3w2t › Citations

A comparative study of the binding modes of recently launched dipeptidyl peptidase IV inhibitors in the active site.

Nabeno M, Akahoshi F, Kishida H, Miyaguchi I, Tanaka Y, Ishii S, Kadowaki T
Biochem Biophys Res Commun 434 191-6 (2013)
Cited: 117 times
EuropePMC logo PMID: 23501107

Abstract

In recent years, various dipeptidyl peptidase IV (DPP-4) inhibitors have been released as therapeutic drugs for type 2 diabetes in many countries. In spite of their diverse chemical structures, no comparative studies of their binding modes in the active site of DPP-4 have been disclosed. We determined the co-crystal structure of vildagliptin with DPP-4 by X-ray crystallography and compared the binding modes of six launched inhibitors in DPP-4. The inhibitors were categorized into three classes on the basis of their binding subsites: (i) vildagliptin and saxagliptin (Class 1) form interactions with the core S1 and S2 subsites and a covalent bond with Ser630 in the catalytic triad; (ii) alogliptin and linagliptin (Class 2) form interactions with the S1' and/or S2' subsites in addition to the S1 and S2 subsites; and (iii) sitagliptin and teneligliptin (Class 3) form interactions with the S1, S2 and S2 extensive subsites. The present study revealed that the additional interactions with the S1', S2' or S2 extensive subsite may increase DPP-4 inhibition beyond the level afforded by the fundamental interactions with the S1 and S2 subsites and are more effective than forming a covalent bond with Ser630.

Reviews - 3w2t mentioned but not cited (2)

  1. Pyrrolidine in Drug Discovery: A Versatile Scaffold for Novel Biologically Active Compounds. Li Petri G, Raimondi MV, Spanò V, Holl R, Barraja P, Montalbano A. Top Curr Chem (Cham) 379 34 (2021)
  2. The perceptions of natural compounds against dipeptidyl peptidase 4 in diabetes: from in silico to in vivo. Lin SR, Chang CH, Tsai MJ, Cheng H, Chen JC, Leong MK, Weng CF. Ther Adv Chronic Dis 10 2040622319875305 (2019)

Articles - 3w2t mentioned but not cited (5)

  1. Natural phenolic compounds potentiate hypoglycemia via inhibition of Dipeptidyl peptidase IV. Huang PK, Lin SR, Chang CH, Tsai MJ, Lee DN, Weng CF. Sci Rep 9 15585 (2019)
  2. Comprehensive analysis of the Co-structures of dipeptidyl peptidase IV and its inhibitor. Nojima H, Kanou K, Terashi G, Takeda-Shitaka M, Inoue G, Atsuda K, Itoh C, Iguchi C, Matsubara H. BMC Struct Biol 16 11 (2016)
  3. Molecular docking studies of α-mangostin, γ-mangostin, and xanthone on peroxisome proliferator-activated receptor gamma diphenyl peptidase-4 enzyme, and aldose reductase enzyme as an antidiabetic drug candidate. Mahmudah R, Adnyana IK, Sukandar EY. J Adv Pharm Technol Res 12 196-208 (2021)
  4. Computational Analysis of Gynura bicolor Bioactive Compounds as Dipeptidyl Peptidase-IV Inhibitor. Rozano L, Abdullah Zawawi MR, Ahmad MA, Jaganath IB. Adv Bioinformatics 2017 5124165 (2017)
  5. Anti-diabetic Activity of Brucine in Streptozotocin-Induced Rats: In Silico, In Vitro, and In Vivo Studies. Khan NU, Qazi NG, Khan AU, Ali F, Hassan SSU, Bungau S. ACS Omega 7 46358-46370 (2022)


Reviews citing this publication (34)

  1. DPP4 in Diabetes. Röhrborn D, Wronkowitz N, Eckel J. Front Immunol 6 386 (2015)
  2. Comparative review of dipeptidyl peptidase-4 inhibitors and sulphonylureas. Deacon CF, Lebovitz HE. Diabetes Obes Metab 18 333-347 (2016)
  3. Clinical Use of DPP-4 Inhibitors. Gallwitz B. Front Endocrinol (Lausanne) 10 389 (2019)
