-7238, a novel, potent, specific and substrate-selective DPP IV inhibitor, improves glycaemic control and beta-cell damage in diabetic mice
Diabetes Obes Metab (2010) 12, 421-430. PubMed Europe PubMed DOI I
Haddley,K.
Dutogliptin tartrate: dipeptidyl peptidase 4 inhibitor treatment of diabetes
Drugs Future (2010) 35, 529-535. DOI I
Han,B., Huan,Y., Lin,Z.Y., Li,P., Shen,Z.F., Yin,D.L. and Huang,H.H.
[Design, synthesis and in vitro activity of glycinamide-bearing compounds as DPP-IV inhibitors]
Yao Xue Xue Bao (2010) 45, 1379-1384. PubMed Europe PubMed I
Jang,S., Chung,T.Y., Shin,J., Lin,K.L., Tzen,J.T. and Li,F.Y.
Docking study of the precursor peptide of mastoparan onto its putative processing enzyme, dipeptidyl peptidase IV: a revisit to molecular ticketing
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Jiang,Y.K.
Molecular docking and 3D-QSAR studies on beta-phenylalanine derivatives as dipeptidyl peptidase IV inhibitors
J Mol Model (2010) 16, 1239-1249. PubMed Europe PubMed DOI I
Johnson,K.M.
Dutogliptin, a dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes mellitus
Curr Opin Investig Drugs (2010) 11, 455-463. PubMed Europe PubMed I
Kawaguchi,M., Okabe,T., Terai,T., Hanaoka,K., Kojima,H., Minegishi,I. and Nagano,T.
A time-resolved fluorescence probe for dipeptidyl peptidase 4 and its application in inhibitor screening
Chemistry (2010) 16, 13479-13486. PubMed Europe PubMed DOI A I
Kichik,N., Tarrago,T. and Giralt,E.
Simultaneous (19)F NMR screening of prolyl oligopeptidase and dipeptidyl peptidase IV inhibitors
Chembiochem (2010) 11, 1115-1119. PubMed Europe PubMed DOI I
Kirby,M., Yu,D.M., O'Connor,S. and Gorrell,M.D.
Inhibitor selectivity in the clinical application of dipeptidyl peptidase-4 inhibition
Clin Sci (Lond) (2010) 118, 31-41. PubMed Europe PubMed DOI I
Lin,C.T., Tang,H.Y., Han,Y.S., Liu,H.P., Huang,S.F., Chien,C.H., Shyy,J., Chiu,J.J. and Chen,X.
Downregulation of signaling-active IGF-1 by dipeptidyl peptidase IV (DPP-IV)
Int J Biomed Sci (2010) 6, 301-309. PubMed Europe PubMed
Lone,A.M., Nolte,W.M., Tinoco,A.D. and Saghatelian,A.
Peptidomics of the prolyl peptidases
AAPS J (2010) 12, 483-491. PubMed Europe PubMed DOI P
Mattei,P., Boehringer,M., Di Giorgio,P., Fischer,H., Hennig,M., Huwyler,J., Kocer,B., Kuhn,B., Loeffler,B.M., Macdonald,A., Narquizian,R., Rauber,E., Sebokova,E. and Sprecher,U.
Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Bioorg Med Chem Lett (2010) 20, 1109-1113. PubMed Europe PubMed DOI S I
Meng,W., Brigance,R.P., Chao,H.J., Fura,A., Harrity,T., Marcinkeviciene,J., O'Connor,S.P., Tamura,J.K., Xie,D., Zhang,Y., Klei,H.E., Kish,K., Weigelt,C.A., Turdi,H., Wang,A., Zahler,R., Kirby,M.S. and Hamann,L.G.
Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors
J Med Chem (2010) 53, 5620-5628. PubMed Europe PubMed DOI I
Mulakayala,N., Reddy CH,U., Iqbal,J. and Pal,M.
Synthesis of dipeptidyl peptidase-4 inhibitors: a brief overview
Tetrahedron (2010) 66, 4919-4938. DOI I
Neumiller,J.J., Wood,L. and Campbell,R.K.
Dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus
Pharmacotherapy (2010) 30, 463-484. PubMed Europe PubMed DOI V I
Nishio,Y., Kimura,H., Tosaki,S., Sugaru,E., Sakai,M., Horiguchi,M., Masui,Y., Ono,M., Nakagawa,T. and Nakahira,H.
Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore
Bioorg Med Chem Lett (2010) 20, 7246-7249. PubMed Europe PubMed DOI I
Peters,J.U. and Mattei,P.
5. Dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes
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Sauve,M., Ban,K., Momen,M.A., Zhou,Y.Q., Henkelman,R.M., Husain,M. and Drucker,D.J.
Genetic deletion or pharmacological inhibition of dipeptidyl peptidase-4 improves cardiovascular outcomes after myocardial infarction in mice
Diabetes (2010) 59, 1063-1073. PubMed Europe PubMed DOI K I
Tanaka-Amino,K., Matsumoto,K., Hatakeyama,Y., Takakura,S. and Mutoh,S.
ASP4000, a slow-binding dipeptidyl peptidase 4 inhibitor, has antihyperglycemic activity of long duration in Zucker fatty rats
Acta Diabetol (2010) 47, 43-48. PubMed Europe PubMed DOI I
Tinoco,A.D., Tagore,D.M. and Saghatelian,A.
Expanding the dipeptidyl peptidase 4-regulated peptidome via an optimized peptidomics platform
J Am Chem Soc (2010) 132, 3819-3830. PubMed Europe PubMed DOI
Vanderheyden,M., Vrints,C., Verstreken,S., Bartunek,J., Beunk,J. and Goethals,M.
B-type natriuretic peptide as a marker of heart failure: new insights from biochemistry and clinical implications
Biomark Med (2010) 4, 315-320. PubMed Europe PubMed DOI
Xu,F., Corley,E., Zacuto,M., Conlon,D.A., Pipik,B., Humphrey,G., Murry,J. and Tschaen,D.
Asymmetric synthesis of a potent, aminopiperidine-fused imidazopyridine dipeptidyl peptidase IV inhibitor
J Org Chem (2010) 75, 1343-1353. PubMed Europe PubMed DOI I
Yeh,T.K., Tsai,T.Y., Hsu,T., Cheng,J.H., Chen,X., Song,J.S., Shy,H.S., Chiou,M.C., Chien,C.H., Tseng,Y.J., Huang,C.Y., Yeh,K.C., Huang,Y.L., Huang,C.H., Huang,Y.W., Wang,M.H., Tang,H.K., Chao,Y.S., Chen,C.T. and Jiaang,W.T.
(2S,4S)-1-[2-(1,1-Dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV
Bioorg Med Chem Lett (2010) 20, 3596-3600. PubMed Europe PubMed DOI I
Zhu,Y., Xia,S., Zhu,M., Yi,W., Cheng,J., Song,G., Li,Z. and Lu,P.
Synthesis, biological assay in vitro and molecular docking studies of new imidazopyrazinone derivatives as potential dipeptidyl peptidase IV inhibitors
Eur J Med Chem (2010) 45, 4953-4962. PubMed Europe PubMed DOI I

2009

Abid,K., Rochat,B., Lassahn,P.G., Stocklin,R., Michalet,S., Brakch,N., Aubert,J.F., Vatansever,B., Tella,P., De Meester,I. and Grouzmann,E.
Kinetic study of neuropeptide Y (NPY) proteolysis in blood and identification of NPY3-35: a new peptide generated by plasma kallikrein
J Biol Chem (2009) 284, 24715-24724. PubMed Europe PubMed DOI PMC EPMC P
Ammirati,M.J., Andrews,K.M., Boyer,D.D., Brodeur,A.M., Danley,D.E., Doran,S.D., Hulin,B., Liu,S., McPherson,R.K., Orena,S.J., Parker,J.C., Polivkova,J., Qiu,X., Soglia,C.B., Treadway,J.L., VanVolkenburg,M.A., Wilder,D.C. and Piotrowski,D.W.
(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-y l)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor
Bioorg Med Chem Lett (2009) 19, 1991-1995. PubMed Europe PubMed DOI I
Arscott,W.T., LaBauve,A.E., May,V. and Wesley,U.V.
Suppression of neuroblastoma growth by dipeptidyl peptidase IV: relevance of chemokine regulation and caspase activation
Oncogene (2009) 28, 479-491. PubMed Europe PubMed DOI PMC EPMC
Asakawa,T., Moritoh,Y., Kataoka,O., Suzuki,N., Takeuchi,K. and Odaka,H.
A novel dipeptidyl peptidase-4 inhibitor, alogliptin (SYR-322), is effective in diabetic rats with sulfonylurea-induced secondary failure
Life Sci (2009) 85, 122-126. PubMed Europe PubMed DOI I
Betancort,J.M., Winn,D.T., Liu,R., Xu,Q., Liu,J., Liao,W., Chen,S.H., Carney,D., Hanway,D., Schmeits,J., Li,X., Gordon,E. and Campbell,D.A.
Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors
Bioorg Med Chem Lett (2009) 19, 4437-4440. PubMed Europe PubMed DOI I
Bouchard,L., Faucher,G., Tchernof,A., Deshaies,Y., Lebel,S., Hould,F.S., Marceau,P. and Vohl,M.C.
Comprehensive genetic analysis of the dipeptidyl peptidase-4 gene and cardiovascular disease risk factors in obese individuals
Acta Diabetol (2009) 46, 13-21. PubMed Europe PubMed DOI M
Cordero,O.J., Salgado,F.J. and Nogueira,M.
On the origin of serum CD26 and its altered concentration in cancer patients
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Edmondson,S.D., Mastracchio,A., Cox,J.M., Eiermann,G.J., He,H., Lyons,K.A., Patel,R.A., Patel,S.B., Petrov,A., Scapin,G., Wu,J.K., Xu,S., Zhu,B., Thornberry,N.A., Roy,R.S. and Weber,A.E.
Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors
Bioorg Med Chem Lett (2009) 19, 4097-4101. PubMed Europe PubMed DOI I
Frerker,N., Raber,K., Bode,F., Skripuletz,T., Nave,H., Klemann,C., Pabst,R., Stephan,M., Schade,J., Brabant,G., Wedekind,D., Jacobs,R., Jorns,A., Forssmann,U., Straub,R.H., Johannes,S., Hoffmann,T., Wagner,L., Demuth,H.U. and von Horsten,S.
Phenotyping of congenic dipeptidyl peptidase 4 (DP4) deficient Dark Agouti (DA) rats suggests involvement of DP4 in neuro-, endocrine, and immune functions
Clin Chem Lab Med (2009) 47, 275-287. PubMed Europe PubMed DOI
Gupta,R., Walunj,S.S., Tokala,R.K., Parsa,K.V., Singh,S.K. and Pal,M.
Emerging drug candidates of dipeptidyl peptidase IV (DPP IV) inhibitor class for the treatment of Type 2 Diabetes
Curr Drug Targets (2009) 10, 71-87. PubMed Europe PubMed DOI I
Gupta,R.C., Chhipa,L., Mandhare,A.B., Zambad,S.P., Chauthaiwale,V., Nadkarni,S.S. and Dutt,C.
Novel N-substituted 4-hydrazino piperidine derivative as a dipeptidyl peptidase IV inhibitor
Bioorg Med Chem Lett (2009) 19, 5021-5025. PubMed Europe PubMed DOI I
Havale,S.H. and Pal,M.
Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes
Bioorg Med Chem (2009) 17, 1783-1802. PubMed Europe PubMed DOI V I
Hsu,T., Chen,C.T., Tsai,T.Y., Cheng,J.H., Wu,S.Y., Chang,C.N., Chien,C.H., Yeh,K.C., Huang,Y.W., Huang,C.L., Huang,C.Y., Wu,S.H., Chiang,Y.K., Wang,M.H., Chao,Y.S., Chen,X. and Jiaang,W.T.
(1,3-diphenyl-1h-pyrazol-4-yl)-methylamine analogues as inhibitors of dipeptidyl peptidases
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Hu,C.X., Huang,H., Zhang,L., Huang,Y., Shen,Z.F., Cheng,K.D., Du,G.H. and Zhu,P.
A new screening method based on yeast-expressed human dipeptidyl peptidase IV and discovery of novel inhibitors
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Jost,M.M., Lamerz,J., Tammen,H., Menzel,C., De Meester,I., Lambeir,A.M., Augustyns,K., Scharpe,S., Zucht,H.D., Rose,H., Jurgens,M., Schulz-Knappe,P. and Budde,P.
In vivo profiling of DPP4 inhibitors reveals alterations in collagen metabolism and accumulation of an amyloid peptide in rat plasma
Biochem Pharmacol (2009) 77, 228-237. PubMed Europe PubMed DOI I
Kintscher,U.
Dipeptidyl peptidase-4 (DPP-4) lnhibtors: a new oral alternative [Dipeptidyl-Peptidase-4 (DPP-4)-lnhibitoren: neue orale Alternative]
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Kirino,Y., Sato,Y., Kamimoto,T., Kawazoe,K., Minakuchi,K. and Nakahori,Y.
Interrelationship of dipeptidyl peptidase IV (DPP4) with the development of diabetes, dyslipidaemia and nephropathy: a streptozotocin-induced model using wild-type and DPP4-deficient rats
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Klemann,C., Schade,J., Pabst,R., Leitner,S., Stiller,J., von Horsten,S. and Stephan,M.
CD26/dipeptidyl peptidase 4-deficiency alters thymic emigration patterns and leukocyte subsets in F344-rats age-dependently
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Krupina,N.A., Kushnareva,E.Y., Khlebnikova,N.N., Zolotov,N.N. and Kryzhanovskii,G.N.
Behavioral changes in rats induced by a dipeptidyl peptidase IV inhibitor methionyl-2(S)-cyanopyrrolidine: experimental model of anxiety-depression disorder
Bull Exp Biol Med (2009) 147, 285-290. PubMed Europe PubMed DOI I
Lim,K.S., Cho,J.Y., Kim,B.H., Kim,J.R., Kim,H.S., Kim,D.K., Kim,S.H., Yim,H.J., Lee,S.H., Shin,S.G., Jang,I.J. and Yu,K.S.
Pharmacokinetics and pharmacodynamics of LC15-0444, a novel dipeptidyl peptidase IV inhibitor, after multiple dosing in healthy volunteers
Br J Clin Pharmacol (2009) 68, 883-890. PubMed Europe PubMed DOI I
Matsuyama-Yokono,A., Tahara,A., Nakano,R., Someya,Y., Hayakawa,M. and Shibasaki,M.
Chronic inhibition of dipeptidyl peptidase-IV with ASP8497 improved the HbA(1c) level, glucose intolerance, and lipid parameter level in streptozotocin-nicotinamide-induced diabetic mice
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Matteucci,E. and Giampietro,O.
Dipeptidyl peptidase-4 (CD26): knowing the function before inhibiting the enzyme
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Nordhoff,S., Bulat,S., Cerezo-Galvez,S., Hill,O., Hoffmann-Enger,B., Lopez-Canet,M., Rosenbaum,C., Rummey,C., Thiemann,M., Matassa,V.G., Edwards,P.J. and Feurer,A.
The design of potent and selective inhibitors of DPP-4: optimization of ADME properties by amide replacements
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Nordhoff,S., Cerezo-Galvez,S., Deppe,H., Hill,O., Lopez-Canet,M., Rummey,C., Thiemann,M., Matassa,V.G., Edwards,P.J. and Feurer,A.
Discovery of beta-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV
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Nordhoff,S., Lopez-Canet,M., Hoffmann-Enger,B., Bulat,S., Cerezo-Galvez,S., Hill,O., Rosenbaum,C., Rummey,C., Thiemann,M., Matassa,V.G., Edwards,P.J. and Feurer,A.
From lead to preclinical candidate: optimization of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV
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Palalau,A.I., Tahrani,A.A., Piya,M.K. and Barnett,A.H.
DPP-4 inhibitors in clinical practice
Postgrad Med (2009) 121, 70-100. PubMed Europe PubMed DOI V I
Rungby,J.
Inhibition of dipeptidyl peptidase 4 by BI-1356, a new drug for the treatment of beta-cell failure in type 2 diabetes
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Saqib,U. and Siddiqi,M.I.
3D-QSAR studies on triazolopiperazine amide inhibitors of dipeptidyl peptidase-IV as anti-diabetic agents
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Thomas,L., Tadayyon,M. and Mark,M.
Chronic treatment with the dipeptidyl peptidase-4 inhibitor BI 1356 [(R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione] increases basal glucagon-like peptide-1 and improves glycemic control in diabetic rodent models
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Thornberry,N.A. and Gallwitz,B.
Mechanism of action of inhibitors of dipeptidyl-peptidase-4 (DPP-4)
Best Pract Res Clin Endocrinol Metab (2009) 23, 479-486. PubMed Europe PubMed DOI I
Tsai,T.Y., Hsu,T., Chen,C.T., Cheng,J.H., Chiou,M.C., Huang,C.H., Tseng,Y.J., Yeh,T.K., Huang,C.Y., Yeh,K.C., Huang,Y.W., Wu,S.H., Wang,M.H., Chen,X., Chao,Y.S. and Jiaang,W.T.
Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (2009) 19, 1908-1912. PubMed Europe PubMed DOI I
Tsai,T.Y., Hsu,T., Chen,C.T., Cheng,J.H., Yeh,T.K., Chen,X., Huang,C.Y., Chang,C.N., Yeh,K.C., Hsieh,S.H., Chien,C.H., Chang,Y.W., Huang,C.H., Huang,Y.W., Huang,C.L., Wu,S.H., Wang,M.H., Lu,C.T., Chao,Y.S. and Jiaang,W.T.
Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors
Bioorg Med Chem (2009) 17, 2388-2399. PubMed Europe PubMed DOI I
Tye,C.E., Pham,C.T., Simmer,J.P. and Bartlett,J.D.
DPPI may activate KLK4 during enamel formation
J Dent Res (2009) 88, 323-327. PubMed Europe PubMed DOI PMC EPMC
Wang,L., Zhang,B., Ji,J., Li,B., Yan,J., Zhang,W., Wu,Y. and Wang,X.
Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors
Eur J Med Chem (2009) 44, 3318-3322. PubMed Europe PubMed DOI I
Yazbeck,R., Howarth,G.S. and Abbott,C.A.
Dipeptidyl peptidase inhibitors, an emerging drug class for inflammatory disease?
Trends Pharmacol Sci (2009) 30, 600-607. PubMed Europe PubMed DOI I

