Literature for peptidase A22.001: presenilin 1

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

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

2026

Martin-Hidalgo,D., Macias-Garcia,B. and Gonzalez-Fernandez,L.
Presenilin-1 is present in boar spermatozoa and regulates acrosome reaction in the absence of glucose
Theriogenology (2026) 251, 117710-117710. PubMed Europe PubMed DOI

2025

Chui,D.H., Tanahashi,H., Ozawa,K., Ikeda,S., Checler,F., Ueda,O., Suzuki,H., Araki,W., Inoue,H., Shirotani,K., Takahashi,K., Gallyas,F. and Tabira,T.
Editorial Expression of Concern: Transgenic mice with Alzheimer presenilin 1 mutations show accelerated neurodegeneration without amyloid plaque formation
Nat Med (2025) 31, 2821-2821. PubMed Europe PubMed DOI
Fremlen,H. and Burmann,B.M.
Maintaining the Integral Membrane Proteome: Revisiting the Functional Repertoire of Integral Membrane Proteases
Chembiochem (2025) , e202500048-e202500048. PubMed Europe PubMed DOI V
Liu,H., Marsh,T.W., Shi,X., Renton,A.E., Bowling,K.M., Ziegemeier,E., Wang,G., Cao,Y., Aristel,A., Li,J., Dickson,A., Perrin,R.J., Goate,A.M., Fernandez,V., Day,G.S., Doering,M., Daniels,A., Gordon,B.A., Benzinger,T.L.S., Hassenstab,J., Ibanez,L., Supnet-Bell,C., Xiong,C., Allegri,R., Berman,S.B., Fox,N.C., Ryan,N., Huey,E.D., Voglein,J., Noble,J.M., Roh,J.H., Jucker,M., Laske,C., Ikeuchi,T., Sanchez-Valle,R., Schofield,P.R., Chrem Mendez,P., Chhatwal,J.P., Farlow,M., Lee,J.H., Levey,A.I., Levin,J., Lopera,F., Martins,R., Niimi,Y., Rosa-Neto,P., Morris,J.C., Bateman,R.J., Karch,C.M., Cruchaga,C., McDade,E. and Llibre-Guerra,J.J.
The landscape of autosomal-dominant Alzheimer's disease: global distribution and age of onset
Brain (2025) PubMed Europe PubMed DOI
Moon,O.R., Newman,A.C., Alanazi,A.S., Wehenkel,S.C., Gawel-Beben,K., Ivetic,A., Price,D.A., Knauper,V. and Ager,A.
TCR activation stimulates regulated intramembrane proteolysis of L-selectin by presenilin 1 and localized proteasomal degradation of the cytoplasmic tail
J Biol Chem (2025) 301, 110473-110473. PubMed Europe PubMed DOI
Nadendla,S. and Mohiuddin,S.S.
Biochemistry, Presenilin
(2025) PubMed Europe PubMed
Nagarajan,V., Libowitz,C.L., Ackley,B.D. and Wolfe,M.S.
A C. elegans model of familial Alzheimer's disease shows age-dependent synaptic degeneration independent of amyloid beta-peptide
bioRxiv (2025) PubMed Europe PubMed DOI PMC EPMC

2024

Acosta-Uribe,J., Villegas-Lanau,A., Vallejo,D., Ramirez-Aguilar,L., Solano,J.M., Mejia-Cupajita,B., Aguillon,D., Moreno,S., Mendez,L.G., Baena,A., Madrigal,L., Bocanegra,Y., Quiroz,Y.T., Garcia,G.P., Vasquez,D., Arbelaez,A., Lopera,F., Beach,T.G., Kosik,K.S., White,C.L., III and Giraldo-Chica,M.
Primary lateral sclerosis associated with PSEN1 Pro284Leu variant in a Colombian family: Clinical and neuropathological features
Alzheimers Dement (2024) 20, 6384-6394. PubMed Europe PubMed DOI
Arafi,P., Devkota,S., Maesako,M. and Wolfe,M.S.
Alzheimer-mutant gamma-secretase complexes stall amyloid beta-peptide production
bioRxiv (2024) PubMed Europe PubMed DOI PMC EPMC
Colijn,M.A. and Ismail,Z.
Presenilin Gene Mutation-associated Psychosis: Phenotypic Characteristics and Clinical Implications
Alzheimer Dis Assoc Disord (2024) 38, 101-106. PubMed Europe PubMed DOI V
Deng,C., Cai,Q., Zhang,J., Chang,K., Peng,T., Liu,X., Cao,F., Yan,X., Cheng,J., Wang,X., Tan,Y. and Hua,Q.
Generation and Characterization of a Novel Knockin Mouse Model Expressing PSEN1 D385A: Implications for Investigating Herbal Drug Effects in gamma-Secretase Activity
J Alzheimers Dis (2024) PubMed Europe PubMed DOI
Perrin,F., Sinha,P., Mitchell,S.P.C., Sadek,M., Maesako,M. and Berezovska,O.
Identification of PS1/gamma-secretase and glutamate transporter GLT-1 interaction sites
J Biol Chem (2024) 300, 107172-107172. PubMed Europe PubMed DOI PMC EPMC
Perrin,F., Anderson,L.C., Mitchell,S.P.C., Sinha,P., Turchyna,Y., Maesako,M., Houser,M.C.Q., Zhang,C., Wagner,S.L., Tanzi,R.E. and Berezovska,O.
PS1/gamma-secretase acts as rogue chaperone of glutamate transporter EAAT2/GLT-1 in Alzheimer's disease
Acta Neuropathol Commun (2024) 12, 166-166. PubMed Europe PubMed DOI PMC EPMC
Yan,K., Zhang,C., Kang,J., Montenegro,P. and Shen,J.
Cortical neurodegeneration caused by Psen1 mutations is independent of Abeta
Proc Natl Acad Sci U S A (2024) 121, e2409343121-e2409343121. PubMed Europe PubMed DOI

2023

Avramouli,A., Krokidis,M.G., Exarchos,T.P. and Vlamos,P.
Protein Structure Prediction for Disease-Related Insertions/Deletions in Presenilin 1 Gene
Adv Exp Med Biol (2023) 1423, 31-40. PubMed Europe PubMed DOI
Kurth,V., Ogorek,I., Munch,C., Lopez-Rios,J., Ousson,S., Lehmann,S., Nieweg,K., Roebroek,A.J.M., Pietrzik,C.U., Beher,D. and Weggen,S.
Pathogenic Abeta production by heterozygous PSEN1 mutations is intrinsic to the mutant protein and not mediated by conformational hindrance of wild-type PSEN1
J Biol Chem (2023) 299, 104997-104997. PubMed Europe PubMed DOI PMC EPMC
Makarov,M., Kushnireva,L., Papa,M. and Korkotian,E.
Presenilins and mitochondria-an intriguing link: mini-review
Front Neurosci (2023) 17, 1249815-1249815. PubMed Europe PubMed DOI PMC EPMC V
Schultz,S.A., Shirzadi,Z., Schultz,A.P., Liu,L., Fitzpatrick,C.D., McDade,E., Barthelemy,N.R., Renton,A., Esposito,B., Joseph-Mathurin,N., Cruchaga,C., Chen,C.D., Goate,A., Allegri,R.F., Benzinger,T.L.S., Berman,S., Chui,H.C., Fagan,A.M., Farlow,M.R., Fox,N.C., Gordon,B.A., Day,G.S., Graff-Radford,N.R., Hassenstab,J.J., Hanseeuw,B.J., Hofmann,A., Jack,C.R., Jr., Jucker,M., Karch,C.M., Koeppe,R.A., Lee,J.H., Levey,A.I., Levin,J., Martins,R.N., Mori,H., Morris,J.C., Noble,J., Perrin,R.J., Rosa-Neto,P., Salloway,S.P., Sanchez-Valle,R., Schofield,P.R., Xiong,C., Johnson,K.A., Bateman,R.J., Sperling,R.A. and Chhatwal,J.P.
Location of pathogenic variants in PSEN1 impacts progression of cognitive, clinical, and neurodegenerative measures in autosomal-dominant Alzheimer's disease
Aging Cell (2023) 22, e13871-e13871. PubMed Europe PubMed DOI PMC EPMC
Serneels,L., Narlawar,R., Perez-Benito,L., Municoy,M., Guallar,V., T'Syen,D., Dewilde,M., Bischoff,F., Fraiponts,E., Tresadern,G., Roevens,P.W.M., Gijsen,H.J.M. and De Strooper,B.
Selective inhibitors of the PSEN1-gamma-secretase complex
J Biol Chem (2023) 299, 104794-104794. PubMed Europe PubMed DOI PMC EPMC
Wu,Y., Thomas,G.M., Thomsen,M., Bahri,S. and Lieberman,R.L.
Lipid environment modulates processivity and kinetics of a presenilin homolog acting on multiple substrates in vitro
J Biol Chem (2023) 299, 105401-105401. PubMed Europe PubMed DOI PMC EPMC
Yang,Y., Bagyinszky,E. and An,S.S.A.
Presenilin-1 (PSEN1) Mutations: Clinical Phenotypes beyond Alzheimer's Disease
Int J Mol Sci (2023) 24 PubMed Europe PubMed DOI PMC EPMC