  4. Dipeptidyl peptidase 4 inhibitors in the treatment of type 2 diabetes mellitus. Deacon CF. Nat Rev Endocrinol 16 642-653 (2020)
  5. DPP4 and ACE2 in Diabetes and COVID-19: Therapeutic Targets for Cardiovascular Complications? Valencia I, Peiró C, Lorenzo Ó, Sánchez-Ferrer CF, Eckel J, Romacho T. Front Pharmacol 11 1161 (2020)
  6. The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected]. Filippatos TD, Athyros VG, Elisaf MS. Expert Opin Drug Metab Toxicol 10 787-812 (2014)
  7. Mechanisms and pathways of anti-inflammatory activity of DPP-4 inhibitors in cardiovascular and renal protection. Tomovic K, Lazarevic J, Kocic G, Deljanin-Ilic M, Anderluh M, Smelcerovic A. Med Res Rev 39 404-422 (2019)
  8. Recent approaches to medicinal chemistry and therapeutic potential of dipeptidyl peptidase-4 (DPP-4) inhibitors. Patel BD, Ghate MD. Eur J Med Chem 74 574-605 (2014)
  9. DPP-4 inhibitors in diabetic complications: role of DPP-4 beyond glucose control. Bae EJ. Arch Pharm Res 39 1114-1128 (2016)
  10. DPP-4 inhibitors: pharmacological differences and their clinical implications. Ceriello A, Sportiello L, Rafaniello C, Rossi F. Expert Opin Drug Saf 13 Suppl 1 S57-68 (2014)
  11. Gemigliptin: An Update of Its Clinical Use in the Management of Type 2 Diabetes Mellitus. Kim SH, Yoo JH, Lee WJ, Park CY. Diabetes Metab J 40 339-353 (2016)
  12. Cysteine cathepsins: their role in tumor progression and recent trends in the development of imaging probes. Löser R, Pietzsch J. Front Chem 3 37 (2015)
  13. Teneligliptin : expectations for its pleiotropic action. Morishita R, Nakagami H. Expert Opin Pharmacother 16 417-426 (2015)
  14. Teneligliptin in management of type 2 diabetes mellitus. Sharma SK, Panneerselvam A, Singh KP, Parmar G, Gadge P, Swami OC. Diabetes Metab Syndr Obes 9 251-260 (2016)
  15. The Role of Dipeptidyl Peptidase - 4 Inhibitors in Diabetic Kidney Disease. Panchapakesan U, Pollock C. Front Immunol 6 443 (2015)
  16. A survey of the role of nitrile groups in protein-ligand interactions. Wang Y, Du Y, Huang N. Future Med Chem 10 2713-2728 (2018)
  17. The importance of synthetic drugs for type 2 diabetes drug discovery. Safavi M, Foroumadi A, Abdollahi M. Expert Opin Drug Discov 8 1339-1363 (2013)
  18. The Unique Pharmacological and Pharmacokinetic Profile of Teneligliptin: Implications for Clinical Practice. Ceriello A, De Nigris V, Iijima H, Matsui T, Gouda M. Drugs 79 733-750 (2019)
  19. Role of Dipeptidyl Peptidase 4 Inhibitors in Antidiabetic Treatment. Yin R, Xu Y, Wang X, Yang L, Zhao D. Molecules 27 3055 (2022)
  20. Glucagon like peptide-1 and its receptor agonists: Their roles in management of Type 2 diabetes mellitus. Gupta A, Jelinek HF, Al-Aubaidy H. Diabetes Metab Syndr 11 225-230 (2017)
  21. Nitrile-containing pharmaceuticals: target, mechanism of action, and their SAR studies. Wang X, Wang Y, Li X, Yu Z, Song C, Du Y. RSC Med Chem 12 1650-1671 (2021)
  22. Vildagliptin , a DPP-4 inhibitor for the twice-daily treatment of type 2 diabetes mellitus with or without metformin. Forst T, Bramlage P. Expert Opin Pharmacother 15 1299-1313 (2014)
  23. Alogliptin benzoate for management of type 2 diabetes. Saisho Y. Vasc Health Risk Manag 11 229-243 (2015)
  24. DPP-4 Inhibitors: Renoprotective Potential and Pharmacokinetics in Type 2 Diabetes Mellitus Patients with Renal Impairment. Mikov M, Pavlović N, Stanimirov B, Đanić M, Goločorbin-Kon S, Stankov K, Al-Salami H. Eur J Drug Metab Pharmacokinet 45 1-14 (2020)
  25. Role of dipeptidyl peptidase-4 inhibitors in new-onset diabetes after transplantation. Lim SW, Jin JZ, Jin L, Jin J, Li C. Korean J Intern Med 30 759-770 (2015)