2008

Ahn,J.H., Park,W.S., Jun,M.A., Shin,M.S., Kang,S.K., Kim,K.Y., Rhee,S.D., Bae,M.A., Kim,K.R., Kim,S.G., Kim,S.Y., Sohn,S.K., Kang,N.S., Lee,J.O., Lee,D.H., Cheon,H.G. and Kim,S.S.
Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (2008) 18, 6525-6529. PubMed Europe PubMed DOI I
Augstein,P., Berg,S., Heinke,P., Altmann,S., Salzsieder,E., Demuth,H.U. and Freyse,E.J.
Efficacy of the dipeptidyl peptidase IV inhibitor isoleucine thiazolidide (P32/98) in fatty Zucker rats with incipient and manifest impaired glucose tolerance
Diabetes Obes Metab (2008) 10, 850-861. PubMed Europe PubMed DOI I
Chia,C.W. and Egan,J.M.
Incretin-based therapies in type 2 diabetes mellitus
J Clin Endocrinol Metab (2008) 93, 3703-3716. PubMed Europe PubMed DOI PMC EPMC V I
Connolly,B.A., Sanford,D.G., Chiluwal,A.K., Healey,S.E., Peters,D.E., Dimare,M.T., Wu,W., Liu,Y., Maw,H., Zhou,Y., Li,Y., Jin,Z., Sudmeier,J.L., Lai,J.H. and Bachovchin,W.W.
Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety
J Med Chem (2008) 51, 6005-6013. PubMed Europe PubMed DOI I
Doupis,J. and Veves,A.
DPP4 Inhibitors: a new approach in diabetes treatment
Adv Ther (2008) 25, 627-643. PubMed Europe PubMed DOI V
Edmondson,S.D., Wei,L., Xu,J., Shang,J., Xu,S., Pang,J., Chaudhary,A., Dean,D.C., He,H., Leiting,B., Lyons,K.A., Patel,R.A., Patel,S.B., Scapin,G., Wu,J.K., Beconi,M.G., Thornberry,N.A. and Weber,A.E.
Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (2008) 18, 2409-2413. PubMed Europe PubMed DOI I
Fukushima,H., Hiratate,A., Takahashi,M., Mikami,A., Saito-Hori,M., Munetomo,E., Kitano,K., Chonan,S., Saito,H., Suzuki,A., Takaoka,Y. and Yamamoto,K.
Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors
Bioorg Med Chem (2008) 16, 4093-4106. PubMed Europe PubMed DOI I
Fukushima,H., Hiratate,A., Takahashi,M., Saito-Hori,M., Munetomo,E., Kitano,K., Saito,H., Takaoka,Y. and Yamamoto,K.
Synthesis and structure-activity relationships of potent 1-(2-substituted-aminoacetyl)-4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors
Chem Pharm Bull (Tokyo) (2008) 56, 1110-1117. PubMed Europe PubMed DOI I
Girardi,A.C., Fukuda,L.E., Rossoni,L.V., Malnic,G. and Reboucas,N.A.
Dipeptidyl peptidase IV inhibition downregulates Na+-H+ exchanger NHE3 in rat renal proximal tubule
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Gwaltney,S.L.
Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase IV
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Jun,M.A., Park,W.S., Kang,S.K., Kim,K.Y., Kim,K.R., Rhee,S.D., Bae,M.A., Kang,N.S., Sohn,S.K., Kim,S.G., Lee,J.O., Lee,D.H., Cheon,H.G., Kim,S.S. and Ahn,J.H.
Synthesis and biological evaluation of pyrazoline analogues with beta-amino acyl group as dipeptidyl peptidase IV inhibitors
Eur J Med Chem (2008) 43, 1889-1902. PubMed Europe PubMed DOI I
Kim,D., Kowalchick,J.E., Brockunier,L.L., Parmee,E.R., Eiermann,G.J., Fisher,M.H., He,H., Leiting,B., Lyons,K., Scapin,G., Patel,S.B., Petrov,A., Pryor,K.D., Roy,R.S., Wu,J.K., Zhang,X., Wyvratt,M.J., Zhang,B.B., Zhu,L., Thornberry,N.A. and Weber,A.E.
Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines
J Med Chem (2008) 51, 589-602. PubMed Europe PubMed DOI I
Koivisto,V.
Discovery of dipeptidyl-peptidase IV - a 40 year journey from bench to patient
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Kondo,T., Nekado,T., Sugimoto,I., Ochi,K., Takai,S., Kinoshita,A., Hatayama,A., Yamamoto,S., Kawabata,K., Nakai,H. and Toda,M.
Discovery of long-acting N-(cyanomethyl)-N-alkyl-l-prolinamide inhibitors of dipeptidyl peptidase IV
Bioorg Med Chem (2008) 16, 190-208. PubMed Europe PubMed DOI I
Kondo,T., Nekado,T., Sugimoto,I., Ochi,K., Takai,S., Kinoshita,A., Hatayama,A., Yamamoto,S., Kishikawa,K., Nakai,H. and Toda,M.
Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group
Bioorg Med Chem (2008) 16, 1613-1631. PubMed Europe PubMed DOI I
Liang,G.B., Qian,X., Biftu,T., Singh,S., Gao,Y.D., Scapin,G., Patel,S., Leiting,B., Patel,R., Wu,J., Zhang,X., Thornberry,N.A. and Weber,A.E.
Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design
Bioorg Med Chem Lett (2008) 18, 3706-3710. PubMed Europe PubMed DOI S I
Lu,I.L., Tsai,K.C., Chiang,Y.K., Jiaang,W.T., Wu,S.H., Mahindroo,N., Chien,C.H., Lee,S.J., Chen,X., Chao,Y.S. and Wu,S.Y.
A three-dimensional pharmacophore model for dipeptidyl peptidase IV inhibitors
Eur J Med Chem (2008) 43, 1603-1611. PubMed Europe PubMed DOI T I
Madsbad,S., Krarup,T., Deacon,C.F. and Holst,J.J.
Glucagon-like peptide receptor agonists and dipeptidyl peptidase-4 inhibitors in the treatment of diabetes: a review of clinical trials
Curr Opin Clin Nutr Metab Care (2008) 11, 491-499. PubMed Europe PubMed DOI I
Matsuyama-Yokono,A., Tahara,A., Nakano,R., Someya,Y., Nagase,I., Hayakawa,M. and Shibasaki,M.
ASP8497 is a novel selective and competitive dipeptidyl peptidase-IV inhibitor with antihyperglycemic activity
Biochem Pharmacol (2008) 76, 98-107. PubMed Europe PubMed DOI I
Metzler,W.J., Yanchunas,J., Weigelt,C., Kish,K., Klei,H.E., Xie,D., Zhang,Y., Corbett,M., Tamura,J.K., He,B., Hamann,L.G., Kirby,M.S. and Marcinkeviciene,J.
Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation
Protein Sci (2008) 17, 240-250. PubMed Europe PubMed DOI PMC EPMC S I
Moore,K.B. and Saudek,C.D.
Therapeutic potential of dipeptidyl peptidase-IV inhibitors in patients with diabetes mellitus
Am J Ther (2008) 15, 484-491. PubMed Europe PubMed DOI V I
Moritoh,Y., Takeuchi,K., Asakawa,T., Kataoka,O. and Odaka,H.
Chronic administration of alogliptin, a novel, potent, and highly selective dipeptidyl peptidase-4 inhibitor, improves glycemic control and beta-cell function in obese diabetic ob/ob mice
Eur J Pharmacol (2008) 588, 325-332. PubMed Europe PubMed DOI I
Neumiller,J.J., Odegard,P.S., White,J.R., Jr., Setter,S.M. and Campbell,R.K.
Looking to the future: focus on DPP-4 inhibitors for the treatment of type 2 diabetes and emerging therapies
Diabetes Educ (2008) 34, 183-200. PubMed Europe PubMed DOI I
Nitta,A., Fujii,H., Sakami,S., Nishimura,Y., Ohyama,T., Satoh,M., Nakaki,J., Satoh,S., Inada,C., Kozono,H., Kumagai,H., Shimamura,M., Fukazawa,T. and Kawai,H.
(3R)-3-Amino-4-(2,4,5-trifluorophenyl)-N-{4-[6-(2-methoxyethoxy)benzothiazol-2-yl]tetrahydropyran-4-yl}butanamide as a potent dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Bioorg Med Chem Lett (2008) 18, 5435-5438. PubMed Europe PubMed DOI I
Ohnuma,K., Takahashi,N., Yamochi,T., Hosono,O., Dang,N.H. and Morimoto,C.
Role of CD26/dipeptidyl peptidase IV in human T cell activation and function
Front Biosci (2008) 13, 2299-2310. PubMed Europe PubMed DOI V
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From the bench to the bedside: dipeptidyl peptidase IV inhibitors, a new class of oral antihyperglycemic agents
Curr Opin Drug Discov Devel (2008) 11, 512-532. PubMed Europe PubMed I
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Emerging role of dipeptidyl peptidase-4 inhibitors in the management of type 2 diabetes
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Sattigeri,J.A., Andappan,M.M., Kishore,K., Thangathirupathy,S., Sundaram,S., Singh,S., Sharma,S., Davis,J.A., Chugh,A. and Bansal,V.S.
Discovery of conformationally rigid 3-azabicyclo[3.1.0]hexane-derived dipeptidyl peptidase-IV inhibitors
Bioorg Med Chem Lett (2008) 18, 4087-4091. PubMed Europe PubMed DOI I
Schade,J., Stephan,M., Schmiedl,A., Wagner,L., Niestroj,A.J., Demuth,H.U., Frerker,N., Klemann,C., Raber,K.A., Pabst,R. and von Horsten,S.
Regulation of expression and function of dipeptidyl peptidase 4 (DP4), DP8/9, and DP10 in allergic responses of the lung in rats
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Someya,Y., Tahara,A., Nakano,R., Matsuyama-Yokono,A., Nagase,I., Fukunaga,Y., Takasu,T., Hayakawa,M. and Shibasaki,M.
Pharmacological profile of ASP8497, a novel, selective, and competitive dipeptidyl peptidase-IV inhibitor, in vitro and in vivo
Naunyn Schmiedebergs Arch Pharmacol (2008) 377, 209-217. PubMed Europe PubMed DOI I
Taldone,T., Zito,S.W. and Talele,T.T.
Inhibition of dipeptidyl peptidase-IV (DPP-IV) by atorvastatin
Bioorg Med Chem Lett (2008) 18, 479-484. PubMed Europe PubMed DOI I
Tanaka-Amino,K., Matsumoto,K., Hatakeyama,Y., Shima,I., Takakura,S. and Muto,S.
ASP4,000, a novel, selective, dipeptidyl peptidase 4 inhibitor with antihyperglycemic activity
Eur J Pharmacol (2008) 590, 444-449. PubMed Europe PubMed DOI I
Thomas,L., Eckhardt,M., Langkopf,E., Tadayyon,M., Himmelsbach,F. and Mark,M.
(R)-8-(3-Amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors
J Pharmacol Exp Ther (2008) 325, 175-182. PubMed Europe PubMed DOI I
Tsai,H.J., Chou,S.Y., Chuang,S.H., Chen,C.C. and Hsu,F.L.
D-420720, a novel orally active sulfonamide compound dipeptidyl peptidase IV inhibitor: structure and activity relationship of arylsulfonamide to dipeptidyl peptidase IV inhibition
Drug Dev Res (2008) 69, 514-519. DOI I
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Dipeptidyl peptidase-IV (DPP-IV) inhibitory activity of metformin
Pharmacologyonline (2008) 2, 372-378. I
Wallace,M.B., Feng,J., Zhang,Z., Skene,R.J., Shi,L., Caster,C.L., Kassel,D.B., Xu,R. and Gwaltney,S.L.
Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (2008) 18, 2362-2367. PubMed Europe PubMed DOI I
Wang,Y., Serradell,N., Rosa,E. and Bolos,J.
Alogliptin benzoate. Dipeptidyl-peptidase IV (DPP IV) inhibitor treatment of type 2 diabetes
Drugs Future (2008) 33, 7-12. DOI I
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Dipeptidyl peptidase-4 as a new target of action for type 2 diabetes mellitus: a systematic review
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2007