2022

Gamez-Belmonte,R., Mahapatro,M., Erkert,L., Gonzalez-Acera,M., Naschberger,E., Yu,Y., Tena-Garitaonaindia,M., Patankar,J.V., Wagner,Y., Podstawa,E., Schodel,L., Bubeck,M., Neurath,M.F., Sturzl,M. and Becker,C.
Epithelial presenilin-1 drives colorectal tumour growth by controlling EGFR-COX2 signalling
Gut (2022) PubMed Europe PubMed DOI
Guo,X., Wang,Y., Zhou,J., Jin,C., Wang,J., Jia,B., Jing,D., Yan,C., Lei,J., Zhou,R. and Shi,Y.
Molecular basis for isoform-selective inhibition of presenilin-1 by MRK-560
Nat Commun (2022) 13, 6299-6299. PubMed Europe PubMed DOI PMC EPMC I
Zhu,W., Zhou,Y., Wang,Q., Li,J., Chu,S., Jin,W., Mao,C., Dong,L., Gao,J. and Xu,Q.
Generation of a human induced pluripotent stem cell (iPSC) line from skin fibroblasts of a patient carrying an E363Q mutation in PSEN1 gene
Stem Cell Res (2022) 61, 102769-102769. PubMed Europe PubMed DOI

2021

Asada-Utsugi,M., Uemura,K., Kubota,M., Noda,Y., Tashiro,Y., Uemura,T.M., Yamakado,H., Urushitani,M., Takahashi,R., Hattori,S., Miyakawa,T., Ageta-Ishihara,N., Kobayashi,K., Kinoshita,M. and Kinoshita,A.
Mice with cleavage-resistant N-cadherin exhibit synapse anomaly in the hippocampus and outperformance in spatial learning tasks
Mol Brain (2021) 14, 23-23. PubMed Europe PubMed DOI PMC EPMC
Bustos,V., Pulina,M.V. and Ledo,J.
Amyloidogenic and anti-amyloidogenic properties of presenilin 1
Adv Pharmacol (2021) 90, 239-251. PubMed Europe PubMed DOI
Cai,T. and Tomita,T.
Sequential conformational changes in transmembrane domains of presenilin 1 in Abeta42 downregulation
J Biochem (2021) PubMed Europe PubMed DOI
Joshi,P., Gardner,M., Lintott,C. and Anderson,T.
Novel Presenilin-1 Mutation (Ala275Ser) Associated With Clinical Features of Dementia With Lewy Bodies
Alzheimer Dis Assoc Disord (2021) PubMed Europe PubMed DOI V
Liu,L., Lauro,B.M., Wolfe,M.S. and Selkoe,D.J.
Hydrophilic loop 1 of Presenilin-1 and the APP GxxxG transmembrane motif regulate gamma-secretase function in generating Alzheimer-causing Abeta peptides
J Biol Chem (2021) , 100393-100393. PubMed Europe PubMed DOI
Yang,G., Zhou,R., Guo,X., Yan,C., Lei,J. and Shi,Y.
Structural basis of gamma-secretase inhibition and modulation by small molecule drugs
Cell (2021) 184, 521-533. PubMed Europe PubMed DOI I

2020

Barman,N.C., Khan,N.M., Islam,M., Nain,Z., Roy,R.K., Haque,A. and Barman,S.K.
CRISPR-Cas9: A Promising Genome Editing Therapeutic Tool for Alzheimer's Disease-A Narrative Review
Neurol Ther (2020) 9, 419-434. PubMed Europe PubMed DOI V
Cai,T. and Tomita,T.
Structure-activity relationship of presenilin in gamma-secretase-mediated intramembrane cleavage
Semin Cell Dev Biol (2020) PubMed Europe PubMed DOI
Cai,T., Hatano,A., Kanatsu,K. and Tomita,T.
Histidine 131 in presenilin 1 is the pH-sensitive residue that causes the increase in Abeta42 level in acidic pH
J Biochem (2020) 167, 463-471. PubMed Europe PubMed DOI
Contino,S., Suelves,N., Vrancx,C., Vadukul,D.M., Payen,V.L., Stanga,S., Bertrand,L. and Kienlen-Campard,P.
Presenilin-Deficient Neurons and Astrocytes Display Normal Mitochondrial Phenotypes
Front Neurosci (2020) 14, 586108-586108. PubMed Europe PubMed DOI PMC EPMC K
Dehury,B., Somavarapu,A.K. and Kepp,K.P.
A computer-simulated mechanism of familial Alzheimer's disease: Mutations enhance thermal dynamics and favor looser substrate-binding to gamma-secretase
J Struct Biol (2020) 212, 107648-107648. PubMed Europe PubMed DOI
Escamilla-Ayala,A., Wouters,R., Sannerud,R. and Annaert,W.
Contribution of the presenilins in the cell biology, structure and function of gamma-secretase
Semin Cell Dev Biol (2020) PubMed Europe PubMed DOI
Escamilla-Ayala,A.A., Sannerud,R., Mondin,M., Poersch,K., Vermeire,W., Paparelli,L., Berlage,C., Koenig,M., Chavez-Gutierrez,L., Ulbrich,M.H., Munck,S., Mizuno,H. and Annaert,W.
Super-resolution microscopy reveals majorly mono- and dimeric presenilin1/gamma-secretase at the cell surface
elife (2020) 9 PubMed Europe PubMed DOI PMC EPMC
Fan,C., Huang,X., Song,H. and Jia,J.
Presenilin 1 intronic polymorphism in sporadic Alzheimer's disease in a Northern Chinese population
Neuroreport (2020) 31, 37-40. PubMed Europe PubMed DOI M
Fray,S., Rassas,A., Messaoud,T. and Belal,S.
Refractory epilepsy in PSEN 1 mutation (I83T)
Neurocase (2020) 26, 167-170. PubMed Europe PubMed DOI M
Gu,X., Zhao,M., Han,X. and Liu,L.
Presenilin-1 mutation is associated with a hippocampus defect in Alzheimer's disease: meta-analysis for neuroimaging research
Clin Neurol Neurosurg (2020) 191, 105679-105679. PubMed Europe PubMed DOI M
Jiang,H., Pederson,S.M., Newman,M., Dong,Y., Barthelson,K. and Lardelli,M.
Transcriptome analysis indicates dominant effects on ribosome and mitochondrial function of a premature termination codon mutation in the zebrafish gene psen2
PLoS ONE (2020) 15, e0232559-e0232559. PubMed Europe PubMed DOI PMC EPMC
Kabir,M.T., Uddin,M.S., Setu,J.R., Ashraf,G.M., Bin-Jumah,M.N. and Abdel-Daim,M.M.
Exploring the Role of PSEN Mutations in the Pathogenesis of Alzheimer's Disease
Neurotox Res (2020) PubMed Europe PubMed DOI
Mehra,R. and Kepp,K.P.
Identification of structural calcium binding sites in membrane-bound presenilin 1 and 2
J Phys Chem B (2020) PubMed Europe PubMed DOI
Mengel,D., Liu,L., Yamamoto,R., Zulow,S., Deuschl,C., Hermann,D.M., Zerr,I., Selkoe,D.J. and Dodel,R.
A novel V272D presenilin mutation associated with logopenia, disorientation, and apraxia in an autosomal-dominant Alzheimer's disease family
Neurobiol Aging (2020) 85, e5-e154. PubMed Europe PubMed DOI M
Norton,D.J., Parra,M.A., Sperling,R.A., Baena,A., Guzman-Velez,E., Jin,D.S., Andrea,N., Khang,J., Schultz,A., Rentz,D.M., Pardilla-Delgado,E., Fuller,J., Johnson,K., Reiman,E.M., Lopera,F. and Quiroz,Y.T.
Visual short-term memory relates to tau and amyloid burdens in preclinical autosomal dominant Alzheimer's disease
Alzheimers Res Ther (2020) 12, 99-99. PubMed Europe PubMed DOI PMC EPMC
Oakley,D.H., Chung,M., Klickstein,N., Commins,C., Hyman,B.T. and Frosch,M.P.
The Alzheimer disease-causing presenilin-1 L435F mutation causes increased production of soluble Abeta43 species in patient-derived iPSC-neurons, closely mimicking matched patient brain tissue
J Neuropathol Exp Neurol (2020) 79, 592-604. PubMed Europe PubMed DOI M
Piaceri,I., Chiari,A., Galli,C., Bagnoli,S., Ferrari,C., Saavedra,S.T., Molinari,M.A., Vinceti,G., Sorbi,S. and Nacmias,B.
Incomplete penetrance in familial Alzheimer's disease with PSEN1 Ala260Gly mutation
Neurol Sci (2020) PubMed Europe PubMed DOI M
Pimenova,A.A. and Goate,A.M.
Novel presenilin 1 and 2 double knock-out cell line for in vitro validation of PSEN1 and PSEN2 mutations
Neurobiol Dis (2020) 138, 104785-104785. PubMed Europe PubMed DOI K
Qiu,Q., Jia,L., Wang,Q., Zhao,L., Jin,H., Li,T., Quan,M., Xu,L., Li,B., Li,Y. and Jia,J.
Identification of a novel PSEN1 Gly111Val missense mutation in a Chinese pedigree with early-onset Alzheimer's disease
Neurobiol Aging (2020) 85, e1-e155. PubMed Europe PubMed DOI M
Santos-Mandujano,R.A., Ryan,N.S., Chavez-Gutierrez,L., Sanchez-Torres,C. and Meraz-Rios,M.A.
Clinical association of white matter hyperintensities localization in a Mexican family with spastic paraparesis carrying the PSEN1 A431E mutation
J Alzheimers Dis (2020) 73, 1075-1083. PubMed Europe PubMed DOI M
Schrank,S., McDaid,J., Briggs,C.A., Mustaly-Kalimi,S., Brinks,D., Houcek,A., Singer,O., Bottero,V., Marr,R.A. and Stutzmann,G.E.
Human-induced neurons from presenilin 1 mutant patients model aspects of Alzheimer's disease pathology
Int J Mol Sci (2020) 21 PubMed Europe PubMed DOI M
Soto-Mercado,V., Mendivil-Perez,M., Velez-Pardo,C., Lopera,F. and Jimenez-Del-Rio,M.
Cholinergic-like neurons carrying PSEN1 E280A mutation from familial Alzheimer's disease reveal intraneuronal sAPPbeta fragments accumulation, hyperphosphorylation of TAU, oxidative stress, apoptosis and Ca2+ dysregulation: therapeutic implications
PLoS ONE (2020) 15, e0221669-e0221669. PubMed Europe PubMed DOI M
Wang,C.Y., Zhang,Q., Xun,Z., Yuan,L., Li,R., Li,X., Tian,S.Y., Xin,N. and Xu,Y.
Increases of iASPP-Keap1 interaction mediated by syringin enhance synaptic plasticity and rescue cognitive impairments via stabilizing Nrf2 in Alzheimer's models
Redox Biol (2020) 36, 101672-101672. PubMed Europe PubMed DOI PMC EPMC
Wang,Y., Yang,J.Q., Hong,T.T., Sun,Y.H., Huang,H.L., Chen,F., Chen,X.J., Chen,H.Y., Dong,S.S., Cui,L.L. and Yang,T.L.
RTN4B-mediated suppression of Sirtuin 2 activity ameliorates beta-amyloid pathology and cognitive impairment in Alzheimer's disease mouse model
Aging Cell (2020) , e13194-e13194. PubMed Europe PubMed DOI
Wong,T.H., Seelaar,H., Melhem,S., Rozemuller,A.J.M. and van Swieten,J.C.
Genetic screening in early-onset Alzheimer's disease identified three novel presenilin mutations
Neurobiol Aging (2020) 86, e9-e201. PubMed Europe PubMed DOI M
You,C., Zeng,W., Deng,L., Lei,Z., Gao,X., Zhang,V.W. and Wang,Y.
Identification and clinical analysis of the first nonsense mutation in the PSEN1 gene in a family with acute encephalopathy and retinitis pigmentosa
Front Neurol (2020) 11, 319-319. PubMed Europe PubMed DOI PMC EPMC M