  26. Teneligliptin: a review in type 2 diabetes. Scott LJ. Clin Drug Investig 35 765-772 (2015)
  27. Treatment of type 2 diabetes, lifestyle, GLP1 agonists and DPP4 inhibitors. Tomkin GH. World J Diabetes 5 636-650 (2014)
  28. Activity and selectivity cliffs for DPP-IV inhibitors: Lessons we can learn from SAR studies and their application to virtual screening. Ojeda-Montes MJ, Gimeno A, Tomas-Hernández S, Cereto-Massagué A, Beltrán-Debón R, Valls C, Mulero M, Pujadas G, Garcia-Vallvé S. Med Res Rev 38 1874-1915 (2018)
  29. Efficacy and Safety of Teneligliptin in Patients With Type 2 Diabetes Mellitus: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. Li X, Huang X, Bai C, Qin D, Cao S, Mei Q, Ye Y, Wu J. Front Pharmacol 9 449 (2018)
  30. Saxagliptin for the treatment of diabetes - a focus on safety. Cernea S, Cahn A, Raz I. Expert Opin Drug Saf 15 697-707 (2016)
  31. Alogliptin for the treatment of type 2 diabetes: a drug safety evaluation. Yabe D, Seino Y. Expert Opin Drug Saf 15 249-264 (2016)
  32. Insight into Structure Activity Relationship of DPP-4 Inhibitors for Development of Antidiabetic Agents. Mathur V, Alam O, Siddiqui N, Jha M, Manaithiya A, Bawa S, Sharma N, Alshehri S, Alam P, Shakeel F. Molecules 28 5860 (2023)
  33. Pharmacological and Clinical Studies of Medicinal Plants That Inhibit Dipeptidyl Peptidase-IV. Rohani, Febrina E, Wahyuni IS, Levita J. Drug Des Devel Ther 17 3473-3491 (2023)
  34. [Pharmacological and clinical profile of a novel DPP-4 inhibitor teneligliptin hydrobromide hydrate (TENELIA(®)]. Goda M, Akahoshi F, Ishii S, Terata R, Hayashi Y. Nihon Yakurigaku Zasshi 142 134-143 (2013)

Articles citing this publication (76)

  1. Gliptin and GLP-1 analog treatment improves survival and vascular inflammation/dysfunction in animals with lipopolysaccharide-induced endotoxemia. Steven S, Hausding M, Kröller-Schön S, Mader M, Mikhed Y, Stamm P, Zinßius E, Pfeffer A, Welschof P, Agdauletova S, Sudowe S, Li H, Oelze M, Schulz E, Klein T, Münzel T, Daiber A. Basic Res Cardiol 110 6 (2015)
  2. Analyzing a dipeptide library to identify human dipeptidyl peptidase IV inhibitor. Lan VT, Ito K, Ohno M, Motoyama T, Ito S, Kawarasaki Y. Food Chem 175 66-73 (2015)
  3. Comparative Binding Analysis of Dipeptidyl Peptidase IV (DPP-4) with Antidiabetic Drugs - An Ab Initio Fragment Molecular Orbital Study. Arulmozhiraja S, Matsuo N, Ishitsubo E, Okazaki S, Shimano H, Tokiwa H. PLoS One 11 e0166275 (2016)
  4. Letter Efficacy and safety of teneligliptin, a dipeptidyl peptidase-4 inhibitor, combined with metformin in Korean patients with type 2 diabetes mellitus: a 16-week, randomized, double-blind, placebo-controlled phase III trial. Kim MK, Rhee EJ, Han KA, Woo AC, Lee MK, Ku BJ, Chung CH, Kim KA, Lee HW, Park IB, Park JY, Chul Jang HC, Park KS, Jang WI, Cha BY. Diabetes Obes Metab 17 309-312 (2015)
  5. Cross-talk between the dipeptidyl peptidase-4 and stromal cell-derived factor-1 in stem cell homing and myocardial repair: Potential impact of dipeptidyl peptidase-4 inhibitors. Anderluh M, Kocic G, Tomovic K, Kocic R, Deljanin-Ilic M, Smelcerovic A. Pharmacol Ther 167 100-107 (2016)
  6. Gliptins Suppress Inflammatory Macrophage Activation to Mitigate Inflammation, Fibrosis, Oxidative Stress, and Vascular Dysfunction in Models of Nonalcoholic Steatohepatitis and Liver Fibrosis. Wang X, Hausding M, Weng SY, Kim YO, Steven S, Klein T, Daiber A, Schuppan D. Antioxid Redox Signal 28 87-109 (2018)