Ahn,J.H., Shin,M.S., Jun,M.A., Jung,S.H., Kang,S.K., Kim,K.R., Rhee,S.D., Kang,N.S., Kim,S.Y., Sohn,S.K., Kim,S.G., Jin,M.S., Lee,J.O., Cheon,H.G. and Kim,S.S.
Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors
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Backes,B.J., Longenecker,K., Hamilton,G.L., Stewart,K., Lai,C., Kopecka,H., von Geldern,T.W., Madar,D.J., Pei,Z., Lubben,T.H., Zinker,B.A., Tian,Z., Ballaron,S.J., Stashko,M.A., Mika,A.K., Beno,D.W., Kempf-Grote,A.J., Black-Schaefer,C., Sham,H.L. and Trevillyan,J.M.
Pyrrolidine-constrained phenethylamines: the design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit
Bioorg Med Chem Lett (2007) 17, 2005-2012. PubMed Europe PubMed DOI I
Biftu,T., Feng,D., Qian,X., Liang,G.B., Kieczykowski,G., Eiermann,G., He,H., Leiting,B., Lyons,K., Petrov,A., Sinha-Roy,R., Zhang,B., Scapin,G., Patel,S., Gao,Y.D., Singh,S., Wu,J., Zhang,X., Thornberry,N.A. and Weber,A.E.
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoro ethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
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Biftu,T., Scapin,G., Singh,S., Feng,D., Becker,J.W., Eiermann,G., He,H., Lyons,K., Patel,S., Petrov,A., Sinha-Roy,R., Zhang,B., Wu,J., Zhang,X., Doss,G.A., Thornberry,N.A. and Weber,A.E.
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin
Bioorg Med Chem Lett (2007) 17, 3384-3387. PubMed Europe PubMed DOI S I
Campbell,R.K.
Rationale for dipeptidyl peptidase 4 inhibitors: a new class of oral agents for the treatment of type 2 diabetes mellitus
Ann Pharmacother (2007) 41, 51-60. PubMed Europe PubMed DOI V I
Chahal,H. and Chowdhury,T.A.
Gliptins: a new class of oral hypoglycaemic agent
QJM (2007) 100, 671-677. PubMed Europe PubMed DOI I
Chen,P., Caldwell,C.G., Mathvink,R.J., Leiting,B., Marsilio,F., Patel,R.A., Wu,J.K., He,H., Lyons,K.A., Thornberry,N.A. and Weber,A.E.
Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes
Bioorg Med Chem Lett (2007) 17, 5853-5857. PubMed Europe PubMed DOI I
Corbett,J.W., Dirico,K., Song,W., Boscoe,B.P., Doran,S.D., Boyer,D., Qiu,X., Ammirati,M., VanVolkenburg,M.A., McPherson,R.K., Parker,J.C. and Cox,E.D.
Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors
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Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors
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Davoodi,J., Kelly,J., Gendron,N.H. and MacKenzie,A.E.
The Simpson-Golabi-Behmel syndrome causative glypican-3, binds to and inhibits the dipeptidyl peptidase activity of CD26
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Dipeptidyl peptidase 4 inhibition with sitagliptin: a new therapy for Type 2 diabetes
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Duffy,J.L., Kirk,B.A., Wang,L., Eiermann,G.J., He,H., Leiting,B., Lyons,K.A., Patel,R.A., Patel,S.B., Petrov,A., Scapin,G., Wu,J.K., Thornberry,N.A. and Weber,A.E.
4-Aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV
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Duffy,N.A., Green,B.D., Irwin,N., Gault,V.A., McKillop,A.M., O'Harte,F.P. and Flatt,P.R.
Effects of antidiabetic drugs on dipeptidyl peptidase IV activity: nateglinide is an inhibitor of DPP IV and augments the antidiabetic activity of glucagon-like peptide-1
Eur J Pharmacol (2007) 568, 278-286. PubMed Europe PubMed DOI I
Eckhardt,M., Langkopf,E., Mark,M., Tadayyon,M., Thomas,L., Nar,H., Pfrengle,W., Guth,B., Lotz,R., Sieger,P., Fuchs,H. and Himmelsbach,F.
8-(3-(R)-Aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin -2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes
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Epstein,B.J.
Drug evaluation: PSN-9301, a short-acting inhibitor of dipeptidyl peptidase IV
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Curr Top Med Chem (2007) 7, 597-608. PubMed Europe PubMed DOI I
Frerker,N., Wagner,L., Wolf,R., Heiser,U., Hoffmann,T., Rahfeld,J.U., Schade,J., Karl,T., Naim,H.Y., Alfalah,M., Demuth,H.U. and von Horsten,S.
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Efficient conversion of tetrapeptide-based TSAO prodrugs to the parent drug by dipeptidyl-peptidase IV (DPPIV/CD26)
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The influence of hepatic impairment on the pharmacokinetics of the dipeptidyl peptidase IV (DPP-4) inhibitor vildagliptin
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Hiramatsu,H., Kyono,K., Yamamoto,A., Saeki,K., Shima,H., Sugiyama,S., Inaka,K. and Shimizu,R.
Crystal structures of human dipeptidyl peptidase IV in its apo and diprotin B-complexed forms
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Idris,I. and Donnelly,R.
Dipeptidyl peptidase-IV inhibitors: a major new class of oral antidiabetic drug
Diabetes Obes Metab (2007) 9, 153-165. PubMed Europe PubMed DOI I
Jackson,E.K., Zhang,M., Liu,W. and Mi,Z.
Inhibition of renal dipeptidyl peptidase IV enhances peptide YY1-36-induced potentiation of angiotensin II-mediated renal vasoconstriction in spontaneously hypertensive rats
J Pharmacol Exp Ther (2007) 323, 431-437. PubMed Europe PubMed DOI
Kaelin,D.E., Smenton,A.L., Eiermann,G.J., He,H., Leiting,B., Lyons,K.A., Patel,R.A., Patel,S.B., Petrov,A., Scapin,G., Wu,J.K., Thornberry,N.A., Weber,A.E. and Duffy,J.L.
4-Arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV
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Kondo,T., Sugimoto,I., Nekado,T., Ochi,K., Ohtani,T., Tajima,Y., Yamamoto,S., Kawabata,K., Nakai,H. and Toda,M.
Design and synthesis of long-acting inhibitors of dipeptidyl peptidase IV
Bioorg Med Chem (2007) 15, 2715-2735. PubMed Europe PubMed DOI I
Kondo,T., Nekado,T., Sugimoto,I., Ochi,K., Takai,S., Kinoshita,A., Tajima,Y., Yamamoto,S., Kawabata,K., Nakai,H. and Toda,M.
Design and synthesis of new potent dipeptidyl peptidase IV inhibitors with enhanced ex vivo duration
Bioorg Med Chem (2007) 15, 2631-2650. PubMed Europe PubMed DOI I
Koo,K.D., Kim,M.J., Kim,S., Kim,K.H., Hong,S.Y., Hur,G.C., Yim,H.J., Kim,G.T., Han,H.O., Kwon,O.H., Kwon,T.S., Koh,J.S. and Lee,C.S.
Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones
Bioorg Med Chem Lett (2007) 17, 4167-4172. PubMed Europe PubMed DOI S I
Kowalchick,J.E., Leiting,B., Pryor,K.D., Marsilio,F., Wu,J.K., He,H., Lyons,K.A., Eiermann,G.J., Petrov,A., Scapin,G., Patel,R.A., Thornberry,N.A., Weber,A.E. and Kim,D.
Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors
Bioorg Med Chem Lett (2007) 17, 5934-5939. PubMed Europe PubMed DOI S I
Kuhn,B., Hennig,M. and Mattei,P.
Molecular recognition of ligands in dipeptidyl peptidase IV
Curr Top Med Chem (2007) 7, 609-619. PubMed Europe PubMed DOI V
Lai,J.H., Wu,W., Zhou,Y., Maw,H.H., Liu,Y., Milo,L.J., Jr., Poplawski,S.E., Henry,G.D., Sudmeier,J.L., Sanford,D.G. and Bachovchin,W.W.
Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines
J Med Chem (2007) 50, 2391-2398. PubMed Europe PubMed DOI I
Lai,K.S., Ho,N.H., Cheng,J.D. and Tung,C.H.
Selective fluorescence probes for dipeptidyl peptidase activity - fibroblast activation protein and dipeptidyl peptidase IV
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Liang,G.B., Qian,X., Feng,D., Biftu,T., Eiermann,G., He,H., Leiting,B., Lyons,K., Petrov,A., Sinha-Roy,R., Zhang,B., Wu,J., Zhang,X., Thornberry,N.A. and Weber,A.E.
Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes
Bioorg Med Chem Lett (2007) 17, 1903-1907. PubMed Europe PubMed DOI I
Lubbers,T., Bohringer,M., Gobbi,L., Hennig,M., Hunziker,D., Kuhn,B., Loffler,B., Mattei,P., Narquizian,R., Peters,J.U., Ruff,Y., Wessel,H.P. and Wyss,P.
1,3-Disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (2007) 17, 2966-2970. PubMed Europe PubMed DOI I
Maes,M.B., Scharpe,S. and De Meester,I.
Dipeptidyl peptidase II (DPPII), a review
Clin Chim Acta (2007) 380, 31-49. PubMed Europe PubMed DOI V
O'Farrell,A.M., Van Vliet,A., Abou Farha,K., Cherrington,J.M., Campbell,D.A., Li,X., Hanway,D., Li,J. and Guler,H.P.
Pharmacokinetic and pharmacodynamic assessments of the dipeptidyl peptidase-4 inhibitor PHX1149: double-blind, placebo-controlled, single- and multiple-dose studies in healthy subjects
Clin Ther (2007) 29, 1692-1705. PubMed Europe PubMed DOI I
Oefner,C., Pierau,S., Schulz,H. and Dale,G.E.
Structural studies of a bifunctional inhibitor of neprilysin and DPP-IV
Acta Crystallogr D Biol Crystallogr (2007) 63, 975-981. PubMed Europe PubMed DOI S I
Panina,G.
The DPP-4 inhibitor vildagliptin: robust glycaemic control in type 2 diabetes and beyond
Diabetes Obes Metab (2007) 9 Suppl 1, 32-39. PubMed Europe PubMed DOI I
Pei,Z., Li,X., von Geldern,T.W., Longenecker,K., Pireh,D., Stewart,K.D., Backes,B.J., Lai,C., Lubben,T.H., Ballaron,S.J., Beno,D.W., Kempf-Grote,A.J., Sham,H.L. and Trevillyan,J.M.
Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors
J Med Chem (2007) 50, 1983-1987. PubMed Europe PubMed DOI I
Peters,J.U.
11 Years of cyanopyrrolidines as DPP-IV inhibitors
Curr Top Med Chem (2007) 7, 579-595. PubMed Europe PubMed DOI I
Pissurlenkar,R.R., Shaikh,M.S. and Coutinho,E.C.
3D-QSAR studies of dipeptidyl peptidase IV inhibitors using a docking based alignment
J Mol Model (2007) 13, 1047-1071. PubMed Europe PubMed DOI I
Reinhold,D., Biton,A., Goihl,A., Pieper,S., Lendeckel,U., Faust,J., Neubert,K., Bank,U., Tager,M., Ansorge,S. and Brocke,S.
Dual inhibition of dipeptidyl peptidase IV and aminopeptidase N suppresses inflammatory immune responses
Ann N Y Acad Sci (2007) 1110, 402-409. PubMed Europe PubMed DOI
Rosenstock,J. and Zinman,B.
Dipeptidyl peptidase-4 inhibitors and the management of type 2 diabetes mellitus
Curr Opin Endocrinol Diabetes Obes (2007) 14, 98-107. PubMed Europe PubMed DOI I
Ruth,D.M., Buckley,S.J., O'Connor,B.F. and O'Fagain,C.
Solvent and thermal stability, and pH kinetics, of proline-specific dipeptidyl peptidase IV-like enzyme from bovine serum
Enzyme Microb Technol (2007) 41, 307-311. DOI
Sakashita,H., Akahoshi,F., Yoshida,T., Kitajima,H., Hayashi,Y., Ishii,S., Takashina,Y., Tsutsumiuchi,R. and Ono,S.
Lead optimization of [(S)-gamma-(arylamino)prolyl]thiazolidine focused on gamma-substituent: indoline compounds as potent DPP-IV inhibitors
Bioorg Med Chem (2007) 15, 641-655. PubMed Europe PubMed DOI I
Scott,R., Wu,M., Sanchez,M. and Stein,P.
Efficacy and tolerability of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy over 12 weeks in patients with type 2 diabetes
Int J Clin Pract (2007) 61, 171-180. PubMed Europe PubMed DOI I
Sebokova,E., Christ,A.D., Boehringer,M. and Mizrahi,J.
Dipeptidyl peptidase IV inhibitors: the next generation of new promising therapies for the management of type 2 diabetes
Curr Top Med Chem (2007) 7, 547-555. PubMed Europe PubMed DOI V I
Sheehan,S.M., Mest,H.J., Watson,B.M., Klimkowski,V.J., Timm,D.E., Cauvin,A., Parsons,S.H., Shi,Q., Canada,E.J., Wiley,M.R., Ruehter,G., Evers,B., Petersen,S., Blaszczak,L.C., Pulley,S.R., Margolis,B.J., Wishart,G.N., Renson,B., Hankotius,D., Mohr,M., Zechel,J.C., Michael Kalbfleisch,J., Dingess-Hammond,E.A., Boelke,A. and Weichert,A.G.
Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site
Bioorg Med Chem Lett (2007) 17, 1765-1768. PubMed Europe PubMed DOI S I
Simpkins,L.M., Bolton,S., Pi,Z., Sutton,J.C., Kwon,C., Zhao,G., Magnin,D.R., Augeri,D.J., Gungor,T., Rotella,D.P., Sun,Z., Liu,Y., Slusarchyk,W.S., Marcinkeviciene,J., Robertson,J.G., Wang,A., Robl,J.A., Atwal,K.S., Zahler,R.L., Parker,R.A., Kirby,M.S. and Hamann,L.G.
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (2007) 17, 6476-6480. PubMed Europe PubMed DOI I
Thielitz,A., Reinhold,D., Vetter,R., Bank,U., Helmuth,M., Hartig,R., Wrenger,S., Wiswedel,I., Lendeckel,U., Kahne,T., Neubert,K., Faust,J., Zouboulis,C.C., Ansorge,S. and Gollnick,H.
Inhibitors of dipeptidyl peptidase IV and aminopeptidase N target major pathogenetic steps in acne initiation
J Invest Dermatol (2007) 127, 1042-1051. PubMed Europe PubMed DOI T I
Thompson,M.A., Ohnuma,K., Abe,M., Morimoto,C. and Dang,N.H.
CD26/dipeptidyl peptidase IV as a novel therapeutic target for cancer and immune disorders
Mini Rev Med Chem (2007) 7, 253-273. PubMed Europe PubMed DOI T
Thornberry,N.A. and Weber,A.E.
Discovery of JANUVIA (Sitagliptin), a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Curr Top Med Chem (2007) 7, 557-568. PubMed Europe PubMed DOI I
Tran,T., Quan,C., Edosada,C.Y., Mayeda,M., Wiesmann,C., Sutherlin,D. and Wolf,B.B.
Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP
Bioorg Med Chem Lett (2007) 17, 1438-1442. PubMed Europe PubMed DOI I
Wright,S.W., Ammirati,M.J., Andrews,K.M., Brodeur,A.M., Danley,D.E., Doran,S.D., Lillquist,J.S., Liu,S., McClure,L.D., McPherson,R.K., Olson,T.V., Orena,S.J., Parker,J.C., Rocke,B.N., Soeller,W.C., Soglia,C.B., Treadway,J.L., VanVolkenburg,M.A., Zhao,Z. and Cox,E.D.
(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: synthesis, in vitro, in vivo, and X-ray crystallographic characterization
Bioorg Med Chem Lett (2007) 17, 5638-5642. PubMed Europe PubMed DOI I
Yoshida,T., Sakashita,H., Akahoshi,F. and Hayashi,Y.
[(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors
Bioorg Med Chem Lett (2007) 17, 2618-2621. PubMed Europe PubMed DOI I
Zeng,J., Liu,G., Tang,Y. and Jiang,H.
3D-QSAR studies on fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors by CoMFA and CoMSIA
J Mol Model (2007) 13, 993-1000. PubMed Europe PubMed DOI I