2019

Selective gamma-secretase inhibition is a potential target for leukemias
Cancer Discov (2019) 9, OF15-OF15. PubMed Europe PubMed DOI I
Aathi,M. and Piramanayagam,S.
From EST to structure models for functional inference of APP, BACE1, PSEN1, PSEN2 genes
Bioinformation (2019) 15, 760-771. PubMed Europe PubMed DOI PMC EPMC I
Arber,C., Villegas-Llerena,C., Toombs,J., Pocock,J.M., Ryan,N.S., Fox,N.C., Zetterberg,H., Hardy,J. and Wray,S.
Amyloid precursor protein processing in human neurons with an allelic series of the PSEN1 intron 4 deletion mutation and total presenilin-1 knockout
Brain Commun (2019) 1, fcz024-fcz024. PubMed Europe PubMed DOI PMC EPMC M
Artuso,V., Benussi,L., Ghidoni,R., Moradi-Bachiller,S., Fusco,F., Curtolo,S., Roiter,I., Forloni,G. and Albani,D.
Asymptomatic carriers of presenilin-1 E318G variant show no cerebrospinal fluid biochemical signs suggestive of Alzheimer's disease in a family with late-onset dementia
Curr Alzheimer Res (2019) 16, 1-7. PubMed Europe PubMed DOI M
Auboyer,L., Monzo,C., Wallon,D., Rovelet-Lecrux,A., Gabelle,A., Gazagne,I., Cacheux,V., Lehmann,S. and Crozet,C.
Generation of induced pluripotent stem cells (IRMBi001-A) from an Alzheimer's disease patient carrying a G217D mutation in the PSEN1 gene
Stem Cell Res (2019) 34, 101381-101381. PubMed Europe PubMed DOI M
Blanco,J.A., Alonso,A., Blanco,J., Rojo,E., Telleria,J.J., Torres,M.A. and Uribe,F.
Novel presenilin 1 mutation (p.Thr-Pro116-117Ser-Thr) in a Spanish family with early-onset Alzheimer's disease
Neurobiol Aging (2019) 84, e19-e238. PubMed Europe PubMed DOI M
Cai,T., Morishima,K., Takagi-Niidome,S., Tominaga,A. and Tomita,T.
Conformational dynamics of transmembrane domain 3 of presenilin 1 is associated with the trimming activity of gamma-secretase
J Neurosci (2019) 39, 8600-8610. PubMed Europe PubMed DOI
Chavez-Garcia,C., Aguayo-Ortiz,R. and Dominguez,L.
Quantifying correlations between mutational sites in the catalytic subunit of gamma-secretase
J Mol Graph Model (2019) 88, 221-227. PubMed Europe PubMed DOI M
Cho,Y.Y., Kwon,O.H., Park,M.K., Kim,T.W. and Chung,S.
Elevated cellular cholesterol in familial Alzheimer's presenilin 1 mutation is associated with lipid raft localization of beta-amyloid precursor protein
PLoS ONE (2019) 14, e0210535-e0210535. PubMed Europe PubMed DOI M
Diaz-Guerra,E., Oria-Muriel,M.A., Moreno-Jimenez,E.P., de Rojasb,I., Rodriguez,C., Rodriguez-Traver,E., Orera,M., Hernandezb,I., Ruizb,A. and Vicario,C.
Generation of an integration-free iPSC line, ICCSICi006-A, derived from a male Alzheimer's disease patient carrying the PSEN1-G206D mutation
Stem Cell Res (2019) 40, 101574-101574. PubMed Europe PubMed DOI M
Gao,Y., Ren,R.J., Zhong,Z.L., Dammer,E., Zhao,Q.H., Shan,S., Zhou,Z., Li,X., Zhang,Y.Q., Cui,H.L., Hu,Y.B., Chen,S.D., Chen,J.J., Guo,Q.H. and Wang,G.
Mutation profile of APP, PSEN1, and PSEN2 in Chinese familial Alzheimer's disease
Neurobiol Aging (2019) 77, 154-157. PubMed Europe PubMed DOI M
Giau,V.V., Bagyinszky,E., Yang,Y.S., Youn,Y.C., An,S.S.A. and Kim,S.Y.
Genetic analyses of early-onset Alzheimer's disease using next generation sequencing
Sci Rep (2019) 9, 8368-8368. PubMed Europe PubMed DOI PMC EPMC M
Guven,G., Erginel-Unaltuna,N., Samanci,B., Gulec,C., Hanagasi,H. and Bilgic,B.
A patient with early-onset Alzheimer's disease with a novel PSEN1 p.Leu424Pro mutation
Neurobiol Aging (2019) 84, e1-e238. PubMed Europe PubMed DOI M
Hitzenberger,M. and Zacharias,M.
Structural modeling of gamma-secretase Abetan complex formation and substrate processing
ACS Chem Neurosci (2019) 10, 1826-1840. PubMed Europe PubMed DOI
Imai,S., Cai,T., Yoshida,C., Tomita,T. and Futai,E.
Specific mutations in presenilin 1 cause conformational changes in gamma-secretase to modulate amyloid beta trimming
J Biochem (2019) 165, 37-46. PubMed Europe PubMed DOI M
Jo,H., Kim,M., Park,S., Park,J.E., Cho,S.H., Kim,S.J., Jang,H., Jung,Y.H., Kim,J., Na,D.L., Seo,S.W., Cho,J.W. and Kim,H.J.
Dopa responsive Parkinsonism in an early onset Alzheimer's disease patient with a presenilin 1 mutation (A434T)
J Alzheimers Dis (2019) 71, 7-13. PubMed Europe PubMed DOI M
Kounnas,M.Z., Durakoglugil,M.S., Herz,J. and Comer,W.T.
NGP 555, a gamma-secretase modulator, shows a beneficial shift in the ratio of amyloid biomarkers in human cerebrospinal fluid at safe doses
Alzheimers Dement (N Y) (2019) 5, 458-467. PubMed Europe PubMed DOI PMC EPMC
Li,Y.S., Yang,Z.H., Zhang,Y., Yang,J., Shang,D.D., Zhang,S.Y., Wu,J., Ji,Y., Zhao,L., Shi,C.H. and Xu,Y.M.
Two novel mutations and a de novo mutation in PSEN1 in early-onset Alzheimer's disease
Aging Dis (2019) 10, 908-914. PubMed Europe PubMed DOI PMC EPMC M
Liu,L., Ding,L., Rovere,M., Wolfe,M.S. and Selkoe,D.J.