  7. The novel dipeptidyl peptidase-4 inhibitor teneligliptin prevents high-fat diet-induced obesity accompanied with increased energy expenditure in mice. Fukuda-Tsuru S, Kakimoto T, Utsumi H, Kiuchi S, Ishii S. Eur J Pharmacol 723 207-215 (2014)
  8. Safety and efficacy of teneligliptin in Japanese patients with type 2 diabetes mellitus: a pooled analysis of two Phase III clinical studies. Kadowaki T, Marubayashi F, Yokota S, Katoh M, Iijima H. Expert Opin Pharmacother 16 971-981 (2015)
  9. The dipeptidyl peptidase-4 inhibitor teneligliptin improved endothelial dysfunction and insulin resistance in the SHR/NDmcr-cp rat model of metabolic syndrome. Nakagami H, Pang Z, Shimosato T, Moritani T, Kurinami H, Koriyama H, Tenma A, Shimamura M, Morishita R. Hypertens Res 37 629-635 (2014)
  10. Elevated CD26 Expression by Skin Fibroblasts Distinguishes a Profibrotic Phenotype Involved in Scar Formation Compared to Gingival Fibroblasts. Mah W, Jiang G, Olver D, Gallant-Behm C, Wiebe C, Hart DA, Koivisto L, Larjava H, Häkkinen L. Am J Pathol 187 1717-1735 (2017)
  11. A comparative study of the binding properties, dipeptidyl peptidase-4 (DPP-4) inhibitory activity and glucose-lowering efficacy of the DPP-4 inhibitors alogliptin, linagliptin, saxagliptin, sitagliptin and vildagliptin in mice. Berger JP, SinhaRoy R, Pocai A, Kelly TM, Scapin G, Gao YD, Pryor KAD, Wu JK, Eiermann GJ, Xu SS, Zhang X, Tatosian DA, Weber AE, Thornberry NA, Carr RD. Endocrinol Diabetes Metab 1 e00002 (2018)
  12. Anagliptin, a potent dipeptidyl peptidase IV inhibitor: its single-crystal structure and enzyme interactions. Watanabe YS, Yasuda Y, Kojima Y, Okada S, Motoyama T, Takahashi R, Oka M. J Enzyme Inhib Med Chem 30 981-988 (2015)
  13. Impact of teneligliptin on oxidative stress and endothelial function in type 2 diabetes patients with chronic kidney disease: a case-control study. Sagara M, Suzuki K, Aoki C, Tanaka S, Taguchi I, Inoue T, Aso Y. Cardiovasc Diabetol 15 76 (2016)
  14. Add-on treatment with teneligliptin ameliorates glucose fluctuations and improves glycemic control index in Japanese patients with type 2 diabetes on insulin therapy. Tanaka S, Suzuki K, Aoki C, Niitani M, Kato K, Tomotsune T, Aso Y. Diabetes Technol Ther 16 840-845 (2014)
  15. Teneligliptin as an initial therapy for newly diagnosed, drug naive subjects with type 2 diabetes. Kutoh E, Hirate M, Ikeno Y. J Clin Med Res 6 287-294 (2014)
  16. Trp-Arg-Xaa tripeptides act as uncompetitive-type inhibitors of human dipeptidyl peptidase IV. Lan VT, Ito K, Ito S, Kawarasaki Y. Peptides 54 166-170 (2014)
  17. Teneligliptin improves glycemic control with the reduction of postprandial insulin requirement in Japanese diabetic patients. Tsuchimochi W, Ueno H, Yamashita E, Tsubouchi C, Sakoda H, Nakamura S, Nakazato M. Endocr J 62 13-20 (2015)
  18. Navigating the chemical space of dipeptidyl peptidase-4 inhibitors. Shoombuatong W, Prachayasittikul V, Anuwongcharoen N, Songtawee N, Monnor T, Prachayasittikul S, Prachayasittikul V, Nantasenamat C. Drug Des Devel Ther 9 4515-4549 (2015)
  19. Glial cell type-specific changes in spinal dipeptidyl peptidase 4 expression and effects of its inhibitors in inflammatory and neuropatic pain. Király K, Kozsurek M, Lukácsi E, Barta B, Alpár A, Balázsa T, Fekete C, Szabon J, Helyes Z, Bölcskei K, Tékus V, Tóth ZE, Pap K, Gerber G, Puskár Z. Sci Rep 8 3490 (2018)