2006

[YEAR:20-12-2006]Bank,U., Heimburg,A., Helmuth,M., Stefin,S., Lendeckel,U., Reinhold,D., Faust,J., Fuchs,P., Sens,B., Neubert,K., Tager,M. and Ansorge,S.
Triggering endogenous immunosuppressive mechanisms by combined targeting of dipeptidyl peptidase IV (DPIV/CD26) and aminopeptidase N (APN/ CD13) - a novel approach for the treatment of inflammatory bowel disease
Int Immunopharmacol (20-12-2006) 6, 1925-1934. PubMed Europe PubMed DOI I
Barnett,A.
DPP-4 inhibitors and their potential role in the management of type 2 diabetes
Int J Clin Pract (2006) 60, 1454-1470. PubMed Europe PubMed DOI V I
Bjelke,J.R., Kanstrup,A.B. and Rasmussen,H.B.
Selectivity among dipeptidyl peptidases of the S9b family
Cell Mol Biol Incl Cyto Enzymol (2006) 52, 3-7. PubMed Europe PubMed DOI P
[YEAR:27-10-2006]Brandt,I., Lambeir,A.M., Ketelslegers,J.M., Vanderheyden,M., Scharpe,S. and De Meester,I.
Dipeptidyl-peptidase IV converts intact B-type natriuretic peptide into its des-SerPro form
Clin Chem (27-10-2006) 52, 82-87. PubMed Europe PubMed DOI I
Edmondson,S.D., Mastracchio,A., Mathvink,R.J., He,J., Harper,B., Park,Y.J., Beconi,M., Di Salvo,J., Eiermann,G.J., He,H., Leiting,B., Leone,J.F., Levorse,D.A., Lyons,K., Patel,R.A., Patel,S.B., Petrov,A., Scapin,G., Shang,J., Roy,R.S., Smith,A., Wu,J.K., Xu,S., Zhu,B., Thornberry,N.A. and Weber,A.E.
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1 ,2,4]triazolo[1,5-a]- pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
J Med Chem (2006) 49, 3614-3627. PubMed Europe PubMed DOI I
[YEAR:22-6-2006]Emanuele,E., Minoretti,P., Martinelli,V., Pesenti,S., Olivieri,V., Aldeghi,A. and Politi,P.
Circulating levels of soluble CD26 are associated with phobic anxiety in women
Prog Neuropsychopharmacol Biol Psychiatry (22-6-2006) 30, 1334-1336. PubMed Europe PubMed DOI
[YEAR:24-8-2006]Garcia-Aparicio,C., Bonache,M.C., De Meester,I., San-Felix,A., Balzarini,J., Camarasa,M.J. and Velazquez,S.
Design and discovery of a novel dipeptidyl-peptidase IV (CD26)-based prodrug approach
J Med Chem (24-8-2006) 49, 5339-5351. PubMed Europe PubMed DOI
[YEAR:18-8-2006]Gilmore,B.F., Carson,L., McShane,L.L., Quinn,D., Coulter,W.A. and Walker,B.
Synthesis, kinetic evaluation, and utilization of a biotinylated dipeptide proline diphenyl phosphonate for the disclosure of dipeptidyl peptidase IV-like serine proteases
Biochem Biophys Res Commun (18-8-2006) 347, 373-379. PubMed Europe PubMed DOI I
[YEAR:6-6-2006]Gilmore,B.F., Lynas,J.F., Scott,C.J., McGoohan,C., Martin,L. and Walker,B.
Dipeptide proline diphenyl phosphonates are potent, irreversible inhibitors of seprase (FAPalpha)
Biochem Biophys Res Commun (6-6-2006) 346, 436-446. PubMed Europe PubMed DOI I
Green,B.D., Flatt,P.R. and Bailey,C.J.
Inhibition of dipeptidylpeptidase IV activity as a therapy of Type 2 diabetes
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[YEAR:27-7-2006]Green,B.D., Irwin,N., Duffy,N.A., Gault,V.A., O'Harte,F.P. and Flatt,P.R.
Inhibition of dipeptidyl peptidase-IV activity by metformin enhances the antidiabetic effects of glucagon-like peptide-1
Eur J Pharmacol (27-7-2006) 547, 192-199. PubMed Europe PubMed DOI I
[YEAR:7-9-2006]Guieu,R., Fenouillet,E., Devaux,C., Fajloun,Z., Carrega,L., Sabatier,J.M., Sauze,N. and Marguet,D.
CD26 modulates nociception in mice via its dipeptidyl-peptidase IV activity
Behav Brain Res (7-9-2006) 166, 230-235. PubMed Europe PubMed DOI
[YEAR:3-3-2006]Ho,N.H., Weissleder,R. and Tung,C.H.
Development of a dual fluorogenic and chromogenic dipeptidyl peptidase IV substrate
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[YEAR:14-1-2006]Holst,J.J.
Glucagon-like peptide-1: from extract to agent. The Claude Bernard Lecture, 2005
Diabetologia (14-1-2006) 49, 253-260. PubMed Europe PubMed DOI V I
[YEAR:1-1-2006]Kim,Y.B., Kopcho,L.M., Kirby,M.S., Hamann,L.G., Weigelt,C.A., Metzler,W.J. and Marcinkeviciene,J.
Mechanism of Gly-Pro-pNA cleavage catalyzed by dipeptidyl peptidase-IV and its inhibition by saxagliptin (BMS-477118)
Arch Biochem Biophys (1-1-2006) 445, 9-18. PubMed Europe PubMed DOI I
[YEAR:27-9-2006]Kurukulasuriya,R., Rohde,J.J., Szczepankiewicz,B.G., Basha,F., Lai,C., Jae,H.S., Winn,M., Stewart,K.D., Longenecker,K.L., Lubben,T.W., Ballaron,S.J., Sham,H.L. and von Geldern,T.W.
Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (27-9-2006) 16, 6226-6230. PubMed Europe PubMed DOI I
[YEAR:20-6-2006]Longenecker,K.L., Stewart,K.D., Madar,D.J., Jakob,C.G., Fry,E.H., Wilk,S., Lin,C.W., Ballaron,S.J., Stashko,M.A., Lubben,T.H., Yong,H., Pireh,D., Pei,Z., Basha,F., Wiedeman,P.E., von Geldern,T.W., Trevillyan,J.M. and Stoll,V.S.
Crystal structures of DPP-IV (CD26) from rat kidney exhibit flexible accommodation of peptidase-selective inhibitors
Biochemistry (20-6-2006) 45, 7474-7482. PubMed Europe PubMed DOI S I
[YEAR:19-10-2006]Madar,D.J., Kopecka,H., Pireh,D., Yong,H., Pei,Z., Li,X., Wiedeman,P.E., Djuric,S.W., von Geldern,T.W., Fickes,M.G., Bhagavatula,L., McDermott,T., Wittenberger,S., Richards,S.J., Longenecker,K.L., Stewart,K.D., Lubben,T.H., Ballaron,S.J., Stashko,M.A., Long,M.A., Wells,H., Zinker,B.A., Mika,A.K., Beno,D.W., Kempf-Grote,A.J., Polakowski,J., Segreti,J., Reinhart,G.A., Fryer,R.M., Sham,H.L. and Trevillyan,J.M.
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes
J Med Chem (19-10-2006) 49, 6416-6420. PubMed Europe PubMed DOI I
[YEAR:19-12-2006]Magnin,D.R., Taunk,P.C., Robertson,J.G., Wang,A., Marcinkeviciene,J., Kirby,M.S. and Hamann,L.G.
Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1
Bioorg Med Chem Lett (19-12-2006) 16, 1731-1734. PubMed Europe PubMed DOI I
Masur,K., Schwartz,F., Entschladen,F., Niggemann,B. and Zaenker,K.S.
DPPIV inhibitors extend GLP-2 mediated tumour promoting effects on intestinal cancer cells
Regul Pept (2006) 137, 147-155. PubMed Europe PubMed DOI I
Mu,J., Woods,J., Zhou,Y.P., Roy,R.S., Li,Z., Zycband,E., Feng,Y., Zhu,L., Li,C., Howard,A.D., Moller,D.E., Thornberry,N.A. and Zhang,B.B.
Chronic inhibition of dipeptidyl peptidase-4 with a sitagliptin analog preserves pancreatic beta-cell mass and function in a rodent model of type 2 diabetes
Diabetes (2006) 55, 1695-1704. PubMed Europe PubMed DOI I
Nordhoff,S., Cerezo-Galvez,S., Feurer,A., Hill,O., Matassa,V.G., Metz,G., Rummey,C., Thiemann,M. and Edwards,P.J.
The reversed binding of beta-phenethylamine inhibitors of DPP-IV: X-ray structures and properties of novel fragment and elaborated inhibitors
Bioorg Med Chem Lett (2006) 16, 1744-1748. PubMed Europe PubMed DOI S I
[YEAR:6-6-2006]Ogawa,Y., Mamura,Y., Murayama,N. and Yanoshita,R.
Characterization and cDNA cloning of dipeptidyl peptidase IV from the venom of Gloydius blomhoffi brevicaudus
Comp Biochem Physiol B Biochem Mol Biol (6-6-2006) 145, 35-42. PubMed Europe PubMed DOI
[YEAR:2-11-2006]Pei,Z., Li,X., von Geldern,T.W., Madar,D.J., Longenecker,K., Yong,H., Lubben,T.H., Stewart,K.D., Zinker,B.A., Backes,B.J., Judd,A.S., Mulhern,M., Ballaron,S.J., Stashko,M.A., Mika,A.K., Beno,D.W., Reinhart,G.A., Fryer,R.M., Preusser,L.C., Kempf-Grote,A.J., Sham,H.L. and Trevillyan,J.M.
Discovery of ((4R,5S)-5-Amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
J Med Chem (2-11-2006) 49, 6439-6442. PubMed Europe PubMed DOI I
[YEAR:15-6-2006]Pei,Z., Li,X., Longenecker,K., von Geldern,T.W., Wiedeman,P.E., Lubben,T.H., Zinker,B.A., Stewart,K., Ballaron,S.J., Stashko,M.A., Mika,A.K., Beno,D.W., Long,M., Wells,H., Kempf-Grote,A.J., Madar,D.J., McDermott,T.S., Bhagavatula,L., Fickes,M.G., Pireh,D., Solomon,L.R., Lake,M.R., Edalji,R., Fry,E.H., Sham,H.L. and Trevillyan,J.M.
Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors
J Med Chem (15-6-2006) 49, 3520-3535. PubMed Europe PubMed DOI I
[YEAR:24-8-2006]Pei,Z., Li,X., Longenecker,K., von Geldern,T.W., Wiedeman,P.E., Lubben,T.H., Zinker,B.A., Stewart,K., Ballaron,S.J., Stashko,M.A., Mika,A.K., Beno,D.W., Long,M., Wells,H., Kempf-Grote,A.J., Madar,D.J., McDermott,T.S., Bhagavatula,L., Fickes,M.G., Pireh,D., Solomon,L.R., Lake,M.R., Edalji,R., Fry,E.H., Sham,H.L. and Trevillyan,J.M.
Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors
J Med Chem (24-8-2006) 49, 5387-5387. PubMed Europe PubMed DOI I
[YEAR:14-10-2006]Qiao,L., Baumann,C.A., Crysler,C.S., Ninan,N.S., Abad,M.C., Spurlino,J.C., DesJarlais,R.L., Kervinen,J., Neeper,M.P., Bayoumy,S.S., Williams,R., Deckman,I.C., Dasgupta,M., Reed,R.L., Huebert,N.D., Tomczuk,B.E. and Moriarty,K.J.
Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (14-10-2006) 16, 123-128. PubMed Europe PubMed DOI I
Rosenstock,J., Brazg,R., Andryuk,P.J., Lu,K. and Stein,P.
Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin added to ongoing pioglitazone therapy in patients with type 2 diabetes: a 24-week, multicenter, randomized, double-blind, placebo-controlled, parallel-group study
Clin Ther (2006) 28, 1556-1568. PubMed Europe PubMed DOI I
[YEAR:3-2-2006]Sakashita,H., Akahoshi,F., Kitajima,H., Tsutsumiuchi,R. and Hayashi,Y.
[(S)-gamma-(Arylamino)prolyl]thiazolidine compounds as a novel series of potent and stable DPP-IV inhibitors
Bioorg Med Chem (3-2-2006) 14, 3662-3671. PubMed Europe PubMed DOI I
Schlesselman,L.S.
Vildagliptin: A dipeptidyl peptidase-IV inhibitor for the treatment of type 2 diabetes
Formulary (2006) 41, 494-500. I
[YEAR:31-3-2006]Tsai,T.Y., Coumar,M.S., Hsu,T., Hsieh,H.P., Chien,C.H., Chen,C.T., Chang,C.N., Lo,Y.K., Wu,S.H., Huang,C.Y., Huang,Y.W., Wang,M.H., Wu,H.Y., Lee,H.J., Chen,X., Chao,Y.S. and Jiaang,W.T.
Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (31-3-2006) 16, 3268-3272. PubMed Europe PubMed DOI I
[YEAR:12-1-2006]Tsu,H., Chen,X., Chen,C.T., Lee,S.J., Chang,C.N., Kao,K.H., Coumar,M.S., Yeh,Y.T., Chien,C.H., Wang,H.S., Lin,K.T., Chang,Y.Y., Wu,S.H., Chen,Y.S., Lu,I.L., Wu,S.Y., Tsai,T.Y., Chen,W.C., Hsieh,H.P., Chao,Y.S. and Jiaang,W.T.
2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl ]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV
J Med Chem (12-1-2006) 49, 373-380. PubMed Europe PubMed DOI I
[YEAR:1-6-2006]Wright,S.W., Ammirati,M.J., Andrews,K.M., Brodeur,A.M., Danley,D.E., Doran,S.D., Lillquist,J.S., McClure,L.D., McPherson,R.K., Orena,S.J., Parker,J.C., Polivkova,J., Qiu,X., Soeller,W.C., Soglia,C.B., Treadway,J.L., VanVolkenburg,M.A., Wang,H., Wilder,D.C. and Olson,T.V.
cis-2,5-Dicyanopyrrolidine inhibitors of dipeptidyl peptidase IV: synthesis and in vitro, in vivo, and X-ray crystallographic characterization
J Med Chem (1-6-2006) 49, 3068-3076. PubMed Europe PubMed DOI S I
[YEAR:2-12-2006]Xu,J., Wei,L., Mathvink,R., Edmondson,S.D., Mastracchio,A., Eiermann,G.J., He,H., Leone,J.F., Leiting,B., Lyons,K.A., Marsilio,F., Patel,R.A., Petrov,A., Wu,J.K., Thornberry,N.A. and Weber,A.E.
Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors
Bioorg Med Chem Lett (2-12-2006) 16, 1346-1349. PubMed Europe PubMed DOI I
[YEAR:16-8-2006]Xu,J., Wei,L., Mathvink,R.J., Edmondson,S.D., Eiermann,G.J., He,H., Leone,J.F., Leiting,B., Lyons,K.A., Marsilio,F., Patel,R.A., Patel,S.B., Petrov,A., Scapin,G., Wu,J.K., Thornberry,N.A. and Weber,A.E.
Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (16-8-2006) 16, 5373-5377. PubMed Europe PubMed DOI I
[YEAR:15-9-2006]Yamazaki,K., Yasuda,N., Inoue,T., Nagakura,T., Kira,K., Shinoda,M., Saeki,T. and Tanaka,I.
7-But-2-ynyl-9-(6-methoxy-pyridin-3-yl)-6-piperazin-1-yl-7,9-dihydro-purin -8-one is a novel competitive and selective inhibitor of dipeptidyl peptidase IV with an antihyperglycemic activity
J Pharmacol Exp Ther (15-9-2006) 319, 1253-1257. PubMed Europe PubMed DOI I
[YEAR:16-8-2006]Yasuda,N., Nagakura,T., Inoue,T., Yamazaki,K., Katsutani,N., Takenaka,O., Clark,R., Matsuura,F., Emori,E., Yoshikawa,S., Kira,K., Ikuta,H., Okada,T., Saeki,T., Asano,O. and Tanaka,I.
E3024, 3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyrida zin-4-one tosylate, is a novel, selective and competitive dipeptidyl peptidase-IV inhibitor
Eur J Pharmacol (16-8-2006) 548, 181-187. PubMed Europe PubMed DOI I
Zhai,W., Cardell,M., De Meester,I., Augustyns,K., Hillinger,S., Inci,I., Arni,S., Jungraithmayr,W., Scharpe,S., Weder,W. and Korom,S.
Ischemia/reperfusion injury: the role of CD26/dipeptidyl-peptidase-IV-inhibition in lung transplantation
Transplant Proc (2006) 38, 3369-3371. PubMed Europe PubMed DOI I