A cellular complex of BACE1 and gamma-secretase sequentially generates Abeta from its full-length precursor
J Cell Biol (2019) 218, 644-663. PubMed Europe PubMed DOI
Lopez-Garcia,S., Jimenez-Bonilla,J., Lopez Delgado,A., Orizaola Balaguer,P., Infante Ceberio,J., Banzo Marraco,I., Rodriguez Rodriguez,E. and Sanchez-Juan,P.
A rare PSEN1 (Leu85Pro) mutation causing Alzheimer's disease in a 29-year-old woman presenting as corticobasal syndrome
J Alzheimers Dis (2019) 70, 655-658. PubMed Europe PubMed DOI M
Miki,T., Yokota,O., Haraguchi,T., Ikeuchi,T., Zhu,B., Takenoshita,S., Terada,S. and Yamada,N.
Young adult-onset, very slowly progressive cognitive decline with spastic paraparesis in Alzheimer's disease with cotton wool plaques due to a novel presenilin1 G417S mutation
Acta Neuropathol Commun (2019) 7, 19-19. PubMed Europe PubMed DOI PMC EPMC M
Monacelli,F., Martella,L., Parodi,M.N., Odetti,P., Fanelli,F. and Tabaton,M.
Frontal variant of Alzheimer's disease: a report of a novel PSEN1 mutation
J Alzheimers Dis (2019) 70, 11-15. PubMed Europe PubMed DOI M
Newman,M., Hin,N., Pederson,S. and Lardelli,M.
Brain transcriptome analysis of a familial Alzheimer's disease-like mutation in the zebrafish presenilin 1 gene implies effects on energy production
Mol Brain (2019) 12, 43-43. PubMed Europe PubMed DOI PMC EPMC K M
Oikawa,N. and Walter,J.
Presenilins and gamma-secretase in membrane proteostasis
Cells (2019) 8 PubMed Europe PubMed DOI
Qiu,Q., Shen,L., Jia,L., Wang,Q., Li,F., Li,Y. and Jia,J.
A novel PSEN1 M139L mutation found in a Chinese pedigree with early-onset Alzheimer's disease increases Abeta42/Abeta40 ratio
J Alzheimers Dis (2019) 69, 199-212. PubMed Europe PubMed DOI M
Ramirez Aguilar,L., Acosta-Uribe,J., Giraldo,M.M., Moreno,S., Baena,A., Alzate,D., Cuastumal,R., Aguillon,D., Madrigal,L., Saldarriaga,A., Navarro,A., Garcia,G.P., Aguirre-Acevedo,D.C., Geier,E.G., Cochran,J.N., Quiroz,Y.T., Myers,R.M., Yokoyama,J.S., Kosik,K.S. and Lopera,F.
Genetic origin of a large family with a novel PSEN1 mutation (Ile416Thr)
Alzheimers Dement (2019) 15, 709-719. PubMed Europe PubMed DOI M
Shen,L., Qin,W., Wu,L., Zhou,A., Tang,Y., Wang,Q., Jia,L. and Jia,J.
Two novel presenilin-1 mutations (I249L and P433S) in early onset Chinese Alzheimer's pedigrees and their functional characterization
Biochem Biophys Res Commun (2019) 516, 264-269. PubMed Europe PubMed DOI M
Tang,N., Dehury,B. and Kepp,K.P.
Computing the pathogenicity of Alzheimer's disease presenilin 1 mutations
J Chem Inf Model (2019) 59, 858-870. PubMed Europe PubMed DOI M
Vallejo-Diez,S., Fleischer,A., Martin-Fernandez,J.M., Sanchez-Gilabert,A., Castresana,M., Aguillon,D., Villegas,A., Mastronardi,C.A., Espinosa,L.G., Arcos-Burgos,M., Del Pozo,A., Herran,E., Gainza,E., Isaza-Ruget,M., Lopera,F. and Bachiller,D.
Generation of one iPSC line (IMEDEAi006-A) from an early-onset familial Alzheimer's Disease (fAD) patient carrying the E280A mutation in the PSEN1 gene
Stem Cell Res (2019) 37, 101440-101440. PubMed Europe PubMed DOI M
Van Giau,V., Pyun,J.M., Suh,J., Bagyinszky,E., An,S.S.A. and Kim,S.Y.
A pathogenic PSEN1 Trp165Cys mutation associated with early-onset Alzheimer's disease
BMC Neurol (2019) 19, 188-188. PubMed Europe PubMed DOI PMC EPMC M
Villalba,A.C., Garcia,J., Ramos,C., Cuastumal,A.R., Aguillon,D., Aguirre-Acevedo,D.C., Madrigal,L. and Lopera,F.
Mental disorders in young adults from families with the presenilin-1 gene mutation E280A in the preclinical stage of Alzheimer's disease
J Alzheimers Dis (2019) PubMed Europe PubMed DOI M
Voglein,J., Willem,M., Trambauer,J., Schonecker,S., Dieterich,M., Biskup,S., Giudici,C., Utz,K., Oberstein,T., Brendel,M., Rominger,A., Danek,A., Steiner,H., Haass,C. and Levin,J.
Identification of a rare presenilin 1 single amino acid deletion mutation (F175del) with unusual amyloid-beta processing effects
Neurobiol Aging (2019) 84, e5-e241. PubMed Europe PubMed DOI M
Wang,H., Sun,R., Shi,Y., Xia,M., Zhao,J., Yang,M., Ma,L., Sun,Y., Li,G., Zhang,H., Qin,W. and Zhang,J.
Probable novel PSEN1 Gln222Leu mutation in a Chinese family with early-onset Alzheimer's disease
Curr Alzheimer Res (2019) 16, 764-769. PubMed Europe PubMed DOI M
Wolfe,M.S.
Dysfunctional gamma-Secretase in Familial Alzheimer's Disease
Neurochem Res (2019) 44, 5-11. PubMed Europe PubMed DOI M
Wu,S., Song,W., Wong,C.C.L. and Shi,Y.
Bax inhibitor 1 is a gamma-secretase-independent presenilin-binding protein
Proc Natl Acad Sci U S A (2019) 116, 141-147. PubMed Europe PubMed DOI M
Yang,G., Zhou,R., Zhou,Q., Guo,X., Yan,C., Ke,M., Lei,J. and Shi,Y.
Structural basis of Notch recognition by human gamma-secretase
Nature (2019) 565, 192-197. PubMed Europe PubMed DOI S