  20. Treatment with anagliptin, a DPP-4 inhibitor, decreases FABP4 concentration in patients with type 2 diabetes mellitus at a high risk for cardiovascular disease who are receiving statin therapy. Furuhashi M, Sakuma I, Morimoto T, Higashiura Y, Sakai A, Matsumoto M, Sakuma M, Shimabukuro M, Nomiyama T, Arasaki O, Node K, Ueda S. Cardiovasc Diabetol 19 89 (2020)
  21. DPP8 is a novel therapeutic target for multiple myeloma. Sato T, Tatekoshi A, Takada K, Iyama S, Kamihara Y, Jawaid P, Rehman MU, Noguchi K, Kondo T, Kajikawa S, Arita K, Wada A, Murakami J, Arai M, Yasuda I, Dang NH, Hatano R, Iwao N, Ohnuma K, Morimoto C. Sci Rep 9 18094 (2019)
  22. Predicting DPP-IV inhibitors with machine learning approaches. Cai J, Li C, Liu Z, Du J, Ye J, Gu Q, Xu J. J Comput Aided Mol Des 31 393-402 (2017)
  23. Tissue distribution of teneligliptin in rats and comparisons with data reported for other dipeptidyl peptidase-4 inhibitors. Nakamaru Y, Akahoshi F, Iijima H, Hisanaga N, Kume T. Biopharm Drug Dispos 37 142-155 (2016)
  24. Docking-generated multiple ligand poses for bootstrapping bioactivity classifying Machine Learning: Repurposing covalent inhibitors for COVID-19-related TMPRSS2 as case study. Hatmal MM, Abuyaman O, Taha M. Comput Struct Biotechnol J 19 4790-4824 (2021)
  25. Effects of teneligliptin on PDMPs and PAI-1 in patients with diabetes on hemodialysis. Okuda Y, Omoto S, Taniura T, Shouzu A, Nomura S. Int J Gen Med 9 65-71 (2016)
  26. Model Optimization and In Silico Analysis of Potential Dipeptidyl Peptidase IV Antagonists from GC-MS Identified Compounds in Nauclea latifolia Leaf Extracts. Iheagwam FN, Ogunlana OO, Chinedu SN. Int J Mol Sci 20 E5913 (2019)
  27. Vildagliptin and its metabolite M20.7 induce the expression of S100A8 and S100A9 in human hepatoma HepG2 and leukemia HL-60 cells. Asakura M, Karaki F, Fujii H, Atsuda K, Itoh T, Fujiwara R. Sci Rep 6 35633 (2016)
  28. Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling. Rea D, Van Elzen R, De Winter H, Van Goethem S, Landuyt B, Luyten W, Schoofs L, Van Der Veken P, Augustyns K, De Meester I, Fülöp V, Lambeir AM. Eur J Med Chem 139 482-491 (2017)
  29. DPP-4 Inhibitors Have Different Effects on Endothelial Low-Grade Inflammation and on the M1-M2 Macrophage Polarization Under Hyperglycemic Conditions. De Nigris V, Prattichizzo F, Iijima H, Ceriello A. Diabetes Metab Syndr Obes 14 1519-1531 (2021)
  30. Anagliptin ameliorates albuminuria and urinary liver-type fatty acid-binding protein excretion in patients with type 2 diabetes with nephropathy in a glucose-lowering-independent manner. Kitada M, Tsuda SI, Konishi K, Takeda-Watanabe A, Fujii M, Kanasaki K, Nishizawa M, Nakagawa A, Koya D. BMJ Open Diabetes Res Care 5 e000391 (2017)
  31. Crystal structures of a bacterial dipeptidyl peptidase IV reveal a novel substrate recognition mechanism distinct from that of mammalian orthologues. Roppongi S, Suzuki Y, Tateoka C, Fujimoto M, Morisawa S, Iizuka I, Nakamura A, Honma N, Shida Y, Ogasawara W, Tanaka N, Sakamoto Y, Nonaka T. Sci Rep 8 2714 (2018)
  32. Efficacy and safety of evogliptin treatment in patients with type 2 diabetes: A multicentre, active-controlled, randomized, double-blind study with open-label extension (the EVERGREEN study). Kim G, Lim S, Kwon HS, Park IB, Ahn KJ, Park CY, Kwon SK, Kim HS, Park SW, Kim SG, Moon MK, Kim ES, Chung CH, Park KS, Kim M, Chung DJ, Lee CB, Kim TH, Lee MK. Diabetes Obes Metab 22 1527-1536 (2020)
  33. Editorial Efficacy and safety of teneligliptin. Singh AK. Indian J Endocrinol Metab 21 11-17 (2017)
  34. Effect of switching to teneligliptin from other dipeptidyl peptidase-4 inhibitors on glucose control and renoprotection in type 2 diabetes patients with diabetic kidney disease. Kitada M, Ogura Y, Nitta K, Fujii M, Kanasaki K, Konishi K, Iida Y, Nakagawa A, Koya D. J Diabetes Investig 10 706-713 (2019)