2005

[YEAR:1-2-2005]Abe,M., Akiyama,T., Umezawa,Y., Yamamoto,K., Nagai,M., Yamazaki,H., Ichikawa,Y. and Muraoka,Y.
Synthesis and biological activity of sulphostin analogues, novel dipeptidyl peptidase IV inhibitors
Bioorg Med Chem (1-2-2005) 13, 785-797. PubMed Europe PubMed DOI I
[YEAR:1-3-2005]Ahn,J.H., Kim,J.A., Kim,H.M., Kwon,H.M., Huh,S.C., Rhee,S.D., Kim,K.R., Yang,S.D., Park,S.D., Lee,J.M., Kim,S.S. and Cheon,H.G.
Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors
Bioorg Med Chem Lett (1-3-2005) 15, 1337-1340. PubMed Europe PubMed DOI I
Ahn,J.H., Jung,S.H., Kim,J.A., Song,S.B., Kwon,S.J., Kim,K.R., Rhee,S.D., Park,S.D., Lee,J.M., Kim,S.S. and Cheon,H.G.
Pyrazolidine derivatives with heteroaryl urea as dipeptidyl peptidase IV inhibitors
Chem Pharm Bull (Tokyo) (2005) 53, 1048-1050. PubMed Europe PubMed DOI I
Ahren,B., Pacini,G., Foley,J.E. and Schweizer,A.
Improved meal-related beta-cell function and insulin sensitivity by the dipeptidyl peptidase-IV inhibitor vildagliptin in metformin-treated patients with type 2 diabetes over 1year
Diabetes Care (2005) 28, 1936-1940. PubMed Europe PubMed DOI I
[YEAR:2-5-2005]Ashton,W.T., Sisco,R.M., Dong,H., Lyons,K.A., He,H., Doss,G.A., Leiting,B., Patel,R.A., Wu,J.K., Marsilio,F., Thornberry,N.A. and Weber,A.E.
Dipeptidyl peptidase IV inhibitors derived from beta-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole
Bioorg Med Chem Lett (2-5-2005) 15, 2253-2258. PubMed Europe PubMed DOI I
[YEAR:28-7-2005]Augeri,D.J., Robl,J.A., Betebenner,D.A., Magnin,D.R., Khanna,A., Robertson,J.G., Wang,A., Simpkins,L.M., Taunk,P., Huang,Q., Han,S.P., Abboa-Offei,B., Cap,M., Xin,L., Tao,L., Tozzo,E., Welzel,G.E., Egan,D.M., Marcinkeviciene,J., Chang,S.Y., Biller,S.A., Kirby,M.S., Parker,R.A. and Hamann,L.G.
Discovery and preclinical profile of saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
J Med Chem (28-7-2005) 48, 5025-5037. PubMed Europe PubMed DOI I
Augustyns,K., Van der Veken,P., Senten,K. and Haemers,A.
The therapeutic potential of inhibitors of dipeptidyl peptidase IV (DPP IV) and related proline-specific dipeptidyl aminopeptidases
Curr Med Chem (2005) 12, 971-998. PubMed Europe PubMed DOI I
[YEAR:1-7-2005]Brandt,I., Joossens,J., Chen,X., Maes,M.B., Scharpe,S., De Meester,I. and Lambeir,A.M.
Inhibition of dipeptidyl-peptidase IV catalyzed peptide truncation by Vildagliptin ((2S)-{[(3-hydroxyadamantan-1-yl)amino]acetyl}-pyrrolidine-2-carbonitrile)
Biochem Pharmacol (1-7-2005) 70, 134-143. PubMed Europe PubMed DOI I
[YEAR:18-7-2005]Burkey,B.F., Li,X., Bolognese,L., Balkan,B., Mone,M., Russell,M., Hughes,T.E. and Wang,P.R.
Acute and chronic effects of the incretin enhancer vildagliptin in insulin-resistant rats
J Pharmacol Exp Ther (18-7-2005) 315, 688-695. PubMed Europe PubMed DOI I
Deacon,C.F.
MK-431 (Merck)
Curr Opin Investig Drugs (2005) 6, 419-426. PubMed Europe PubMed I
Demuth,H.U., McIntosh,C.H. and Pederson,R.A.
Type 2 diabetes - therapy with dipeptidyl peptidase IV inhibitors
Biochim Biophys Acta Proteins Proteom (2005) 1751, 33-44. PubMed Europe PubMed DOI I
[YEAR:15-6-2005]Edmondson,S.D., Mastracchio,A., Duffy,J.L., Eiermann,G.J., He,H., Ita,I., Leiting,B., Leone,J.F., Lyons,K.A., Makarewicz,A.M., Patel,R.A., Petrov,A., Wu,J.K., Thornberry,N.A. and Weber,A.E.
Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (15-6-2005) 15, 3048-3052. PubMed Europe PubMed DOI I
[YEAR:7-3-2005]Geier,M.S., Tenikoff,D., Yazbeck,R., McCaughan,G.W., Abbott,C.A. and Howarth,G.S.
Development and resolution of experimental colitis in mice with targeted deletion of dipeptidyl peptidase IV
J Cell Physiol (7-3-2005) 204, 687-692. PubMed Europe PubMed DOI
[YEAR:8-12-2005]Gorrell,M.D.
Dipeptidyl peptidase IV and related enzymes in cell biology and liver disorders
Clin Sci (Lond) (8-12-2005) 108, 277-292. PubMed Europe PubMed DOI V
Herman,G.A., Stevens,C., Van Dyck,K., Bergman,A., Yi,B., De Smet,M., Snyder,K., Hilliard,D., Tanen,M., Tanaka,W., Wang,A.Q., Zeng,W., Musson,D., Winchell,G., Davies,M.J., Ramael,S., Gottesdiener,K.M. and Wagner,J.A.
Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses
Clin Pharmacol Ther (2005) 78, 675-688. PubMed Europe PubMed DOI I
[YEAR:25-6-2005]Hsiung,H.M., Smiley,D.L., Zhang,X.Y., Zhang,L., Yan,L.Z., Craft,L., Heiman,M.L. and Smith,D.P.
Potent peptide agonists for human melanocortin 3 and 4 receptors derived from enzymatic cleavages of human beta-MSH(5-22) by dipeptidyl peptidase I and dipeptidyl peptidase IV
Peptides (25-6-2005) 26, 1988-1996. PubMed Europe PubMed DOI
Hu,Y., Ma,L., Wu,M., Wong,M.S., Li,B., Corral,S., Yu,Z., Nomanbhoy,T., Alemayehu,S., Fuller,S.R., Rosenblum,J.S., Rozenkrants,N., Minimo,L.C., Ripka,W.C., Szardenings,A.K., Kozarich,J.W. and Shreder,K.R.
Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7
Bioorg Med Chem Lett (2005) 15, 4239-4242. PubMed Europe PubMed DOI I
[YEAR:19-8-2005]Hulin,B., Cabral,S., Lopaze,M.G., Van Volkenburg,M.A., Andrews,K.M. and Parker,J.C.
New fluorinated pyrrolidine and azetidine amides as dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (19-8-2005) 15, 4770-4773. PubMed Europe PubMed DOI I
Hunziker,D., Hennig,M. and Peters,J.U.
Inhibitors of dipeptidyl peptidase IV - recent advances and structural views
Curr Top Med Chem (2005) 5, 1623-1637. PubMed Europe PubMed DOI V I
[YEAR:28-1-2005]Islam,M.S., Rahman,S.A., Mirzaei,Z. and Islam,K.B.
Engineered beta-cells secreting dipeptidyl peptidase IV-resistant glucagon-like peptide-1 show enhanced glucose-responsiveness
Life Sci (28-1-2005) 76, 1239-1248. PubMed Europe PubMed DOI
Kikkawa,F., Kajiyama,H., Shibata,K., Ino,K., Nomura,S. and Mizutani,S.
Dipeptidyl peptidase IV in tumor progression
Biochim Biophys Acta Proteins Proteom (2005) 1751, 45-51. PubMed Europe PubMed DOI
[YEAR:13-1-2005]Kim,D., Wang,L., Beconi,M., Eiermann,G.J., Fisher,M.H., He,H., Hickey,G.J., Kowalchick,J.E., Leiting,B., Lyons,K., Marsilio,F., McCann,M.E., Patel,R.A., Petrov,A., Scapin,G., Patel,S.B., Roy,R.S., Wu,J.K., Wyvratt,M.J., Zhang,B.B., Zhu,L., Thornberry,N.A. and Weber,A.E.
(2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin -7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
J Med Chem (13-1-2005) 48, 141-151. PubMed Europe PubMed DOI I
[YEAR:25-7-2005]Kim,K.R., Rhee,S.D., Kim,H.Y., Jung,W.H., Yang,S.D., Kim,S.S., Ahn,J.H. and Cheon,H.G.
KR-62436, 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile, is a novel dipeptidyl peptidase-IV (DPP-IV) inhibitor with anti-hyperglycemic activity
Eur J Pharmacol (25-7-2005) 518, 63-70. PubMed Europe PubMed DOI I
[YEAR:15-4-2005]Kopcho,L.M., Kim,Y.B., Wang,A., Liu,M.A., Kirby,M.S. and Marcinkeviciene,J.
Probing prime substrate binding sites of human dipeptidyl peptidase-IV using competitive substrate approach
Arch Biochem Biophys (15-4-2005) 436, 367-376. PubMed Europe PubMed DOI P
Lankas,G.R., Leiting,B., Roy,R.S., Eiermann,G.J., Beconi,M.G., Biftu,T., Chan,C.C., Edmondson,S., Feeney,W.P., He,H., Ippolito,D.E., Kim,D., Lyons,K.A., Ok,H.O., Patel,R.A., Petrov,A.N., Pryor,K.A., Qian,X., Reigle,L., Woods,A., Wu,J.K., Zaller,D., Zhang,X., Zhu,L., Weber,A.E. and Thornberry,N.A.
Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9
Diabetes (2005) 54, 2988-2994. PubMed Europe PubMed DOI I
[YEAR:27-5-2005]Lautar,S.L., Rojas,C., Slusher,B.S., Wozniak,K.M., Wu,Y., Thomas,A.G., Waldon,D., Li,W., Ferraris,D. and Belyakov,S.
DPP IV inhibitor blocks mescaline-induced scratching and amphetamine-induced hyperactivity in mice
Brain Res (27-5-2005) 1048, 177-184. PubMed Europe PubMed DOI I
Lindsay,J.R., Duffy,N.A., McKillop,A.M., Ardill,J., O'Harte,F.P., Flatt,P.R. and Bell,P.M.
Inhibition of dipeptidyl peptidase IV activity by oral metformin in Type 2 diabetes
Diabet Med (2005) 22, 654-657. PubMed Europe PubMed DOI
[YEAR:1-7-2005]Lu,I.L., Lee,S.J., Tsu,H., Wu,S.Y., Kao,K.H., Chien,C.H., Chang,Y.Y., Chen,Y.S., Cheng,J.H., Chang,C.N., Chen,T.W., Chang,S.P., Chen,X. and Jiaang,W.T.
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors
Bioorg Med Chem Lett (1-7-2005) 15, 3271-3275. PubMed Europe PubMed DOI I
[YEAR:10-5-2005]Mari,A., Sallas,W.M., He,Y.L., Watson,C., Ligueros-Saylan,M., Dunning,B.E., Deacon,C.F., Holst,J.J. and Foley,J.E.
Vildagliptin, a dipeptidyl peptidase-IV inhibitor, improves model-assessed beta-cell function in patients with type 2 diabetes
J Clin Endocrinol Metab (10-5-2005) 90, 4888-4894. PubMed Europe PubMed DOI I
[YEAR:16-3-2005]Mest,H.J. and Mentlein,R.
Dipeptidyl peptidase inhibitors as new drugs for the treatment of type 2 diabetes
Diabetologia (16-3-2005) 48, 616-620. PubMed Europe PubMed DOI
Monod,M., Lechenne,B., Jousson,O., Grand,D., Zaugg,C., Stocklin,R. and Grouzmann,E.
Aminopeptidases and dipeptidyl-peptidases secreted by the dermatophyte Trichophyton rubrum
Microbiology (Reading) (2005) 151, 145-155. PubMed Europe PubMed DOI
Nauck,M.A. and El-Ouaghlidi,A.
The therapeutic actions of DPP-IV inhibition are not mediated by glucagon-like peptide-1
Diabetologia (2005) 48, 608-611. PubMed Europe PubMed DOI
[YEAR:15-5-2005]Nielsen,L.L.
Incretin mimetics and DPP-IV inhibitors for the treatment of type 2 diabetes
Drug Discov Today (15-5-2005) 10, 703-710. PubMed Europe PubMed DOI I
[YEAR:16-7-2005]Plamboeck,A., Holst,J.J., Carr,R.D. and Deacon,C.F.
Neutral endopeptidase 24.11 and dipeptidyl peptidase IV are both mediators of the degradation of glucagon-like peptide 1 in the anaesthetised pig
Diabetologia (16-7-2005) 48, 1882-1890. PubMed Europe PubMed DOI
Rigolet,P., Xi,X.G., Rety,S. and Chich,J.F.
The structural comparison of the bacterial PepX and human DPP-IV reveals sites for the design of inhibitors of PepX activity
FEBS J (2005) 272, 2050-2059. PubMed Europe PubMed DOI
Ristic,S., Byiers,S., Foley,J. and Holmes,D.
Improved glycaemic control with dipeptidyl peptidase-4 inhibition in patients with type 2 diabetes: vildagliptin (LAF237) dose response
Diabetes Obes Metab (2005) 7, 692-698. PubMed Europe PubMed DOI I
Sorbera,L.A. and Castaner,J.
MK-0431 - agent for type 2 diabetes dipeptidyl-peptidase IV (CD26) inhibitor
Drugs Future (2005) 30, 337-343. I
Wargent,E., Stocker,C., Augstein,P., Heinke,P., Meyer,A., Hoffmann,T., Subramanian,A., Sennitt,M.V., Demuth,H.U., Arch,J.R. and Cawthorne,M.A.
Improvement of glucose tolerance in Zucker diabetic fatty rats by long-term treatment with the dipeptidyl peptidase inhibitor P32/98: comparison with and combination with rosiglitazone
Diabetes Obes Metab (2005) 7, 170-181. PubMed Europe PubMed DOI I
[YEAR:28-1-2005]Weihofen,W.A., Liu,J., Reutter,W., Saenger,W. and Fan,H.
Crystal structures of HIV-1 Tat-derived nonapeptides Tat-(1-9) and Trp2-Tat-(1-9) bound to the active site of dipeptidyl-peptidase IV (CD26)
J Biol Chem (28-1-2005) 280, 14911-14917. PubMed Europe PubMed DOI S
[YEAR:16-5-2005]Xu,J., Wei,L., Mathvink,R., He,J., Park,Y.J., He,H., Leiting,B., Lyons,K.A., Marsilio,F., Patel,R.A., Wu,J.K., Thornberry,N.A. and Weber,A.E.
Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (16-5-2005) 15, 2533-2536. PubMed Europe PubMed DOI I
[YEAR:14-10-2005]Xu,S., Zhu,B., Teffera,Y., Pan,D.E., Caldwell,C.G., Doss,G., Stearns,R.A., Evans,D.C. and Beconi,M.G.
Metabolic activation of fluoropyrrolidine dipeptidyl peptidase-IV inhibitors by rat liver microsomes
Drug Metab Dispos (14-10-2005) 33, 121-130. PubMed Europe PubMed DOI I
[YEAR:18-7-2005]Zhao,G., Taunk,P.C., Magnin,D.R., Simpkins,L.M., Robl,J.A., Wang,A., Robertson,J.G., Marcinkeviciene,J., Sitkoff,D.F., Parker,R.A., Kirby,M.S. and Hamann,L.G.
Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (18-7-2005) 15, 3992-3995. PubMed Europe PubMed DOI I

2004

Abe,M., Akiyama,T., Nakamura,H., Kojima,F., Harada,S. and Muraoka,Y.
First synthesis and determination of the absolute configuration of sulphostin, a novel inhibitor of dipeptidyl peptidase IV
J Nat Prod (2004) 67, 999-1004. PubMed Europe PubMed DOI I
[YEAR:1-8-2004]Adams,S., Miller,G.T., Jesson,M.I., Watanabe,T., Jones,B. and Wallner,B.P.
PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism
Cancer Res (1-8-2004) 64, 5471-5480. PubMed Europe PubMed DOI I
Aertgeerts,K., Ye,S., Tennant,M.G., Kraus,M.L., Rogers,J., Sang,B.C., Skene,R.J., Webb,D.R. and Prasad,G.S.
Crystal structure of human dipeptidyl peptidase IV in complex with a decapeptide reveals details on substrate specificity and tetrahedral intermediate formation
Protein Sci (2004) 13, 412-421. PubMed Europe PubMed DOI PMC EPMC S
Aertgeerts,K., Ye,S., Shi,L., Prasad,S.G., Witmer,D., Chi,E., Sang,B.C., Wijnands,R.A., Webb,D.R. and Swanson,R.V.
N-linked glycosylation of dipeptidyl peptidase IV (CD26): effects on enzyme activity, homodimer formation, and adenosine deaminase binding
Protein Sci (2004) 13, 145-154. PubMed Europe PubMed DOI PMC EPMC
[YEAR:6-9-2004]Ahn,J.H., Kim,H.M., Jung,S.H., Kang,S.K., Kim,K.R., Rhee,S.D., Yang,S.D., Cheon,H.G. and Kim,S.S.
Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents
Bioorg Med Chem Lett (6-9-2004) 14, 4461-4465. PubMed Europe PubMed DOI
Ahren,B. and Schmitz,O.
GLP-1 receptor agonists and DPP-4 inhibitors in the treatment of type 2 diabetes
Horm Metab Res (2004) 36, 867-876. PubMed Europe PubMed DOI V
Ahren,B., Gomis,R., Standl,E., Mills,D. and Schweizer,A.
Twelve- and 52-week efficacy of the dipeptidyl peptidase IV inhibitor LAF237 in metformin-treated patients with type 2 diabetes
Diabetes Care (2004) 27, 2874-2880. PubMed Europe PubMed DOI I
Ahren,B., Landin-Olsson,M., Jansson,P.A., Svensson,M., Holmes,D. and Schweizer,A.
Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes
J Clin Endocrinol Metab (2004) 89, 2078-2084. PubMed Europe PubMed DOI I
Aytac,U. and Dang,N.H.
CD26/dipeptidyl peptidase IV: a regulator of immune function and a potential molecular target for therapy
Curr Drug Targets Immune Endocr Metabol Disord (2004) 4, 11-18. PubMed Europe PubMed DOI
[YEAR:2-6-2004]Bjelke,J.R., Christensen,J., Branner,S., Wagtmann,N., Olsen,C., Kanstrup,A.B. and Rasmussen,H.B.
Tyrosine 547 constitutes an essential part of the catalytic mechanism of dipeptidyl peptidase IV
J Biol Chem (2-6-2004) 279, 34691-34697. PubMed Europe PubMed DOI I
[YEAR:20-9-2004]Brockunier,L.L., He,J., Colwell,L.F., Jr., Habulihaz,B., He,H., Leiting,B., Lyons,K.A., Marsilio,F., Patel,R.A., Teffera,Y., Wu,J.K., Thornberry,N.A., Weber,A.E. and Parmee,E.R.
Substituted piperazines as novel dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (20-9-2004) 14, 4763-4766. PubMed Europe PubMed DOI I
[YEAR:17-5-2004]Cheon,H.G., Lee,C.M., Kim,B.T. and Hwang,K.J.
Lead discovery of quinoxalinediones as an inhibitor of dipeptidyl peptidase-IV (DPP-IV) by high-throughput screening
Bioorg Med Chem Lett (17-5-2004) 14, 2661-2664. PubMed Europe PubMed DOI I
Chien,C.H., Huang,L.H., Chou,C.Y., Chen,Y.S., Han,Y.S., Chang,G.G., Liang,P.H. and Chen,X.
One site mutation disrupts dimer formation in human DPP-IV proteins
J Biol Chem (2004) 279, 52338-52345. PubMed Europe PubMed DOI
Deacon,C.F., Ahren,B. and Holst,J.J.
Inhibitors of dipeptidyl peptidase IV: a novel approach for the prevention and treatment of Type 2 diabetes?
Expert Opin Investig Drugs (2004) 13, 1091-1102. PubMed Europe PubMed DOI I
Dikov,A., Dimitrova,M., Krieg,R. and Halbhuber,K.J.
New fluorescent method for the histochemical detection of dipeptidyl peptidase IV using glycyl-L-prolyl-2-anthraquinonyl hydrazide as substrate
Cell Mol Biol (Noisy-le-grand) (2004) 50, OL553-OL558. PubMed Europe PubMed
[YEAR:18-10-2004]Edmondson,S.D., Mastracchio,A., Beconi,M., Colwell,L.F., Jr., Habulihaz,B., He,H., Kumar,S., Leiting,B., Lyons,K.A., Mao,A., Marsilio,F., Patel,R.A., Wu,J.K., Zhu,L., Thornberry,N.A., Weber,A.E. and Parmee,E.R.
Potent and selective proline derived dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (18-10-2004) 14, 5151-5155. PubMed Europe PubMed DOI I
[YEAR:15-11-2004]Ferraris,D., Ko,Y.S., Calvin,D., Chiou,T., Lautar,S., Thomas,B., Wozniak,K., Rojas,C., Kalish,V. and Belyakov,S.
Ketopyrrolidines and ketoazetidines as potent dipeptidyl peptidase IV (DPP IV) inhibitors
Bioorg Med Chem Lett (15-11-2004) 14, 5579-5583. PubMed Europe PubMed DOI I
[YEAR:1-12-2004]Fukushima,H., Hiratate,A., Takahashi,M., Saito,M., Munetomo,E., Kitano,K., Saito,H., Takaoka,Y. and Yamamoto,K.
Synthesis and structure-activity relationships of potent 3- or 4-substituted-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors
Bioorg Med Chem (1-12-2004) 12, 6053-6061. PubMed Europe PubMed DOI I
[YEAR:22-6-2004]Girardi,A.C., Knauf,F., Demuth,H.U. and Aronson,P.S.
Role of dipeptidyl peptidase IV in regulating activity of Na+/H+ exchanger isoform NHE3 in proximal tubule cells
Am J Physiol Cell Physiol (22-6-2004) 287, C1238-C1245. PubMed Europe PubMed DOI I
Hiramatsu,H., Yamamoto,A., Kyono,K., Higashiyama,Y., Fukushima,C., Shima,H., Sugiyama,S., Inaka,K. and Shimizu,R.
The crystal structure of human dipeptidyl peptidase IV (DPPIV) complex with diprotin A
Biol Chem (2004) 385, 561-564. PubMed Europe PubMed DOI S
[YEAR:9-1-2004]Ludwig,K., Fan,H., Dobers,J., Berger,M., Reutter,W. and Bottcher,C.
3D structure of the CD26-ADA complex obtained by cryo-EM and single particle analysis
Biochem Biophys Res Commun (9-1-2004) 313, 223-229. PubMed Europe PubMed DOI S
[YEAR:6-5-2004]Magnin,D.R., Robl,J.A., Sulsky,R.B., Augeri,D.J., Huang,Y., Simpkins,L.M., Taunk,P.C., Betebenner,D.A., Robertson,J.G., Abboa-Offei,B.E., Wang,A., Cap,M., Xin,L., Tao,L., Sitkoff,D.F., Malley,M.F., Gougoutas,J.Z., Khanna,A., Huang,Q., Han,S.P., Parker,R.A. and Hamann,L.G.
Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of alpha-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors
J Med Chem (6-5-2004) 47, 2587-2598. PubMed Europe PubMed DOI I
McIntyre,J.A. and Castaner,J.
Vildagliptin. Agent for type 2 diabetes, dipeptidyl-peptidase IV inhibitor
Drugs Future (2004) 29, 887-891. I
McIntyre,J.A. and Castaner,J.
Talabostat. Oncolytic, hematopoietic agent, dipeptidyl-peptidase IV (CD26) inhibitor, fibroblast activation protein inhibitor
Drugs Future (2004) 29, 882-886. I
Misumi,Y. and Ikehara,Y.
Dipeptidyl-peptidase IV
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[YEAR:5-1-2004]Parmee,E.R., He,J., Mastracchio,A., Edmondson,S.D., Colwell,L., Eiermann,G., Feeney,W.P., Habulihaz,B., He,H., Kilburn,R., Leiting,B., Lyons,K., Marsilio,F., Patel,R.A., Petrov,A., Di Salvo,J., Wu,J.K., Thornberry,N.A. and Weber,A.E.
4-amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (5-1-2004) 14, 43-46. PubMed Europe PubMed DOI I
[YEAR:22-3-2004]Peters,J.U., Weber,S., Kritter,S., Weiss,P., Wallier,A., Boehringer,M., Hennig,M., Kuhn,B. and Loeffler,B.M.
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents
Bioorg Med Chem Lett (22-3-2004) 14, 1491-1493. PubMed Europe PubMed DOI I
Pro,B. and Dang,N.H.
CD26/dipeptidyl peptidase IV and its role in cancer
Histol Histopathol (2004) 19, 1345-1351. PubMed Europe PubMed
[YEAR:23-2-2004]Takasaki,K., Iwase,M., Nakajima,T., Ueno,K., Nomoto,Y., Nakanishi,S. and Higo,K.
K579, a slow-binding inhibitor of dipeptidyl peptidase IV, is a long-acting hypoglycemic agent
Eur J Pharmacol (23-2-2004) 486, 335-342. PubMed Europe PubMed DOI I
[YEAR:28-11-2004]Takasaki,K., Takada,H., Nakajima,T., Ueno,K., Ushiki,J. and Higo,K.
Involvement of the active metabolites in the inhibitory activity of K579 on rat plasma dipeptidyl peptidase IV
Eur J Pharmacol (28-11-2004) 505, 237-241. PubMed Europe PubMed DOI I
[YEAR:22-6-2004]Weihofen,W.A., Liu,J., Reutter,W., Saenger,W. and Fan,H.
Crystal structure of CD26/dipeptidyl-peptidase IV in complex with adenosine deaminase reveals a highly amphiphilic interface
J Biol Chem (22-6-2004) 279, 43330-43335. PubMed Europe PubMed DOI S
[YEAR:20-9-2004]Xu,J., Ok,H.O., Gonzalez,E.J., Colwell,L.F., Jr., Habulihaz,B., He,H., Leiting,B., Lyons,K.A., Marsilio,F., Patel,R.A., Wu,J.K., Thornberry,N.A., Weber,A.E. and Parmee,E.R.
Discovery of potent and selective beta-homophenylalanine based dipeptidyl peptidase IV inhibitors
Bioorg Med Chem Lett (20-9-2004) 14, 4759-4762. PubMed Europe PubMed DOI I