2018

Aguayo-Ortiz,R. and Dominguez,L.
Simulating the gamma-secretase enzyme: recent advances and future directions
Biochimie (2018) 147, 130-135. PubMed Europe PubMed DOI
Appel-Cresswell,S., Guella,I., Lehman,A., Foti,D. and Farrer,M.J.
PSEN1 p.Met233Val in a complex neurodegenerative movement and neuropsychiatric disorder
J Mov Disord (2018) 11, 45-48. PubMed Europe PubMed DOI M
Bagyinszky,E., Lee,H.M., Van Giau,V., Koh,S.B., Jeong,J.H., An,S.S.A. and Kim,S.
PSEN1 p.Thr116Ile variant in two Korean families with young onset Alzheimer's disease
Int J Mol Sci (2018) 19 PubMed Europe PubMed DOI M
Barthet,G., Jorda-Siquier,T., Rumi-Masante,J., Bernadou,F., Muller,U. and Mulle,C.
Presenilin-mediated cleavage of APP regulates synaptotagmin-7 and presynaptic plasticity
Nat Commun (2018) 9, 4780-4780. PubMed Europe PubMed DOI PMC EPMC K
Clemente,N., Abdine,A., Ubarretxena-Belandia,I. and Wang,C.
Coupled transmembrane substrate docking and helical unwinding in intramembrane proteolysis of amyloid precursor protein
Sci Rep (2018) 8, 12411-12411. PubMed Europe PubMed DOI PMC EPMC
Dhaliwal,J., Kannangara,T.S., Vaculik,M., Xue,Y., Kumar,K.L., Maione,A., Beique,J.C., Shen,J. and Lagace,D.C.
Adult hippocampal neurogenesis occurs in the absence of presenilin 1 and presenilin 2
Sci Rep (2018) 8, 17931-17931. PubMed Europe PubMed DOI PMC EPMC K
Giau,V.V., Wang,M.J., Bagyinszky,E., Youn,Y.C., An,S.S.A. and Kim,S.
Novel PSEN1 p.Gly417Ala mutation in a Korean patient with early-onset Alzheimer's disease with parkinsonism
Neurobiol Aging (2018) 72, e13-e188. PubMed Europe PubMed DOI M
Hsu,S., Gordon,B.A., Hornbeck,R., Norton,J.B., Levitch,D., Louden,A., Ziegemeier,E., Laforce R Jr, Chhatwal,J., Day,G.S., McDade,E., Morris,J.C., Fagan,A.M., Benzinger,T.L.S., Goate,A.M., Cruchaga,C., Bateman,R.J. and Karch,C.M.
Discovery and validation of autosomal dominant Alzheimer's disease mutations
Alzheimers Res Ther (2018) 10, 67-67. PubMed Europe PubMed DOI PMC EPMC M
Huang,Q., Voloudakis,G., Ren,Y., Yoon,Y., Zhang,E., Kajiwara,Y., Shao,Z., Xuan,Z., Lebedev,D., Georgakopoulos,A. and Robakis,N.K.
Presenilin1/gamma-secretase protects neurons from glucose deprivation-induced death by regulating miR-212 and PEA15
FASEB J (2018) 32, 243-253. PubMed Europe PubMed DOI
Khan,I., Krishnaswamy,S., Sabale,M., Groth,D., Wijaya,L., Morici,M., Berger,I., Schaffitzel,C., Fraser,P.E., Martins,R.N. and Verdile,G.
Efficient production of a mature and functional gamma secretase protease
Sci Rep (2018) 8, 12834-12834. PubMed Europe PubMed DOI PMC EPMC E
Li,L., Roh,J.H., Chang,E.H., Lee,Y., Lee,S., Kim,M., Koh,W., Chang,J.W., Kim,H.J., Nakanishi,M., Barker,R.A., Na,D.L. and Song,J.
iPSC Modeling of presenilin1 mutation in Alzheimer's disease with cerebellar ataxia
Exp Neurobiol (2018) 27, 350-364. PubMed Europe PubMed DOI PMC EPMC M
Liu,Z., Thakar,A., Santoro,S.W. and Pratt,K.G.
Presenilin regulates retinotectal synapse formation through EphB2 receptor processing
Dev Neurobiol (2018) 78, 1171-1190. PubMed Europe PubMed DOI
Ma,L., Zhang,J., Shi,Y., Wang,W., Ren,Z., Xia,M., Zhang,Y. and Yang,M.
Gene mutations in a Han Chinese Alzheimer's disease cohort
Brain Behav (2018) , e01180-e01180. PubMed Europe PubMed DOI M
Pine,S.R.
Rethinking gamma-secretase inhibitors for treatment of non-small-cell lung cancer: is Notch the target?
Clin Cancer Res (2018) 24, 6136-6141. PubMed Europe PubMed DOI I
Rocha,A.L., Costa,A., Garrett,M.C. and Meireles,J.
Difficult case of a rare form of familial Alzheimer's disease with PSEN1 P117L mutation
BMJ Case Rep (2018) 11 PubMed Europe PubMed DOI M
Sasaguri,H., Nagata,K., Sekiguchi,M., Fujioka,R., Matsuba,Y., Hashimoto,S., Sato,K., Kurup,D., Yokota,T. and Saido,T.C.
Introduction of pathogenic mutations into the mouse Psen1 gene by Base Editor and Target-AID
Nat Commun (2018) 9, 2892-2892. PubMed Europe PubMed DOI PMC EPMC
Schauenburg,L., Liebsch,F., Eravci,M., Mayer,M.C., Weise,C. and Multhaup,G.
APLP1 is endoproteolytically cleaved by gamma-secretase without previous ectodomain shedding
Sci Rep (2018) 8, 1916-1916. PubMed Europe PubMed DOI
Shi,T.W., Bai,N., Zhang,J.A., Lu,F., Chen,X.B., Kong,X.D. and Yu,J.B.
Mutations in the gamma-secretase genes PSEN1, PSENEN, and NCSTN in a family with acne inversa
Eur J Dermatol (2018) 28, 374-376. PubMed Europe PubMed DOI M
Stanga,S., Vrancx,C., Tasiaux,B., Marinangeli,C., Karlstrom,H. and Kienlen-Campard,P.
Specificity of presenilin-1- and presenilin-2-dependent gamma-secretases towards substrate processing
J Cell Mol Med (2018) 22, 823-833. PubMed Europe PubMed DOI I
Stenovec,M., Trkov Bobnar,S., Smolic,T., Kreft,M., Parpura,V. and Zorec,R.
Presenilin PS1E9 disrupts mobility of secretory organelles in rat astrocytes
Acta Physiol (Oxf) (2018) 223, e13046-e13046. PubMed Europe PubMed DOI M
Sutovsky,S., Smolek,T., Turcani,P., Petrovic,R., Brandoburova,P., Jadhav,S., Novak,P., Attems,J. and Zilka,N.
Neuropathology and biochemistry of early onset familial Alzheimer's disease caused by presenilin-1 missense mutation Thr116Asn
J Neural Transm (Vienna) (2018) 125, 965-976. PubMed Europe PubMed DOI M
Takahashi,Y., Ohta,Y., Sasaki,R., Tadokoro,K., Sato,K., Shang,J., Takemoto,M., Hishikawa,N., Yamashita,T., Haraguchi,T., Ikeuchi,T. and Abe,K.
A novel presenilin 1 mutation (Leu418Trp) associated with spasticity, parkinsonism, and white matter lesion in a dominant Alzheimer's family
J Neurol Sci (2018) 387, 166-169. PubMed Europe PubMed DOI M
Tang,N. and Kepp,K.P.
Abeta42/Abeta40 ratios of presenilin 1 mutations correlate with clinical onset of Alzheimer's disease
J Alzheimers Dis (2018) 66, 939-945. PubMed Europe PubMed DOI M
Tiedt,H.O., Benjamin,B., Niedeggen,M. and Lueschow,A.
Phenotypic variability in autosomal dominant familial Alzheimer disease due to the S170F mutation of presenilin-1
Neurodegener Dis (2018) 18, 57-68. PubMed Europe PubMed DOI M
Wang,J.C., Alinaghi,S., Tafakhori,A., Sikora,E., Azcona,L.J., Karkheiran,S., Goate,A., Paisan-Ruiz,C. and Darvish,H.
Genetic screening in two Iranian families with early-onset Alzheimer's disease identified a novel PSEN1 mutation
Neurobiol Aging (2018) 62, e15-e244. PubMed Europe PubMed DOI M
Wei,K., Qin,L.Z., Wang,X.J., Li,W., Lu,F. and Li,S.J.
[Presenilin 1 p. F105L mutation was associated with a Chinese pedigree with early-onset familial Alzheimer's disease]
Zhonghua Yi Xue Za Zhi (2018) 98, 3324-3327. PubMed Europe PubMed DOI M
Zhang,S., Cai,F., Wu,Y., Bozorgmehr,T., Wang,Z., Zhang,S., Huang,D., Guo,J., Shen,L., Rankin,C., Tang,B. and Song,W.
A presenilin-1 mutation causes Alzheimer disease without affecting Notch signaling
Mol Psychiatry (2018) DOI M
Zoltowska,K.M. and Berezovska,O.
Dynamic nature of presenilin1/gamma-secretase: implication for Alzheimer's disease pathogenesis
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2017