  35. Effects of vildagliptin versus saxagliptin on daily acute glucose fluctuations in Chinese patients with T2DM inadequately controlled with a combination of metformin and sulfonylurea. Xiaoyan C, Jing W, Xiaochun H, Yuyu T, Shunyou D, Yingyu F. Curr Med Res Opin 32 1131-1136 (2016)
  36. Teneligliptin Decreases Uric Acid Levels by Reducing Xanthine Dehydrogenase Expression in White Adipose Tissue of Male Wistar Rats. Moriya C, Satoh H. J Diabetes Res 2016 3201534 (2016)
  37. The pathological significance of dipeptidyl peptidase-4 in endothelial cell homeostasis and kidney fibrosis. Kanasaki K. Diabetol Int 7 212-220 (2016)
  38. Design, Synthesis and Biological Evaluation of Imidazo[1,2-a]pyridine Derivatives as Novel DPP-4 Inhibitors. Li Q, Zhou M, Han L, Cao Q, Wang X, Zhao L, Zhou J, Zhang H. Chem Biol Drug Des 86 849-856 (2015)
  39. Hydrophobic interactions at subsite S1' of human dipeptidyl peptidase IV contribute significantly to the inhibitory effect of tripeptides. Araki M, Kanegawa N, Iwata H, Sagae Y, Ito K, Masuda K, Okuno Y. Heliyon 6 e04227 (2020)
  40. Investigation of Chlorella pyrenoidosa Protein as a Source of Novel Angiotensin I-Converting Enzyme (ACE) and Dipeptidyl Peptidase-IV (DPP-IV) Inhibitory Peptides. Li Y, Aiello G, Fassi EMA, Boschin G, Bartolomei M, Bollati C, Roda G, Arnoldi A, Grazioso G, Lammi C. Nutrients 13 1624 (2021)
  41. Novel hydrazine derivatives as selective DPP-IV inhibitors: findings from virtual screening and validation through molecular dynamics simulations. Tanwar O, Deora GS, Tanwar L, Kumar G, Janardhan S, Alam M, Shaquiquzzaman, Akhter M. J Mol Model 20 2118 (2014)
  42. SARS-CoV-2 and diabetes: A potential therapeutic effect of dipeptidyl peptidase 4 inhibitors in diabetic patients diagnosed with COVID-19. Kifle ZD, Woldeyohanin AE, Demeke CA. Metabol Open 12 100134 (2021)
  43. The Dipeptidyl Peptidase-4 Inhibitor Linagliptin Directly Enhances the Contractile Recovery of Mouse Hearts at a Concentration Equivalent to that Achieved with Standard Dosing in Humans. Batchu SN, Yerra VG, Liu Y, Advani SL, Klein T, Advani A. Int J Mol Sci 21 E5756 (2020)
  44. The contribution of Tannerella forsythia dipeptidyl aminopeptidase IV in the breakdown of collagen. Yost S, Duran-Pinedo AE. Mol Oral Microbiol 33 407-419 (2018)
  45. Design and synthesis of sulfonamide derivatives of pyrrolidine and piperidine as anti-diabetic agents. Sharma R, Soman SS. Eur J Med Chem 90 342-350 (2015)
  46. Design of potent dipeptidyl peptidase IV (DPP-4) inhibitors by employing a strategy to form a salt bridge with Lys554. Maezaki H, Tawada M, Yamashita T, Banno Y, Miyamoto Y, Yamamoto Y, Ikedo K, Kosaka T, Tsubotani S, Tani A, Asakawa T, Suzuki N, Oi S. Bioorg Med Chem Lett 27 3565-3571 (2017)
  47. Dipeptidyl peptidase-4 inhibitors and bone metabolism: is vitamin D the link? Barchetta I, Cimini FA, Bloise D, Cavallo MG. Acta Diabetol 53 839-844 (2016)
  48. Dipeptidyl peptidase-IV inhibitory action of Calebin A: An in silico and in vitro analysis. Chalichem NSS, Jupudi S, Yasam VR, Basavan D. J Ayurveda Integr Med 12 663-672 (2021)
  49. Efficacy and Safety of Switching to Teneligliptin in Patients with Type 2 Diabetes Inadequately Controlled with Dipeptidyl Peptidase-4 Inhibitors: A 12-Week Interim Report. Kim HJ, Kim YS, Lee CB, Choi MG, Chang HJ, Kim SK, Yu JM, Kim TH, Lee JH, Ahn KJ, Kim K, Lee KW. Diabetes Ther 10 1271-1282 (2019)