2003

Bar,J., Weber,A., Hoffmann,T., Stork,J., Wermann,M., Wagner,L., Aust,S., Gerhartz,B. and Demuth,H.U.
Characterisation of human dipeptidyl peptidase IV expressed in Pichia pastoris. A structural and mechanistic comparison between the recombinant human and the purified porcine enzyme
Biol Chem (2003) 384, 1553-1563. PubMed Europe PubMed DOI E
Beconi,M.G., Mao,A., Liu,D.Q., Kochansky,C., Pereira,T., Raab,C., Pearson,P. and Lee Chiu,S.H.
Metabolism and pharmacokinetics of a dipeptidyl peptidase IV inhibitor in rats, dogs, and monkeys with selective carbamoyl glucuronidation of the primary amine in dogs
Drug Metab Dispos (2003) 31, 1269-1277. PubMed Europe PubMed DOI I
Boonacker,E. and Van Noorden,C.J.
The multifunctional or moonlighting protein CD26/DPPIV
Eur J Cell Biol (2003) 82, 53-73. PubMed Europe PubMed DOI
[YEAR:15-6-2003]Christopherson,K.W., Cooper,S. and Broxmeyer,H.E.
Cell surface peptidase CD26/DPPIV mediates G-CSF mobilization of mouse progenitor cells
Blood (15-6-2003) 101, 4680-4686. PubMed Europe PubMed DOI
[YEAR:27-5-2003]Conarello,S.L., Li,Z., Ronan,J., Roy,R.S., Zhu,L., Jiang,G., Liu,F., Woods,J., Zycband,E., Moller,D.E., Thornberry,N.A. and Zhang,B.B.
Mice lacking dipeptidyl peptidase IV are protected against obesity and insulin resistance
Proc Natl Acad Sci U S A (27-5-2003) 100, 6825-6830. PubMed Europe PubMed DOI PMC EPMC K
[YEAR:29-4-2003]Engel,M., Hoffmann,T., Wagner,L., Wermann,M., Heiser,U., Kiefersauer,R., Huber,R., Bode,W., Demuth,H.U. and Brandstetter,H.
The crystal structure of dipeptidyl peptidase IV (CD26) reveals its functional regulation and enzymatic mechanism
Proc Natl Acad Sci U S A (29-4-2003) 100, 5063-5068. PubMed Europe PubMed DOI PMC EPMC S
[YEAR:30-5-2003]Gabrilovac,J., Abramic,M., Uzarevic,B., Andreis,A. and Poljak,L.
Dipeptidyl peptidase IV (DPPIV) enzyme activity on immature T-cell line R1.1 is down-regulated by dynorphin-A(1-17) as a non-substrate inhibitor
Life Sci (30-5-2003) 73, 151-166. PubMed Europe PubMed DOI I
[YEAR:21-3-2003]Hiramatsu,H., Kyono,K., Higashiyama,Y., Fukushima,C., Shima,H., Sugiyama,S., Inaka,K., Yamamoto,A. and Shimizu,R.
The structure and function of human dipeptidyl peptidase IV, possessing a unique eight-bladed beta-propeller fold
Biochem Biophys Res Commun (21-3-2003) 302, 849-854. PubMed Europe PubMed DOI S
[YEAR:1-5-2003]Kajiyama,H., Kikkawa,F., Khin,E., Shibata,K., Ino,K. and Mizutani,S.
Dipeptidyl peptidase IV overexpression induces up-regulation of E-cadherin and tissue inhibitors of matrix metalloproteinases, resulting in decreased invasive potential in ovarian carcinoma cells
Cancer Res (1-5-2003) 63, 2278-2283. PubMed Europe PubMed
[YEAR:15-9-2003]Karl,T., Chwalisz,W.T., Wedekind,D., Hedrich,H.J., Hoffmann,T., Jacobs,R., Pabst,R. and von Horsten,S.
Localization, transmission, spontaneous mutations, and variation of function of the Dpp4 (dipeptidyl-peptidase IV; CD26) gene in rats
Regul Pept (15-9-2003) 115, 81-90. PubMed Europe PubMed DOI
Karl,T., Hoffmann,T., Pabst,R. and von Horsten,S.
Extreme reduction of dipeptidyl peptidase IV activity in F344 rat substrains is associated with various behavioral differences
Physiol Behav (2003) 80, 123-134. PubMed Europe PubMed DOI M
Kholova,I., Ludvikova,M., Ryska,A., Topolcan,O., Pikner,R., Pecen,L., Cap,J. and Holubec,L., Jr.
Diagnostic role of markers dipeptidyl peptidase IV and thyroid peroxidase in thyroid tumors
Anticancer Res (2003) 23, 871-875. PubMed Europe PubMed
Lambeir,A.M., Durinx,C., Scharpe,S. and De Meester,I.
Dipeptidyl-peptidase IV from bench to bedside: an update on structural properties, functions, and clinical aspects of the enzyme DPP IV
Crit Rev Clin Lab Sci (2003) 40, 209-294. PubMed Europe PubMed DOI
[YEAR:15-4-2003]Leiting,B., Pryor,K.D., Wu,J.K., Marsilio,F., Patel,R.A., Craik,C.S., Ellman,J.A., Cummings,R.T. and Thornberry,N.A.
Catalytic properties and inhibition of proline-specific dipeptidyl peptidases II, IV and VII
Biochem J (15-4-2003) 371, 525-532. PubMed Europe PubMed DOI PMC EPMC P
Lorey,S., Stockel-Maschek,A., Faust,J., Brandt,W., Stiebitz,B., Gorrell,M.D., Kahne,T., Mrestani-Klaus,C., Wrenger,S., Reinhold,D., Ansorge,S. and Neubert,K.
Different modes of dipeptidyl peptidase IV (CD26) inhibition by oligopeptides derived from the N-terminus of HIV-1 Tat indicate at least two inhibitor binding sites
Eur J Biochem (2003) 270, 2147-2156. PubMed Europe PubMed DOI I
[YEAR:25-4-2003]Ludwig,K., Yan,S., Fan,H., Reutter,W. and Bottcher,C.
The 3D structure of rat DPPIV/CD26 as obtained by cryo-TEM and single particle analysis
Biochem Biophys Res Commun (25-4-2003) 304, 73-77. PubMed Europe PubMed DOI S
Nagakura,T., Yasuda,N., Yamazaki,K., Ikuta,H. and Tanaka,I.
Enteroinsular axis of db/db mice and efficacy of dipeptidyl peptidase IV inhibition
Metabolism (2003) 52, 81-86. PubMed Europe PubMed DOI
Oefner,C., D'arcy,A., Mac Sweeney,A., Pierau,S., Gardiner,R. and Dale,G.E.
High-resolution structure of human apo dipeptidyl peptidase IV/CD26 and its complex with 1-[([2-[(5-iodopyridin-2-yl)amino]-ethyl]amino)-acetyl]-2-cyano-(S)-pyrrol idine
Acta Crystallogr D Biol Crystallogr (2003) 59, 1206-1212. PubMed Europe PubMed DOI S I
Pospisilik,J.A., Martin,J., Doty,T., Ehses,J.A., Pamir,N., Lynn,F.C., Piteau,S., Demuth,H.U., McIntosh,C.H. and Pederson,R.A.
Dipeptidyl peptidase IV inhibitor treatment stimulates beta-cell survival and islet neogenesis in streptozotocin-induced diabetic rats
Diabetes (2003) 52, 741-750. PubMed Europe PubMed DOI I
Rasmussen,H.B., Branner,S., Wiberg,F.C. and Wagtmann,N.
Crystal structure of human dipeptidyl peptidase IV/CD26 in complex with a substrate analog
Nat Struct Biol (2003) 10, 19-25. PubMed Europe PubMed DOI S
[YEAR:15-8-2003]Sakurada,C., Sakurada,S., Hayashi,T., Katsuyama,S., Tan-No,K. and Sakurada,T.
Degradation of endomorphin-2 at the supraspinal level in mice is initiated by dipeptidyl peptidase IV: an in vitro and in vivo study
Biochem Pharmacol (15-8-2003) 66, 653-661. PubMed Europe PubMed DOI
Thoma,R., Loffler,B., Stihle,M., Huber,W., Ruf,A. and Hennig,M.
Structural basis of proline-specific exopeptidase activity as observed in human dipeptidyl peptidase-IV
Structure (2003) 11, 947-959. PubMed Europe PubMed DOI S
[YEAR:19-6-2003]Villhauer,E.B., Brinkman,J.A., Naderi,G.B., Burkey,B.F., Dunning,B.E., Prasad,K., Mangold,B.L., Russell,M.E. and Hughes,T.E.
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties
J Med Chem (19-6-2003) 46, 2774-2789. PubMed Europe PubMed DOI I
Williams,Y.N., Baba,H., Hayashi,S., Ikai,H., Sugita,T., Tanaka,S., Miyasaka,N. and Kubota,T.
Dipeptidyl peptidase IV on activated T cells as a target molecule for therapy of rheumatoid arthritis
Clin Exp Immunol (2003) 131, 68-74. PubMed Europe PubMed DOI PMC EPMC
[YEAR:20-6-2003]Zhu,L., Tamvakopoulos,C., Xie,D., Dragovic,J., Shen,X., Fenyk-Melody,J.E., Schmidt,K., Bagchi,A., Griffin,P.R., Thornberry,N.A. and Sinha Roy,R.
The role of dipeptidyl peptidase IV in the cleavage of glucagon family peptides: in vivo metabolism of pituitary adenylate cyclase activating polypeptide-(1-38)
J Biol Chem (20-6-2003) 278, 22418-22423. PubMed Europe PubMed DOI

2002

Ahren,B., Simonsson,E., Larsson,H., Landin-Olsson,M., Torgeirsson,H., Jansson,P.A., Sandqvist,M., Bavenholm,P., Efendic,S., Eriksson,J.W., Dickinson,S. and Holmes,D.
Inhibition of dipeptidyl peptidase IV improves metabolic control over a 4-week study period in type 2 diabetes
Diabetes Care (2002) 25, 869-875. PubMed Europe PubMed DOI I
[YEAR:22-3-2002]Alfalah,M., Jacob,R. and Naim,H.Y.
Intestinal dipeptidyl peptidase IV is efficiently sorted to the apical membrane through the concerted action of N- and O-glycans as well as association with lipid microdomains
J Biol Chem (22-3-2002) 277, 10683-10690. PubMed Europe PubMed DOI
Christopherson,K.W., Hangoc,G. and Broxmeyer,H.E.
Cell surface peptidase CD26/dipeptidylpeptidase IV regulates CXCL12/stromal cell-derived factor-1 alpha-mediated chemotaxis of human cord blood CD34+ progenitor cells
J Immunol (2002) 169, 7000-7008. PubMed Europe PubMed
Deacon,C.F., Wamberg,S., Bie,P., Hughes,T.E. and Holst,J.J.
Preservation of active incretin hormones by inhibition of dipeptidyl peptidase IV suppresses meal-induced incretin secretion in dogs
J Endocrinol (2002) 172, 355-362. PubMed Europe PubMed DOI I
Dobers,J., Zimmermann-Kordmann,M., Leddermann,M., Schewe,T., Reutter,W. and Fan,H.
Expression, purification, and characterization of human dipeptidyl peptidase IV/CD26 in Sf9 insect cells
Protein Expr Purif (2002) 25, 527-532. PubMed Europe PubMed DOI E
Ikushima,H., Munakata,Y., Iwata,S., Ohnuma,K., Kobayashi,S., Dang,N.H. and Morimoto,C.
Soluble CD26/dipeptidyl peptidase IV enhances transendothelial migration via its interaction with mannose 6-phosphate/insulin-like growth factor II receptor
Cell Immunol (2002) 215, 106-110. PubMed Europe PubMed DOI
[YEAR:15-12-2002]Lambeir,A.M., Proost,P., Scharpe,S. and De Meester,I.
A kinetic study of glucagon-like peptide-1 and glucagon-like peptide-2 truncation by dipeptidyl peptidase IV, in vitro
Biochem Pharmacol (15-12-2002) 64, 1753-1756. PubMed Europe PubMed DOI
[YEAR:6-9-2002]Lorey,S., Faust,J., Mrestani-Klaus,C., Kahne,T., Ansorge,S., Neubert,K. and Buhling,F.
Transcellular proteolysis demonstrated by novel cell surface-associated substrates of dipeptidyl peptidase IV (CD26)
J Biol Chem (6-9-2002) 277, 33170-33177. PubMed Europe PubMed DOI
Ludwig,A., Schiemann,F., Mentlein,R., Lindner,B. and Brandt,E.
Dipeptidyl peptidase IV (CD26) on T cells cleaves the CXC chemokine CXCL11 (I-TAC) and abolishes the stimulating but not the desensitizing potential of the chemokine
J Leukoc Biol (2002) 72, 183-191. PubMed Europe PubMed
Mitani,H., Takimoto,M. and Kimura,M.
Dipeptidyl peptidase IV inhibitor NVP-DPP728 ameliorates early insulin response and glucose tolerance in aged rats but not in aged Fischer 344 rats lacking its enzyme activity
Jpn J Pharmacol (2002) 88, 451-458. PubMed Europe PubMed DOI I
Pospisilik,J.A., Stafford,S.G., Demuth,H.U., Brownsey,R., Parkhouse,W., Finegood,D.T., McIntosh,C.H. and Pederson,R.A.
Long-term treatment with the dipeptidyl peptidase IV inhibitor P32/98 causes sustained improvements in glucose tolerance, insulin sensitivity, hyperinsulinemia, and beta-cell glucose responsiveness in VDF (fa/fa) Zucker rats
Diabetes (2002) 51, 943-950. PubMed Europe PubMed I
Pospisilik,J.A., Stafford,S.G., Demuth,H.U., McIntosh,C.H. and Pederson,R.A.
Long-term treatment with dipeptidyl peptidase IV inhibitor improves hepatic and peripheral insulin sensitivity in the VDF Zucker rat: a euglycemic-hyperinsulinemic clamp study
Diabetes (2002) 51, 2677-2683. PubMed Europe PubMed I
Reimer,M.K., Holst,J.J. and Ahren,B.
Long-term inhibition of dipeptidyl peptidase IV improves glucose tolerance and preserves islet function in mice
Eur J Endocrinol (2002) 146, 717-727. PubMed Europe PubMed I
[YEAR:31-5-2002]Richard,E., Alam,S.M., Arredondo-Vega,F.X., Patel,D.D. and Hershfield,M.S.
Clustered charged amino acids of human adenosine deaminase comprise a functional epitope for binding the adenosine deaminase complexing Protein CD26/Dipeptidyl Peptidase IV
J Biol Chem (31-5-2002) 277, 19720-19726. PubMed Europe PubMed DOI
Shinosaki,T., Kobayashi,T., Kimura,K. and Kurihara,H.
Involvement of dipeptidyl peptidase IV in immune complex-mediated glomerulonephritis
Lab Invest (2002) 82, 505-513. PubMed Europe PubMed
Sudre,B., Broqua,P., White,R.B., Ashworth,D., Evans,D.M., Haigh,R., Junien,J.L. and Aubert,M.L.
Chronic inhibition of circulating dipeptidyl peptidase IV by FE 999011 delays the occurrence of diabetes in male zucker diabetic fatty rats
Diabetes (2002) 51, 1461-1469. PubMed Europe PubMed I
[YEAR:6-6-2002]Villhauer,E.B., Brinkman,J.A., Naderi,G.B., Dunning,B.E., Mangold,B.L., Mone,M.D., Russell,M.E., Weldon,S.C. and Hughes,T.E.
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties
J Med Chem (6-6-2002) 45, 2362-2365. PubMed Europe PubMed DOI I