Aguayo-Ortiz,R., Chavez-Garcia,C., Straub,J.E. and Dominguez,L.
Characterizing the structural ensemble of gamma-secretase using a multiscale molecular dynamics approach
Chem Sci (2017) 8, 5576-5584. PubMed Europe PubMed DOI PMC EPMC
Bolduc,D.M., Selkoe,D.J. and Wolfe,M.S.
Enzymatic assays for studying intramembrane proteolysis
Methods Enzymol (2017) 584, 295-308. PubMed Europe PubMed DOI A
Bursavich,M.G., Harrison,B.A., Acharya,R., Costa,D.E., Freeman,E.A., Hodgdon,H.E., Hrdlicka,L.A., Jin,H., Kapadnis,S., Moffit,J.S., Murphy,D.A., Nolan,S., Patzke,H., Tang,C., Wen,M., Koenig,G., Blain,J.F. and Burnett,D.A.
Design, synthesis and evaluation of a novel series of oxadiazine gamma secretase modulators for familial Alzheimer's disease
J Med Chem (2017) 60, 2383-2400. PubMed Europe PubMed DOI
Dong,J., Qin,W., Wei,C., Tang,Y., Wang,Q. and Jia,J.
A novel PSEN1 K311R mutation discovered in Chinese families with late-onset Alzheimer's disease affects amyloid-beta production and tau phosphorylation
J Alzheimers Dis (2017) 57, 613-623. PubMed Europe PubMed DOI M
Frost,G.R., Wong,E. and Li,Y.M.
Versatility of presenilin 1
Proc Natl Acad Sci U S A (2017) 114, 6885-6887. PubMed Europe PubMed DOI
Gallo,M., Frangipane,F., Cupidi,C., De Bartolo,M., Turone,S., Ferrari,C., Nacmias,B., Grimaldi,G., Lagana,V., Colao,R., Bernardi,L., Anfossi,M., Conidi,M.E., Vasso,F., Curcio,S.A.M., Mirabelli,M., Smirne,N., Torchia,G., Muraca,M.G., Puccio,G., Di Lorenzo,R., Piccininni,M., Tedde,A., Maletta,R.G., Sorbi,S. and Bruni,A.C.
The novel PSEN1 M84V mutation associated to frontal dysexecutive syndrome, spastic paraparesis, and cerebellar atrophy in a dominant Alzheimer's disease family
Neurobiol Aging (2017) 56, e7-e213. PubMed Europe PubMed DOI M
Gertsik,N., Am Ende,C.W., Geoghegan,K.F., Nguyen,C., Mukherjee,P., Mente,S., Seneviratne,U., Johnson,D.S. and Li,Y.M.
Mapping the binding site of BMS-708163 on gamma-secretase with cleavable photoprobes
Cell Chem Biol (2017) 24, 3-8. PubMed Europe PubMed DOI I
Grigorenko,A.P., Moliaka,Y.K., Plotnikova,O.V., Smirnov,A., Nikishina,V.A., Goltsov,A.Y., Gusev,F., Andreeva,T.V., Nelson,O., Bezprozvanny,I. and Rogaev,E.I.
Mutational re-modeling of di-aspartyl intramembrane proteases: uncoupling physiologically-relevant activities from those associated with Alzheimer's disease
Oncotarget (2017) 8, 82006-82026. PubMed Europe PubMed DOI M
Hu,C., Xu,J., Zeng,L., Li,T., Cui,M.Z. and Xu,X.
Pen-2 and presenilin are sufficient to catalyze notch processing
J Alzheimers Dis (2017) 56, 1263-1269. PubMed Europe PubMed DOI
Johnson,D.S., Li,Y.M., Pettersson,M. and St George-Hyslop,P.H.
Structural and chemical biology of presenilin complexes
Cold Spring Harb Perspect Med (2017) 7, a024067-a024067. PubMed Europe PubMed DOI
Kang,J., Shin,S., Perrimon,N. and Shen,J.
An evolutionarily conserved role of presenilin in neuronal protection in the aging Drosophila brain
Genetics (2017) 206, 1479-1493. PubMed Europe PubMed DOI
Kelleher RJ 3rd and Shen,J.
Presenilin-1 mutations and Alzheimer's disease
Proc Natl Acad Sci U S A (2017) 114, 629-631. PubMed Europe PubMed DOI M
Langosch,D. and Steiner,H.
Substrate processing in intramembrane proteolysis by gamma-secretase - the role of protein dynamics
Biol Chem (2017) 398, 441-453. PubMed Europe PubMed DOI P
Lanoiselee,H.M., Nicolas,G., Wallon,D., Rovelet-Lecrux,A., Lacour,M., Rousseau,S., Richard,A.C., Pasquier,F., Rollin-Sillaire,A., Martinaud,O., Quillard-Muraine,M., de la Sayette,V., Boutoleau-Bretonniere,C., Etcharry-Bouyx,F., Chauvire,V., Sarazin,M., le Ber,I., Epelbaum,S., Jonveaux,T., Rouaud,O., Ceccaldi,M., Felician,O., Godefroy,O., Formaglio,M., Croisile,B., Auriacombe,S., Chamard,L., Vincent,J.L., Sauvee,M., Marelli-Tosi,C., Gabelle,A., Ozsancak,C., Pariente,J., Paquet,C., Hannequin,D. and Campion,D.
APP, PSEN1, and PSEN2 mutations in early-onset Alzheimer disease: A genetic screening study of familial and sporadic cases
PLoS Med (2017) 14, e1002270-e1002270. PubMed Europe PubMed DOI PMC EPMC M
Lee,J.Y., Feng,Z., Xie,X.Q. and Bahar,I.
Allosteric modulation of intact gamma-secretase structural dynamics
Biophys J (2017) 113, 2634-2649. PubMed Europe PubMed DOI
Li,S., Zhang,W. and Han,W.
Initial substrate binding of gamma-secretase: the role of substrate flexibility
ACS Chem Neurosci (2017) 8, 1279-1290. PubMed Europe PubMed DOI
Liu,C.Y., Ohki,Y., Tomita,T., Osawa,S., Reed,B.R., Jagust,W., Van Berlo,V., Jin,L.W., Chui,H.C., Coppola,G. and Ringman,J.M.
Two novel mutations in the first transmembrane domain of presenilin1 cause young-onset Alzheimer's disease
J Alzheimers Dis (2017) 58, 1035-1041. PubMed Europe PubMed DOI M
Maesako,M., Horlacher,J., Zoltowska,K.M., Kastanenka,K.V., Kara,E., Svirsky,S., Keller,L.J., Li,X., Hyman,B.T., Bacskai,B.J. and Berezovska,O.
Pathogenic PS1 phosphorylation at Ser367
elife (2017) 6 PubMed Europe PubMed DOI PMC EPMC
Martin-Maestro,P., Gargini,R., A Sproul,A., Garcia,E., Anton,L.C., Noggle,S., Arancio,O., Avila,J. and Garcia-Escudero,V.
Mitophagy failure in fibroblasts and iPSC-derived neurons of Alzheimer's disease-associated presenilin 1 mutation
Front Mol Neurosci (2017) 10, 291-291. PubMed Europe PubMed DOI PMC EPMC M
Natelson Love,M., Clark,D.G., Cochran,J.N., Den Beste,K.A., Geldmacher,D.S., Benzinger,T.L., Gordon,B.A., Morris,J.C., Bateman,R.J. and Roberson,E.D.
Clinical, imaging, pathological, and biochemical characterization of a novel presenilin 1 mutation (N135Y) causing Alzheimer's disease
Neurobiol Aging (2017) 49, 216-216. PubMed Europe PubMed DOI M
Park,J., An,S.S.A., Giau,V.V., Shim,K., Youn,Y.C., Bagyinszky,E. and Kim,S.
Identification of a novel PSEN1 mutation (Leu232Pro) in a Korean patient with early-onset Alzheimer's disease and a family history of dementia
Neurobiol Aging (2017) 56, e11-e212. PubMed Europe PubMed DOI M
Sun,L., Zhou,R., Yang,G. and Shi,Y.
Analysis of 138 pathogenic mutations in presenilin-1 on the in vitro production of Abeta42 and Abeta40 peptides by gamma-secretase
Proc Natl Acad Sci U S A (2017) 114, E476-E476. PubMed Europe PubMed DOI M
Szaruga,M., Munteanu,B., Lismont,S., Veugelen,S., Horre,K., Mercken,M., Saido,T.C., Ryan,N.S., De Vos,T., Savvides,S.N., Gallardo,R., Schymkowitz,J., Rousseau,F., Fox,N.C., Hopf,C., De Strooper,B. and Chavez-Gutierrez,L.
Alzheimer's-causing mutations shift Abeta length by destabilizing gamma-secretase-abetan interactions
Cell (2017) 170, 443-456. PubMed Europe PubMed DOI
Tagami,S., Yanagida,K., Kodama,T.S., Takami,M., Mizuta,N., Oyama,H., Nishitomi,K., Chiu,Y.W., Okamoto,T., Ikeuchi,T., Sakaguchi,G., Kudo,T., Matsuura,Y., Fukumori,A., Takeda,M., Ihara,Y. and Okochi,M.
Semagacestat is a pseudo-inhibitor of gamma-secretase
Cell Rep (2017) 21, 259-273. PubMed Europe PubMed DOI I
Tomita,T.
Probing the structure and function relationships of presenilin by substituted-cysteine accessibility method
Methods Enzymol (2017) 584, 185-205. PubMed Europe PubMed DOI
Wagner,S.L., Rynearson,K.D., Duddy,S.K., Zhang,C., Nguyen,P.D., Becker,A., Vo,U., Masliah,D., Monte,L., Klee,J.B., Echmalian,C.M., Xia,W., Quinti,L., Johnson,G., Lin,J.H., Kim,D.Y., Mobley,W.C., Rissman,R.A. and Tanzi,R.E.
Pharmacological and toxicological properties of the potent oral gamma-secretase modulator BPN-15606
J Pharmacol Exp Ther (2017) 362, 31-44. PubMed Europe PubMed DOI
Wang,W., Moerman-Herzog,A.M., Slaton,A. and Barger,S.W.
Presenilin 1 mutations influence processing and trafficking of the ApoE receptor apoER2
Neurobiol Aging (2017) 49, 145-153. PubMed Europe PubMed DOI M
Watanabe,H. and Shen,J.
Dominant negative mechanism of presenilin-1 mutations in FAD
Proc Natl Acad Sci U S A (2017) 114, 12635-12637. PubMed Europe PubMed DOI M
Yan,Y., Xu,T.H., Melcher,K. and Xu,H.E.
Defining the minimum substrate and charge recognition model of gamma-secretase
Acta Pharmacol Sin (2017) 38, 1412-1424. PubMed Europe PubMed DOI P
Zhan,Y., Zheng,H., Wang,C., Rong,Z., Xiao,N., Ma,Q. and Zhang,Y.W.
A novel presenilin 1 mutation (F388L) identified in a Chinese family with early-onset Alzheimer's disease
Neurobiol Aging (2017) 50, 168-168. PubMed Europe PubMed DOI M
Zhou,R., Yang,G. and Shi,Y.
Dominant negative effect of the loss-of-function gamma-secretase mutants on the wild-type enzyme through heterooligomerization
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2016