  50. Novel Potent and Selective DPP-4 Inhibitors: Design, Synthesis and Molecular Docking Study of Dihydropyrimidine Phthalimide Hybrids. Mourad AAE, Khodir AE, Saber S, Mourad MAE. Pharmaceuticals (Basel) 14 144 (2021)
  51. Phenolic Extracts from Extra Virgin Olive Oils Inhibit Dipeptidyl Peptidase IV Activity: In Vitro, Cellular, and In Silico Molecular Modeling Investigations. Lammi C, Bartolomei M, Bollati C, Cecchi L, Bellumori M, Sabato E, Giulio V, Mulinacci N, Arnoldi A. Antioxidants (Basel) 10 1133 (2021)
  52. Synthesis and biological evaluation of triazole based uracil derivatives as novel DPP-4 inhibitors. Li Q, Han L, Zhang B, Zhou J, Zhang H. Org Biomol Chem 14 9598-9611 (2016)
  53. A Single Second Shell Amino Acid Determines Affinity and Kinetics of Linagliptin Binding to Type 4 Dipeptidyl Peptidase and Fibroblast Activation Protein. Schnapp G, Hoevels Y, Bakker RA, Schreiner P, Klein T, Nar H. ChemMedChem 16 630-639 (2021)
  54. Design, Synthesis and Biological Evaluation of Neogliptin, a Novel 2-Azabicyclo[2.2.1]heptane-Based Inhibitor of Dipeptidyl Peptidase-4 (DPP-4). Maslov IO, Zinevich TV, Kirichenko OG, Trukhan MV, Shorshnev SV, Tuaeva NO, Gureev MA, Dahlén AD, Porozov YB, Schiöth HB, Trukhan VM. Pharmaceuticals (Basel) 15 273 (2022)
  55. Differential Effects of DPP-4 Inhibitors, Anagliptin and Sitagliptin, on PCSK9 Levels in Patients with Type 2 Diabetes Mellitus who are Receiving Statin Therapy. Furuhashi M, Sakuma I, Morimoto T, Higashiura Y, Sakai A, Matsumoto M, Sakuma M, Shimabukuro M, Nomiyama T, Arasaki O, Node K, Ueda S. J Atheroscler Thromb 29 24-37 (2022)
  56. Effect of Switching from Linagliptin to Teneligliptin Dipeptidyl Peptidase-4 Inhibitors in Older Patients with Type 2 Diabetes Mellitus. Han E, Lee M, Lee YH, Kim HS, Lee BW, Cha BS, Kang ES. Diabetes Metab Syndr Obes 13 4113-4121 (2020)
  57. Efficacy and safety of teneligliptin added to metformin in Chinese patients with type 2 diabetes mellitus inadequately controlled with metformin: A phase 3, randomized, double-blind, placebo-controlled study. Ji L, Li L, Ma J, Li X, Li D, Meng B, Lu W, Sun J, Liu Y, Takayanagi G, Wang Y. Endocrinol Diabetes Metab 4 e00222 (2021)
  58. Inhibition of Dipeptidyl Peptidase-4 by Flavonoids: Structure-Activity Relationship, Kinetics and Interaction Mechanism. Pan J, Zhang Q, Zhang C, Yang W, Liu H, Lv Z, Liu J, Jiao Z. Front Nutr 9 892426 (2022)
  59. Phase III, randomized, double-blind, placebo-controlled study to evaluate the efficacy and safety of teneligliptin monotherapy in Chinese patients with type 2 diabetes mellitus inadequately controlled with diet and exercise. Ji L, Ma J, Lu W, Liu J, Zeng J, Yang J, Li W, Zhang X, Xiao X, Takayanagi G, Wang Y. J Diabetes Investig 12 537-545 (2021)
  60. The dipeptidyl peptidase IV inhibitors vildagliptin and K-579 inhibit a phospholipase C: a case of promiscuous scaffolds in proteins. Chakraborty S, Rendón-Ramírez A, Ásgeirsson B, Dutta M, Ghosh AS, Oda M, Venkatramani R, Rao BJ, Dandekar AM, Goñi FM. F1000Res 2 286 (2013)
  61. Application of a Combined Peptidomics and In Silico Approach for the Identification of Novel Dipeptidyl Peptidase-IV-Inhibitory Peptides in In Vitro Digested Pinto Bean Protein Extract. Martini S, Cattivelli A, Conte A, Tagliazucchi D. Curr Issues Mol Biol 44 139-151 (2021)
  62. DOCLASP - Docking ligands to target proteins using spatial and electrostatic congruence extracted from a known holoenzyme and applying simple geometrical transformations. Chakraborty S. F1000Res 3 262 (2014)