2001

Akiyama,T., Abe,M., Harada,S., Kojima,F., Sawa,R., Takahashi,Y., Naganawa,H., Homma,Y., Hamada,M., Yamaguchi,A., Aoyagi,T., Muraoka,Y. and Takeuchi,T.
Sulphostin, a potent inhibitor for dipeptidyl peptidase IV from Streptomyces sp. MK251-43F3
J Antibiot (Tokyo) (2001) 54, 744-746. PubMed Europe PubMed I
Deacon,C.F., Danielson,P., Klarskov,L., Olesen,M. and Holst,J.J.
Dipeptidyl peptidase IV inhibition reduces the degradation and clearance of GIP and potentiates its insulinotropic and antihyperglycemic effects in anesthetized pigs
Diabetes (2001) 50, 1588-1597. PubMed Europe PubMed
[YEAR:15-4-2001]Gonzalez-Gronow,M., Grenett,H.E., Weber,M.R., Gawdi,G. and Pizzo,S.V.
Interaction of plasminogen with dipeptidyl peptidase IV initiates a signal transduction mechanism which regulates expression of matrix metalloproteinase-9 by prostate cancer cells
Biochem J (15-4-2001) 355, 397-407. PubMed Europe PubMed DOI PMC EPMC
Gorrell,M.D., Gysbers,V. and McCaughan,G.W.
CD26: a multifunctional integral membrane and secreted protein of activated lymphocytes
Scand J Immunol (2001) 54, 249-264. PubMed Europe PubMed DOI
Hass,G.M., Meyer,J.L., Newitt,R.A., Labuda,T., Brown,L., Aebersold,R. and Vessella,R.L.
Identification of the target of monoclonal antibody A6H as dipeptidyl peptidase IV/CD26 by LC MS\MS
Hybridoma (2001) 20, 231-236. PubMed Europe PubMed DOI
Hildebrandt,M., Arck,P.C., Kruber,S., Demuth,H.U., Reutter,W. and Klapp,B.F.
Inhibition of dipeptidyl peptidase IV (DP IV, CD26) activity abrogates stress-induced, cytokine-mediated murine abortions
Scand J Immunol (2001) 53, 449-454. PubMed Europe PubMed DOI I
[YEAR:10-8-2001]Lambeir,A.M., Proost,P., Durinx,C., Bal,G., Senten,K., Augustyns,K., Scharpe,S., Van Damme,J. and De Meester,I.
Kinetic investigation of chemokine truncation by CD26/dipeptidyl peptidase IV reveals a striking selectivity within the chemokine family
J Biol Chem (10-8-2001) 276, 29839-29845. PubMed Europe PubMed DOI
[YEAR:2-11-2001]Lambeir,A.M., Durinx,C., Proost,P., Van Damme,J., Scharpe,S. and De Meester,I.
Kinetic study of the processing by dipeptidyl-peptidase IV/CD26 of neuropeptides involved in pancreatic insulin secretion
FEBS Lett (2-11-2001) 507, 327-330. PubMed Europe PubMed DOI
[YEAR:8-6-2001]Nagakura,T., Yasuda,N., Yamazaki,K., Ikuta,H., Yoshikawa,S., Asano,O. and Tanaka,I.
Improved glucose tolerance via enhanced glucose-dependent insulin secretion in dipeptidyl peptidase IV-deficient Fischer rats
Biochem Biophys Res Commun (8-6-2001) 284, 501-506. PubMed Europe PubMed DOI
[YEAR:12-1-2001]Pospisilik,J.A., Hinke,S.A., Pederson,R.A., Hoffmann,T., Rosche,F., Schlenzig,D., Glund,K., Heiser,U., McIntosh,C.H. and Demuth,H.
Metabolism of glucagon by dipeptidyl peptidase IV (CD26)
Regul Pept (12-1-2001) 96, 133-141. PubMed Europe PubMed DOI I
Sentandreu,M.A. and Toldra,F.
Dipeptidyl peptidase IV from porcine skeletal muscle: purification and biochemical properties
Food Chem (2001) 75, 159-168.
[YEAR:1-2-2001]Steinbrecher,A., Reinhold,D., Quigley,L., Gado,A., Tresser,N., Izikson,L., Born,I., Faust,J., Neubert,K., Martin,R., Ansorge,S. and Brocke,S.
Targeting dipeptidyl peptidase IV (CD26) suppresses autoimmune encephalomyelitis and up-regulates TGF-beta1 secretion in vivo
J Immunol (1-2-2001) 166, 2041-2048. PubMed Europe PubMed I

2000

Dobers,J., Grams,S., Reutter,W. and Fan,H.
Roles of cysteines in rat dipeptidyl peptidase IV/CD26 in processing and proteolytic activity
Eur J Biochem (2000) 267, 5093-5100. PubMed Europe PubMed DOI
[YEAR:2-4-2000]Erickson,R.H., Lai,R.S. and Kim,Y.S.
Role of hepatocyte nuclear factor 1alpha and 1beta in the transcriptional regulation of human dipeptidyl peptidase IV during differentiation of Caco-2 cells
Biochem Biophys Res Commun (2-4-2000) 270, 235-239. PubMed Europe PubMed DOI
Gorrell,M.D., Abbott,C.A., Kahne,T., Levy,M.T., Church,W.B. and McCaughan,G.W.
Relating structure to function in the beta-propeller domain of dipeptidyl peptidase IV. Point mutations that influence adenosine deaminase binding, antibody binding and enzyme activity
Adv Exp Med Biol (2000) 477, 89-95. PubMed Europe PubMed DOI
Hildebrandt,M., Reutter,W., Arck,P., Rose,M. and Klapp,B.F.
A guardian angel: the involvement of dipeptidyl peptidase IV in psychoneuroendocrine function, nutrition and immune defence
Clin Sci (Lond) (2000) 99, 93-104. PubMed Europe PubMed
[YEAR:11-2-2000]Hinke,S.A., Pospisilik,J.A., Demuth,H.U., Mannhart,S., Kuhn-Wache,K., Hoffmann,T., Nishimura,E., Pederson,R.A. and McIntosh,C.H.
Dipeptidyl peptidase IV (DPIV/CD26) degradation of glucagon. Characterization of glucagon degradation products and DPIV-resistant analogs
J Biol Chem (11-2-2000) 275, 3827-3834. PubMed Europe PubMed DOI
[YEAR:6-6-2000]Marguet,D., Baggio,L., Kobayashi,T., Bernard,A.M., Pierres,M., Nielsen,P.F., Ribel,U., Watanabe,T., Drucker,D.J. and Wagtmann,N.
Enhanced insulin secretion and improved glucose tolerance in mice lacking CD26
Proc Natl Acad Sci U S A (6-6-2000) 97, 6874-6879. PubMed Europe PubMed DOI PMC EPMC K
Pethiyagoda,C.L., Welch,D.R. and Fleming,T.P.
Dipeptidyl peptidase IV (DPPIV) inhibits cellular invasion of melanoma cells
Clin Exp Metastasis (2000) 18, 391-400. PubMed Europe PubMed DOI
[YEAR:6-11-2000]Richard,E., Arredondo-Vega,F.X., Santisteban,I., Kelly,S.J., Patel,D.D. and Hershfield,M.S.
The binding site of human adenosine deaminase for CD26/Dipeptidyl peptidase IV: the Arg142Gln mutation impairs binding to cd26 but does not cause immune deficiency
J Exp Med (6-11-2000) 192, 1223-1236. PubMed Europe PubMed DOI PMC EPMC
[YEAR:15-6-2000]Stockel-Maschek,A., Mrestani-Klaus,C., Stiebitz,B., Demuth,H. and Neubert,K.
Thioxo amino acid pyrrolidides and thiazolidides: new inhibitors of proline specific peptidases
Biochim Biophys Acta (15-6-2000) 1479, 15-31. PubMed Europe PubMed DOI I
Stockel-Maschek,A., Stiebitz,B., Born,I., Faust,J., Mogelin,W. and Neubert,K.
Potent inhibitors of dipeptidyl peptidase IV and their mechanisms of inhibition
Adv Exp Med Biol (2000) 477, 117-123. PubMed Europe PubMed DOI I
[YEAR:21-7-2000]Wrenger,S., Faust,J., Mrestani-Klaus,C., Fengler,A., Stockel-Maschek,A., Lorey,S., Kahne,T., Brandt,W., Neubert,K., Ansorge,S. and Reinhold,D.
Down-regulation of T cell activation following inhibition of dipeptidyl peptidase IV/CD26 by the N-terminal part of the thromboxane A2 receptor
J Biol Chem (21-7-2000) 275, 22180-22186. PubMed Europe PubMed
[YEAR:21-1-2000]Wrenger,S., Kahne,T., Bohuon,C., Weglohner,W., Ansorge,S. and Reinhold,D.
Amino-terminal truncation of procalcitonin, a marker for systemic bacterial infections, by dipeptidyl peptidase IV (DP IV)
FEBS Lett (21-1-2000) 466, 155-159. PubMed Europe PubMed DOI

1999

Abbott,C.A., McCaughan,G.W., Levy,M.T., Church,W.B. and Gorrell,M.D.
Binding to human dipeptidyl peptidase IV by adenosine deaminase and antibodies that inhibit ligand binding involves overlapping, discontinuous sites on a predicted beta propeller domain
Eur J Biochem (1999) 266, 798-810. PubMed Europe PubMed DOI
Augustyns,K., Bal,G., Thonus,G., Belyaev,A., Zhang,X.M., Bollaert,W., Lambeir,A.M., Durinx,C., Goossens,F. and Haemers,A.
The unique properties of dipeptidyl-peptidase IV (DPP IV/CD26) and the therapeutic potential of DPP IV inhibitors
Curr Med Chem (1999) 6, 311-327. PubMed Europe PubMed I
Belyaev,A., Zhang,X., Augustyns,K., Lambeir,A.M., De Meester,I., Vedernikova,I., Scharpe,S. and Haemers,A.
Structure-activity relationship of diaryl phosphonate esters as potent irreversible dipeptidyl peptidase IV inhibitors
J Med Chem (1999) 42, 1041-1052. PubMed Europe PubMed DOI I
Cheng,H.C., Abdel-Ghany,M., Zhang,S. and Pauli,B.U.
Is the Fischer 344/CRJ rat a protein-knock-out model for dipeptidyl peptidase IV-mediated lung metastasis of breast cancer?
Clin Exp Metastasis (1999) 17, 609-615. PubMed Europe PubMed DOI K
[YEAR:15-2-1999]Erickson,R.H., Gum,J.R., Lotterman,C.D., Hicks,J.W., Lai,R.S. and Kim,Y.S.
Regulation of the gene for human dipeptidyl peptidase IV by hepatocyte nuclear factor 1alpha
Biochem J (15-2-1999) 338, 91-97. PubMed Europe PubMed DOI PMC EPMC
Gilmartin,L. and O'Cuinn,G.
Dipeptidyl aminopeptidase IV and aminopeptidase P, two proline specific enzymes from the cytoplasm of guinea-pig brain: their role in metabolism of peptides containing consecutive prolines
Neurosci Res (1999) 34, 1-11. PubMed Europe PubMed DOI
Grondin,G., Hooper,N.M. and LeBel,D.
Specific localization of membrane dipeptidase and dipeptidyl peptidase IV in secretion granules of two different pancreatic islet cells
J Histochem Cytochem (1999) 47, 489-498. PubMed Europe PubMed
[YEAR:7-9-1999]Hughes,T.E., Mone,M.D., Russell,M.E., Weldon,S.C. and Villhauer,E.B.
NVP-DPP728 (1-[[[2-[(5-cyanopyridin-2-yl) amino]ethyl] amino] acetyl]-2-cyano-(S)-pyrrolidine), a slow-binding inhibitor of dipeptidyl peptidase IV
Biochemistry (7-9-1999) 38, 11597-11603. PubMed Europe PubMed DOI I
Siegel,E.G., Scharf,G., Gallwitz,B., Mentlein,R., Morys-Wortmann,C., Folsch,U.R. and Schmidt,W.E.
Comparison of the effect of native glucagon-like peptide 1 and dipeptidyl peptidase IV-resistant analogues on insulin release from rat pancreatic islets
Eur J Clin Invest (1999) 29, 610-614. PubMed Europe PubMed DOI
Wagner,L., Naude,R.J., Oelofsen,W., Naganuma,T. and Muramoto,K.
Isolation and partial characterization of dipeptidyl peptidase IV from ostrich kidney
Enzyme Microb Technol (1999) 25, 576-583.