An,S.S., Bagyinszky,E., Kim,H.R., Seok,J.W., Shin,H.W., Bae,S., Kim,S. and Youn,Y.C.
Novel PSEN1 G209A mutation in early-onset Alzheimer dementia supported by structural prediction
BMC Neurol (2016) 16, 71-71. PubMed Europe PubMed DOI PMC EPMC M
Blain,J.F., Bursavich,M.G., Freeman,E.A., Hrdlicka,L.A., Hodgdon,H.E., Chen,T., Costa,D.E., Harrison,B.A., Kapadnis,S., Murphy,D.A., Nolan,S., Tu,Z., Tang,C., Burnett,D.A., Patzke,H. and Koenig,G.
Characterization of FRM-36143 as a new gamma-secretase modulator for the potential treatment of familial Alzheimer's disease
Alzheimers Res Ther (2016) 8, 34-34. PubMed Europe PubMed DOI PMC EPMC
Bolduc,D.M., Montagna,D.R., Gu,Y., Selkoe,D.J. and Wolfe,M.S.
Nicastrin functions to sterically hinder gamma-secretase-substrate interactions driven by substrate transmembrane domain
Proc Natl Acad Sci U S A (2016) 113, E509-E518. PubMed Europe PubMed DOI
Bolduc,D.M., Montagna,D.R., Seghers,M.C., Wolfe,M.S. and Selkoe,D.J.
The amyloid-beta forming tripeptide cleavage mechanism of gamma-secretase
elife (2016) 5 PubMed Europe PubMed DOI P
Chavez-Gutierrez,L. and De Strooper,B.
Probing gamma-secretase-substrate interactions at the single amino acid residue level
EMBO J (2016) 35, 1597-1599. PubMed Europe PubMed DOI
Crump,C.J., Murrey,H.E., Ballard,T.E., Am Ende,C.W., Wu,X., Gertsik,N., Johnson,D.S. and Li,Y.M.
Development of sulfonamide photoaffinity inhibitors for probing cellular gamma-secretase
ACS Chem Neurosci (2016) 7, 1166-1173. PubMed Europe PubMed DOI I
Duggan,S.P. and McCarthy,J.V.
Beyond gamma-secretase activity: the multifunctional nature of presenilins in cell signalling pathways
Cell Signal (2016) 28, 1-11. PubMed Europe PubMed DOI
Fernandez,M.A., Biette,K.M., Dolios,G., Seth,D., Wang,R. and Wolfe,M.S.
Transmembrane substrate determinants for gamma-secretase processing of APP CTFbeta
Biochemistry (2016) 55, 5675-5688. PubMed Europe PubMed DOI
Fleck,D., Voss,M., Brankatschk,B., Giudici,C., Hampel,H., Schwenk,B., Edbauer,D., Fukumori,A., Steiner,H., Kremmer,E., Haug-Kroper,M., Rossner,M.J., Fluhrer,R., Willem,M. and Haass,C.
Proteolytic processing of neuregulin 1 type III by three intramembrane-cleaving proteases
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Fray,S., Ali,N.B., Rassas,A.A., Kechaou,M., Oudiaa,N., Cherif,A., Echebbi,S., Messaoud,T. and Belal,S.
Early psychiatrics symptoms in familial Alzheimer's disease with presenilin 1 mutation (I83T)
J Neural Transm (Vienna) (2016) 123, 451-453. PubMed Europe PubMed DOI M
Fukumori,A. and Steiner,H.
Substrate recruitment of gamma-secretase and mechanism of clinical presenilin mutations revealed by photoaffinity mapping
EMBO J (2016) 35, 1628-1643. PubMed Europe PubMed DOI
Futai,E., Osawa,S., Cai,T., Fujisawa,T., Ishiura,S. and Tomita,T.
Suppressor mutations for presenilin 1 familial Alzheimer disease mutants modulate gamma-secretase activities
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Hu,C., Zeng,L., Li,T., Meyer,M.A., Cui,M.Z. and Xu,X.
Nicastrin is required for amyloid precursor protein (APP) but not Notch processing while anterior pharynx-defective 1 is dispensable for processing of both APP and Notch
J Neurochem (2016) 136, 1246-1258. PubMed Europe PubMed DOI
Kretner,B., Trambauer,J., Fukumori,A., Mielke,J., Kuhn,P.H., Kremmer,E., Giese,A., Lichtenthaler,S.F., Haass,C., Arzberger,T. and Steiner,H.
Generation and deposition of Abeta43 by the virtually inactive presenilin-1 L435F mutant contradicts the presenilin loss-of-function hypothesis of Alzheimer's disease
EMBO Mol Med (2016) 8, 458-465. PubMed Europe PubMed DOI M
Li,N., Liu,K., Qiu,Y., Ren,Z., Dai,R., Deng,Y. and Qing,H.
Effect of presenilin mutations on APP cleavage; insights into the pathogenesis of FAD
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Meckler,X. and Checler,F.
Presenilin 1 and presenilin 2 target gamma-secretase complexes to distinct cellular compartments
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Otto,G.P., Sharma,D. and Williams,R.S.B.
Non-catalytic roles of presenilin throughout evolution
J Alzheimer's Dis (2016) 52, 1177-1187. PubMed Europe PubMed DOI
Pham,K. and Miksovska,J.
Molecular insight of DREAM and presenilin 1 C-terminal fragment interactions
FEBS Lett (2016) 590, 1114-1122. PubMed Europe PubMed DOI
Piccoli,E., Rossi,G., Rossi,T., Pelliccioni,G., D'Amato,I., Tagliavini,F. and Di Fede,G.
Novel PSEN1 mutations (H214N and R220P) associated with familial Alzheimer's disease identified by targeted exome sequencing
Neurobiol Aging (2016) 40, e7-e11. PubMed Europe PubMed DOI M
Poon,A., Li,T., Pires,C., Nielsen,T.T., Nielsen,J.E., Holst,B., Dinnyes,A., Hyttel,P. and Freude,K.K.
Derivation of induced pluripotent stem cells from a familial Alzheimer's disease patient carrying the L282F mutation in presenilin 1
Stem Cell Res (2016) 17, 470-473. PubMed Europe PubMed DOI M
Poon,A., Schmid,B., Pires,C., Nielsen,T.T., Hjermind,L.E., Nielsen,J.E., Holst,B., Hyttel,P. and Freude,K.K.
Generation of a gene-corrected isogenic control hiPSC line derived from a familial Alzheimer's disease patient carrying a L150P mutation in presenilin 1
Stem Cell Res (2016) 17, 466-469. PubMed Europe PubMed DOI M
Ravenscroft,T.A., Pottier,C., Murray,M.E., Baker,M., Christopher,E., Levitch,D., Brown,P.H., Barker,W., Duara,R., Greig-Custo,M., Betancourt,A., English,M., Sun,X., Ertekin-Taner,N., Graff-Radford,N.R., Dickson,D.W. and Rademakers,R.