  63. Efficacy and Safety of Novel Dipeptidyl-Peptidase-4 Inhibitor Evogliptin in the Management of Type 2 Diabetes Mellitus: A Meta-Analysis. Dutta D, Bhattacharya S, Krishnamurthy A, Sharma LK, Sharma M. Indian J Endocrinol Metab 24 434-445 (2020)
  64. Efficacy and Safety of Switching to Teneligliptin in Patients with Type 2 Diabetes Inadequately Controlled with Dipeptidyl Peptidase-4 Inhibitors: 52-Week Results from a Prospective Observational Study. Kim HJ, Kim YS, Lee CB, Choi MG, Chang HJ, Kim SK, Yu JM, Kim TH, Lee JH, Ahn KJ, Min KW, Kyung EJ, Kim YK, Lee KW. Diabetes Ther 12 2907-2920 (2021)
  65. Inhibitory activity of xanthoangelol isolated from Ashitaba (Angelica keiskei Koidzumi) towards α-glucosidase and dipeptidyl peptidase-IV: in silico and in vitro studies. Aulifa DL, Adnyana IK, Sukrasno S, Levita J. Heliyon 8 e09501 (2022)
  66. Structural insights of dipeptidyl peptidase-IV inhibitors through molecular dynamics-guided receptor-dependent 4D-QSAR studies. Patil RB, Barbosa EG, Sangshetti JN, Zambre VP, Sawant SD. Mol Divers 22 575-583 (2018)
  67. Teneligliptin, a Chemotype Prolyl-Thiazolidine-Based Novel Dipeptidyl Peptidase-4 Inhibitor with Insulin Sensitizing Properties. Kutoh E, Wada A, Terayama S. Clin Drug Investig 36 809-818 (2016)
  68. Chemoproteomic identification of a DPP4 homolog in Bacteroides thetaiotaomicron. Keller LJ, Nguyen TH, Liu LJ, Hurysz BM, Lakemeyer M, Guerra M, Gelsinger DJ, Chanin R, Ngo N, Lum KM, Faucher F, Ipock P, Niphakis MJ, Bhatt AS, O'Donoghue AJ, Huang KC, Bogyo M. Nat Chem Biol (2023)
  69. Discovery of imeglimin-inspired novel 1,3,5-triazine derivatives as antidiabetic agents in streptozotocin-induced diabetes in Wistar rats via inhibition of DPP-4. Gupta A, Bhat HR, Singh UP. RSC Med Chem 14 1512-1536 (2023)
  70. Efficacy of omarigliptin, once-weekly dipeptidyl peptidase-4 inhibitor, in patients with type 2 diabetes. Kawasaki E, Nakano Y, Fukuyama T, Uchida A, Sagara Y, Tamai H, Tojikubo M, Hiromatsu Y, Koga N. World J Diabetes 12 2087-2095 (2021)
  71. Molecular Characterization and Functional Analysis of the Dipeptidyl Peptidase IV from Venom of the Ectoparasitoid Scleroderma guani. Wu C, Yang C, Wang Y, Wang J, Zhu J. Toxins (Basel) 15 311 (2023)
  72. Novel hit of DPP-4Is as promising antihyperglycemic agents with dual antioxidant/anti-inflammatory effects for type 2 diabetes with/without COVID-19. Mahgoub S, Fatahala SS, Sayed AI, Atya HB, El-Shehry MF, Afifi H, Awad SM, El-Hameed RHA, Taha H. Bioorg Chem 128 106092 (2022)
  73. Protection against Oxidative Stress and Metabolic Alterations by Synthetic Peptides Derived from Erythrina edulis Seed Protein. Rodríguez-Arana N, Jiménez-Aliaga K, Intiquilla A, León JA, Flores E, Zavaleta AI, Izaguirre V, Solis-Calero C, Hernández-Ledesma B. Antioxidants (Basel) 11 2101 (2022)
  74. Repurposing of existing antibiotics for the treatment of diabetes mellitus. Alam MS, Uddin MS, Shamsuddin T, Rubayed M, Sharmin T, Akter R, Hosen SMZ. In Silico Pharmacol 10 4 (2022)
  75. Teneligliptin Real-World Effectiveness Assessment in Patients with Type 2 Diabetes Mellitus in India: A Retrospective Analysis (TREAT-INDIA 2). Ghosh S, Tiwaskar M, Chawla R, Jaggi S, Asirvatham A, Panikar V. Diabetes Ther 11 2257-2268 (2020)
  76. Therapeutic Effects of Switching to Anagliptin from Other DPP-4 Inhibitors in T2DM Patients with Inadequate Glycemic Control: A Non-interventional, Single-Arm, Open-Label, Multicenter Observational Study. Kim SY, Kim S. Diabetes Ther 14 109-121 (2023)


Quick links