1998

Ben-Shooshan,I. and Parola,A.H.
The CP-I subunit of adenosine deaminase complexing protein from calf kidney is identical to human, mouse, and rat dipeptidyl peptidase IV
Comp Biochem Physiol B Biochem Mol Biol (1998) 119, 289-292. PubMed Europe PubMed DOI
Holst,J.J. and Deacon,C.F.
Inhibition of the activity of dipeptidyl-peptidase IV as a treatment for type 2 diabetes
Diabetes (1998) 47, 1663-1670. PubMed Europe PubMed DOI
Iwaki-Egawa,S., Watanabe,Y., Kikuya,Y. and Fujimoto,Y.
Dipeptidyl peptidase IV from human serum: purification, characterization, and N-terminal amino acid sequence
J Biochem (1998) 124, 428-433. PubMed Europe PubMed
[YEAR:15-6-1998]Niedermeyer,J., Enenkel,B., Park,J.E., Lenter,M., Rettig,W.J., Damm,K. and Schnapp,A.
Mouse fibroblast-activation protein - conserved Fap gene organization and biochemical function as a serine protease
Eur J Biochem (15-6-1998) 254, 650-654. PubMed Europe PubMed DOI

1997

Brandt,W.
A molecular model of the active site of dipeptidyl peptidase IV. Explanation of the substrate specificity and interaction with inhibitors
Adv Exp Med Biol (1997) 421, 171-178. PubMed Europe PubMed
Van Noorden,C.J., Boonacker,E., Bissell,E.R., Meijer,A.J., van Marle,J. and Smith,R.E.
Ala-Pro-Cresyl violet, a synthetic fluorogenic substrate for the analysis of kinetic parameters of dipeptidyl peptidase IV (CD26) in individual living rat hepatocytes
Anal Biochem (1997) 252, 71-77. PubMed Europe PubMed DOI A

1996

Mentzel,S., Dijkman,H.B., van Son,J.P., Koene,R.A. and Assmann,K.J.
Organ distribution of aminopeptidase A and dipeptidyl peptidase IV in normal mice
J Histochem Cytochem (1996) 44, 445-461. PubMed Europe PubMed
Pederson,R.A., Kieffer,T.J., Pauly,R., Kofod,H., Kwong,J. and McIntosh,C.H.
The enteroinsular axis in dipeptidyl peptidase IV-negative rats
Metabolism (1996) 45, 1335-1341. PubMed Europe PubMed DOI K
Shibuya-Saruta,H., Kasahara,Y. and Hashimoto,Y.
Human serum dipeptidyl peptidase IV (DPPIV) and its unique properties
J Clin Lab Anal (1996) 10, 435-440. PubMed Europe PubMed DOI I

1995

Bohm,S.K., Gum,J.R., Jr., Erickson,R.H., Hicks,J.W. and Kim,Y.S.
Human dipeptidyl peptidase IV gene promoter: tissue-specific regulation from a TATA-less GC-rich sequence characteristic of a housekeeping gene promoter
Biochem J (1995) 311, 835-843. PubMed Europe PubMed PMC EPMC
Borloo,M., Augustyns,K., Belyaev,A., De Meester,I., Lambeir,A.M., Goossens,F., Bollaert,W., Rajan,P., Scharpe,S. and Haemers,A.
Synthesis and evaluation of azaproline peptides as potential inhibitors of dipeptidyl peptidase IV and prolyl oligopeptidase
Lett Pept Sci (1995) 2, 198-202. DOI I
Iwaki-Egawa,S., Watanabe,Y. and Fujimoto,Y.
Is CD26/dipeptidyl peptidase IV a really important molecule in T cell activation of a certain rat strain?
Immunobiology (1995) 194, 429-442. PubMed Europe PubMed DOI
Li,J., Wilk,E. and Wilk,S.
Aminoacylpyrrolidine-2-nitriles: potent and stable inhibitors of dipeptidyl-peptidase IV (CD 26)
Arch Biochem Biophys (1995) 323, 148-154. PubMed Europe PubMed DOI I
Shibuya-Saruta,H., Sugiyama,M. and Kasahara,Y.
Colorimetrical rate assay for urinary dipeptidyl peptidase IV (DPPIV) activity using a new substrate
J Clin Lab Anal (1995) 9, 113-118. PubMed Europe PubMed DOI A I

1994

Bernard,A.M., Mattei,M.G., Pierres,M. and Marguet,D.
Structure of the mouse dipeptidyl peptidase IV (CD26) gene
Biochemistry (1994) 33, 15204-15214. PubMed Europe PubMed DOI
[YEAR:11-11-1994]Boduszek,B., Oleksyszyn,J., Kam,C.M., Selzler,J., Smith,R.E. and Powers,J.C.
Dipeptide phosphonates as inhibitors of dipeptidyl peptidase IV
J Med Chem (11-11-1994) 37, 3969-3976. PubMed Europe PubMed DOI I
Borloo,M. and De Meester,I.
Dipeptidyl peptidase IV: development, design, synthesis and biological evaluation of inhibitors
Verh K Acad Geneeskd Belg (1994) 56, 57-88. PubMed Europe PubMed I
Ikehara,Y., Ogata,S. and Misumi,Y.
Dipeptidyl-peptidase IV from rat liver
Methods Enzymol (1994) 244, 215-227. PubMed Europe PubMed DOI V
Ohkubo,I., Huang,K., Ochiai,Y., Takagaki,M. and Kani,K.
Dipeptidyl peptidase IV from porcine seminal plasma: purification, characterization, and N-terminal amino acid sequence
J Biochem (1994) 116, 1182-1186. PubMed Europe PubMed I

1993

[YEAR:15-8-1993]David,F., Bernard,A.M., Pierres,M. and Marguet,D.
Identification of serine 624, aspartic acid 702, and histidine 734 as the catalytic triad residues of mouse dipeptidyl-peptidase IV (CD26). A member of a novel family of nonclassical serine hydrolases
J Biol Chem (15-8-1993) 268, 17247-17252. PubMed Europe PubMed

1992

Barrett,A.J. and Rawlings,N.D.
Oligopeptidases, and the emergence of the prolyl oligopeptidase family
Biol Chem Hoppe Seyler (1992) 373, 353-360. PubMed Europe PubMed
Darmoul,D., Lacasa,M., Baricault,L., Marguet,D., Sapin,C., Trotot,P., Barbat,A. and Trugnan,G.
Dipeptidyl peptidase IV (CD 26) gene expression in enterocyte-like colon cancer cell lines HT-29 and Caco-2. Cloning of the complete human coding sequence and changes of dipeptidyl peptidase IV mRNA levels during cell differentiation
J Biol Chem (1992) 267, 4824-4833. PubMed Europe PubMed
[YEAR:15-6-1992]Fujiwara,T., Tsuji,E., Misumi,Y., Takami,N. and Ikehara,Y.
Selective cell-surface expression of dipeptidyl peptidase IV with mutations at the active site sequence
Biochem Biophys Res Commun (15-6-1992) 185, 776-784. PubMed Europe PubMed DOI
Misumi,Y., Hayashi,Y., Arakawa,F. and Ikehara,Y.
Molecular cloning and sequence analysis of human dipeptidyl peptidase IV, a serine proteinase on the cell surface
Biochim Biophys Acta (1992) 1131, 333-336. PubMed Europe PubMed DOI
Ogata,S., Misumi,Y., Tsuji,E., Takami,N., Oda,K. and Ikehara,Y.
Identification of the active site residues in dipeptidyl peptidase IV by affinity labeling and site-directed mutagenesis
Biochemistry (1992) 31, 2582-2587. PubMed Europe PubMed DOI I
[YEAR:1-12-1992]Tsuji,E., Misumi,Y., Fujiwara,T., Takami,N., Ogata,S. and Ikehara,Y.
An active-site mutation (Gly633 - >Arg) of dipeptidyl peptidase IV causes its retention and rapid degradation in the endoplasmic reticulum
Biochemistry (1-12-1992) 31, 11921-11927. PubMed Europe PubMed DOI K

1991

[YEAR:15-2-1991]Flentke,G.R., Munoz,E., Huber,B.T., Plaut,A.G., Kettner,C.A. and Bachovchin,W.W.
Inhibition of dipeptidyl aminopeptidase IV (DP-IV) by Xaa-boroPro dipeptides and use of these inhibitors to examine the role of DP-IV in T-cell function
Proc Natl Acad Sci U S A (15-2-1991) 88, 1556-1559. PubMed Europe PubMed PMC EPMC I

1990

[YEAR:5-2-1990]Tiruppathi,C., Ganapathy,V. and Leibach,F.H.
Evidence for tripeptide-proton symport in renal brush border membrane vesicles. Studies in a novel rat strain with a genetic absence of dipeptidyl peptidase IV
J Biol Chem (5-2-1990) 265, 2048-2053. PubMed Europe PubMed K

1989

Ogata,S., Misumi,Y. and Ikehara,Y.
Primary structure of rat liver dipeptidyl peptidase IV deduced from its cDNA and identification of the NH2-terminal signal sequence as the membrane-anchoring domain
J Biol Chem (1989) 264, 3596-3601. PubMed Europe PubMed

1984

[YEAR:1-11-1984]Harada,M., Hiraoka,B.Y., Fukasawa,K.M. and Fukasawa,K.
Chemical modification of dipeptidyl peptidase IV: involvement of an essential tryptophan residue at the substrate binding site
Arch Biochem Biophys (1-11-1984) 234, 622-628. PubMed Europe PubMed
[YEAR:28-2-1984]Heins,J., Neubert,K., Barth,A., Canizaro,P.C. and Behal,F.J.
Kinetic investigation of the hydrolysis of aminoacyl p-nitroanilides by dipeptidyl peptidase IV from human and pig kidney
Biochim Biophys Acta (28-2-1984) 785, 30-35. PubMed Europe PubMed
Umezawa,H., Aoyagi,T., Ogawa,K., Naganawa,H., Hamada,M. and Takeuchi,T.
Diprotins A and B, inhibitors of dipeptidyl aminopeptidase IV, produced by bacteria
J Antibiot (Tokyo) (1984) 37, 422-425. PubMed Europe PubMed I

1983

[YEAR:20-4-1983]Erickson,R.H., Bella,A.M., Jr., Brophy,E.J., Kobata,A. and Kim,Y.S.
Purification and molecular characterization of rat intestinal brush border membrane dipeptidyl aminopeptidase IV
Biochim Biophys Acta (20-4-1983) 756, 258-265. PubMed Europe PubMed
[YEAR:22-11-1983]Miura,S., Song,I.S., Morita,A., Erickson,R.H. and Kim,Y.S.
Distribution and biosynthesis of aminopeptidase N and dipeptidyl aminopeptidase IV in rat small intestine
Biochim Biophys Acta (22-11-1983) 761, 66-75. PubMed Europe PubMed DOI
Morita,A., Chung,Y.C., Freeman,H.J., Erickson,R.H., Sleisenger,M.H. and Kim,Y.S.
Intestinal assimilation of a proline-containing tetrapeptide. Role of a brush border membrane postproline dipeptidyl aminopeptidase IV
J Clin Invest (1983) 72, 610-616. PubMed Europe PubMed DOI PMC EPMC
[YEAR:15-10-1983]Saison,M., Verlinden,J., Van Leuven,F., Cassiman,J.J. and Van Den Berghe,H.
Identification of cell surface dipeptidylpeptidase IV in human fibroblasts
Biochem J (15-10-1983) 216, 177-183. PubMed Europe PubMed PMC EPMC

1982

[YEAR:1-10-1982]Bella,A.M., Jr., Erickson,R.H. and Kim,Y.S.
Rat intestinal brush border membrane dipeptidyl-aminopeptidase IV: kinetic properties and substrate specificities of the purified enzyme
Arch Biochem Biophys (1-10-1982) 218, 156-162. PubMed Europe PubMed
Feller,A.C., Heijnen,C.J., Ballieux,R.E. and Parwaresch,M.R.
Enzymehistochemical staining of T mu lymphocytes for glycyl-proline-4-methoxy-beta-naphthylamide-peptidase (DAP IV)
Br J Haematol (1982) 51, 227-234. PubMed Europe PubMed
[YEAR:5-3-1982]Hama,T., Okada,M., Kojima,K., Kato,T., Matsuyama,M. and Nagatsu,T.
Purification of dipeptidyl-aminopeptidase IV from human kidney by anti dipeptidyl-aminopeptidase IV affinity chromatography
Mol Cell Biochem (5-3-1982) 43, 35-42. PubMed Europe PubMed
[YEAR:17-12-1982]Ichinose,M., Maeda,R., Fukuda,T., Watanabe,B., Ishimaru,T., Izumi,M., Miyake,S. and Takamori,M.
Partial purification and characterization of glycylprolyl dipeptidyl aminopeptidase in porcine pancreas
Biochim Biophys Acta (17-12-1982) 719, 527-531. PubMed Europe PubMed
Yoshimoto,T., Kita,T., Ichinose,M. and Tsuru,D.
Dipeptidyl aminopeptidase IV from porcine pancreas
J Biochem (1982) 92, 275-282. PubMed Europe PubMed

1980

Barth,A., Mager,H., Fischer,G., Neubert,K. and Schwarz,G.
[Structure-activity relationship in the enzymatic hydrolysis of dipeptide aryl amides by dipeptidyl peptidase IV]
Acta Biol Med Ger (1980) 39, 1129-1142. PubMed Europe PubMed
Iijima,K.I., Takei,T., Hino,M. and Hayakawa,T.
A new fluorescence assay for dipeptidylpeptidase IV using tripeptide L-prolyl-L-prolyl-L-alanine as substrate
J Biochem Biophys Methods (1980) 3, 89-96. PubMed Europe PubMed DOI A
Kreil,G., Haiml,L. and Suchanek,G.
Stepwise cleavage of the pro part of promelittin by dipeptidylpeptidase IV. Evidence for a new type of precursor-product conversion
Eur J Biochem (1980) 111, 49-58. PubMed Europe PubMed

1979

[YEAR:15-9-1979]Fukasawa,K.M., Fukasawa,K. and Harada,M.
Immunochemical identity of dipeptidyl aminopeptidase IV from pig serum, liver, submaxillary gland and kidney
Experientia (15-9-1979) 35, 1142-1143. PubMed Europe PubMed
[YEAR:3-4-1979]Gossrau,R.
[Peptidases II. Localization of dipeptidylpeptidase IV (DPP IV). Histochemical and biochemical study]
Histochemistry (3-4-1979) 60, 231-248. PubMed Europe PubMed L
[YEAR:5-3-1979]Kato,T., Iwase,K., Nagatsu,T., Hino,M., Takemoto,T. and Sakakibara,S.
A new assay of X-prolyl dipeptidyl-aminopeptidase activity in human serum with glycylproline p-phenylazoanilide as substrate
Mol Cell Biochem (5-3-1979) 24, 9-13. PubMed Europe PubMed A
[YEAR:26-2-1979]Krutzsch,H.C. and Pisano,J.J.
Preparation of dipeptidyl aminopeptidase IV for polypeptide sequencing
Biochim Biophys Acta (26-2-1979) 576, 280-289. PubMed Europe PubMed

1978

[YEAR:21-7-1978]Fukasawa,K.M., Fukasawa,K. and Harada,M.
Dipeptidyl aminopeptidase IV, a glycoprotein from pig kidney
Biochim Biophys Acta (21-7-1978) 535, 161-166. PubMed Europe PubMed
[YEAR:15-7-1978]Heymann,E. and Mentlein,R.
Liver dipeptidyl aminopeptidase IV hydrolyzes substance P
FEBS Lett (15-7-1978) 91, 360-364. PubMed Europe PubMed DOI
[YEAR:7-8-1978]Kato,T., Nagatsu,T., Fukasawa,K., Harada,M., Nagatsu,I. and Sakakibara,S.
Successive cleavage of N-terminal Arg1--Pro2 and Lys3-Pro4 from substance P but no release of Arg1-Pro2 from bradykinin, by X-Pro dipeptidyl-aminopeptidase
Biochim Biophys Acta (7-8-1978) 525, 417-422. PubMed Europe PubMed P
Kato,T., Nagatsu,T., Kimura,T. and Sakakibara,S.
Fluorescence assay of X-prolyl dipeptidyl-aminopeptidase activity with a new fluorogenic substrate
Biochem Med (1978) 19, 351-359. PubMed Europe PubMed A
[YEAR:15-3-1978]Kato,T., Nagatsu,T., Kimura,T. and Sakakibara,S.
Studies on substrate specificity of X-prolyl dipeptidyl-aminopeptidase during new chromogenic substrates, X-Y-p-nitroanilides
Experientia (15-3-1978) 34, 319-320. PubMed Europe PubMed P
Kullertz,G., Fischer,G. and Barth,A.
[Catalytic mechanism of dipeptidyl-peptidase IV]
Acta Biol Med Ger (1978) 37, 559-567. PubMed Europe PubMed
Wolf,B., Fischer,G. and Barth,A.
[Kinetics of dipeptidyl-peptidase IV]
Acta Biol Med Ger (1978) 37, 409-420. PubMed Europe PubMed

1976

Hino,M., Fuyamada,H., Hayakawa,T., Nagatsu,T. and Oya,H.
X-Prolyl dipeptidyl-aminopeptidase activity, with X-proline p-nitroanilides as substrates, in normal and pathological human sera
Clin Chem (1976) 22, 1256-1261. PubMed Europe PubMed
[YEAR:1-7-1976]Kenny,A.J., Booth,A.G., George,S.G., Ingram,J., Kershaw,D., Wood,E.J. and Young,A.R.
Dipeptidyl peptidase IV, a kidney brush-border serine peptidase
Biochem J (1-7-1976) 157, 169-182. PubMed Europe PubMed PMC EPMC

1975

[YEAR:9-7-1975]Hino,M., Nagatsu,T., Kakumu,S., Okuyama,S., Yoshii,Y. and Nagatsu,I.
Glycylprolyl beta-naphthylamidase activity in human serum
Clin Chim Acta (9-7-1975) 62, 5-11. PubMed Europe PubMed

1974

Oya,H., Harada,M. and Nagatsu,T.
Peptidase activity of glycylprolyl beta-naphthylamidase from human submaxillary gland
Arch Oral Biol (1974) 19, 489-491. PubMed Europe PubMed

1972

[YEAR:28-2-1972]Oya,H., Nagatsu,I. and Nagatsu,T.
Purification and properties of glycylprolyl beta-naphthylamidase in human submaxillary gland
Biochim Biophys Acta (28-2-1972) 258, 591-599. PubMed Europe PubMed

1970

Hopsu-Havu,V.K., Jansen,C.T. and Jarvinen,M.
A human serum aminopeptidase capable of splitting juxtaterminal bonds involving proline. Basic characteristics, normal values and clinical variations
Clin Chim Acta (1970) 28, 25-36. PubMed Europe PubMed

1968

Hopsu-Havu,V.K., Rintola,P. and Glenner,G.G.
A hog kidney aminopeptidase liberating N-terminal dipeptides. Partial purification and characteristics
Acta Chem Scand (1968) 22, 299-308. PubMed Europe PubMed
[YEAR:15-4-1968]Nagatsu,I., Nagatsu,T. and Yamamoto,T.
Hydrolysis of amino acid beta-naphthylamides by aminopeptidases in human parotid salva and human serum
Experientia (15-4-1968) 24, 347-348. PubMed Europe PubMed DOI

1967

Hopsu-Havu,V.K. and Sarimo,S.R.
Purification and characterization of an aminopeptidase hydrolyzing glycyl-proline-naphthylamide
Hoppe Seylers Z Physiol Chem (1967) 348, 1540-1550. PubMed Europe PubMed

1966

Hopsu-Havu,V.K. and Glenner,G.G.
A new dipeptide naphthylamidase hydrolyzing glycyl-prolyl-beta-naphthylamide
Histochemie (1966) 7, 197-201. PubMed Europe PubMed DOI