The presenilin 1 p.Gly206Ala mutation is a frequent cause of early-onset Alzheimer's disease in Hispanics in Florida
Am J Neurodegener Dis (2016) 5, 94-101. PubMed Europe PubMed PMC EPMC M
Ravenscroft,T.A., Pottier,C., Murray,M.E., Baker,M., Christopher,E., Levitch,D., Brown,P.H., Barker,W., Duara,R., Greig-Custo,M., Betancourt,A., English,M., Sun,X., Ertekin-Taner,N., Graff-Radford,N.R., Dickson,D.W. and Rademakers,R.
The presenilin 1 p.Gly206Ala mutation is a frequent cause of early-onset alzheimer's disease in Hispanics in Florida
Am J Neurodegenerative Dis (2016) 5, 94-101. M
Sanders,C.R.
How gamma-secretase hits a moving target
elife (2016) 5 PubMed Europe PubMed DOI PMC EPMC
Sarroca,S., Molina-Martinez,P., Areste,C., Etzrodt,M., Garcia de Frutos,P., Gasa,R., Antonell,A., Molinuevo,J.L., Sanchez-Valle,R., Saura,C.A., Llado,A. and Sanfeliu,C.
Preservation of cell-survival mechanisms by the presenilin-1 K239N mutation may cause its milder clinical phenotype
Neurobiol Aging (2016) 46, 169-179. PubMed Europe PubMed DOI M
Scannevin,R.H., Chollate,S., Brennan,M.S., Snodgrass-Belt,P.A., Peng,H., Xu,L., Jung,M.Y., Bussiere,T., Arastu,M.F., Talreja,T., Xin,Z., Dunstan,R.W., Fahrer,D., Rohde,E., Dunah,A.W., Wang,J., Kumaravel,G., Taveras,A.G., Moore Arnold,H. and Rhodes,K.J.
BIIB042, a novel gamma-secretase modulator, reduces amyloidogenic Abeta isoforms in primates and rodents and plaque pathology in a mouse model of Alzheimer's disease
Neuropharmacology (2016) 103, 57-68. PubMed Europe PubMed DOI
Smith,R., Wibom,M., Olsson,T., Hagerstrom,D., Jogi,J., Rabinovici,G.D. and Hansson,O.
Posterior accumulation of tau and concordant hypometabolism in an early-onset Alzheimer's disease patient with presenilin-1 mutation
J Alzheimers Dis (2016) 51, 339-343. PubMed Europe PubMed DOI M
Soares,H.D., Gasior,M., Toyn,J.H., Wang,J.S., Hong,Q., Berisha,F., Furlong,M.T., Raybon,J., Lentz,K.A., Sweeney,F., Zheng,N., Akinsanya,B., Berman,R.M., Thompson,L.A., Olson,R.E., Morrison,J., Drexler,D.M., Macor,J.E., Albright,C.F., Ahlijanian,M.K. and AbuTarif,M.
The gamma-secretase modulator, BMS-932481, modulates Abeta peptides in the plasma and cerebrospinal fluid of healthy volunteers
J Pharmacol Exp Ther (2016) 358, 138-150. PubMed Europe PubMed DOI
Somavarapu,A.K. and Kepp,K.P.
The dynamic mechanism of presenilin-1 function: sensitive gate dynamics and loop unplugging control protein access
Neurobiol Dis (2016) 89, 147-156. PubMed Europe PubMed DOI
Somavarapu,A.K. and Kepp,K.P.
Loss of stability and hydrophobicity of presenilin 1 mutations causing Alzheimer's Disease
J Neurochem (2016) 137, 101-111. PubMed Europe PubMed DOI M
Tedde,A., Bartoli,A., Piaceri,I., Ferrara,S., Bagnoli,S., Serio,A., Sorbi,S. and Nacmias,B.
Novel presenilin 1 mutation (Ile408Thr) in an Italian family with late-onset Alzheimer's disease
Neurosci Lett (2016) 610, 150-153. PubMed Europe PubMed DOI M
Theobald,D.L.
Presenilin adopts the ClC channel fold
Protein Sci (2016) 25, 1363-1365. PubMed Europe PubMed DOI S
Tominaga,A., Cai,T., Takagi-Niidome,S., Iwatsubo,T. and Tomita,T.
Conformational changes in transmembrane domain 4 of presenilin 1 are associated with altered amyloid-beta 42 production
J Neurosci (2016) 36, 1362-1372. PubMed Europe PubMed DOI
Tong,B.C., Lee,C.S., Cheng,W.H., Lai,K.O., Foskett,J.K. and Cheung,K.H.
Familial Alzheimer's disease-associated presenilin 1 mutants promote gamma-secretase cleavage of STIM1 to impair store-operated Ca2+ entry
Sci Signal (2016) 9, ra89-ra89. PubMed Europe PubMed DOI M
Toyn,J.H., Boy,K.M., Raybon,J., Meredith,J.E., Robertson,A.S., Guss,V., Hoque,N., Sweeney,F., Zhuo,X., Clarke,W., Snow,K., Denton,R.R., Zuev,D., Thompson,L.A., Morrison,J., Grace,J., Berisha,F., Furlong,M., Wang,J.-S., Lentz,K.A., Padmanabha,R., Cook,L., Wei,C., Drexler,D.M., Macor,J.E., Albright,C.F., Gasior,M., Olson,R.E., Hong,Q., Soares,H.D., AbuTarif,M. and Ahlijanian,M.K.
Robust translation of gamma-secretase modulator pharmacology across preclinical species and human subjects
J Pharmacol Exp Ther (2016) 358, 125-137. PubMed Europe PubMed DOI
Veugelen,S., Saito,T., Saido,T.C., Chavez-Gutierrez,L. and De Strooper,B.
Familial Alzheimer's disease mutations in presenilin generate amyloidogenic Abeta peptide seeds
Neuron (2016) 90, 410-416. PubMed Europe PubMed DOI M
Wu,W.L., Burnett,D.A., Clader,J., Greenlee,W.J., Jiang,Q., Hyde,L.A., Del Vecchio,R.A., Cohen-Williams,M.E., Song,L., Lee,J., Terracina,G., Zhang,Q., Nomeir,A., Parker,E.M. and Zhang,L.
Design and synthesis of water soluble beta-aminosulfone analogues of SCH 900229 as gamma-secretase inhibitors
Bioorg Med Chem Lett (2016) 26, 5836-5841. PubMed Europe PubMed DOI I
Yonemura,Y., Futai,E., Yagishita,S., Kaether,C. and Ishiura,S.
Specific combinations of presenilins and Aph1s affect the substrate specificity and activity of gamma-secretase
Biochem Biophys Res Commun (2016) 478, 1751-1757. PubMed Europe PubMed DOI
Zhao,Z., Pissarnitski,D.A., Josien,H.B., Bara,T.A., Clader,J.W., Li,H., McBriar,M.D., Rajagopalan,M., Xu,R., Terracina,G., Hyde,L., Song,L., Zhang,L., Parker,E.M., Osterman,R. and Buevich,A.V.
Substituted 4-morpholine N-arylsulfonamides as gamma-secretase inhibitors
Eur J Med Chem (2016) 124, 36-48. PubMed Europe PubMed DOI I

2015

Achouri-Rassas,A., BenAli,N., Fray,S., HadjFredj,S., Kechaou,M., Zakraoui,N.O., Cherif,A., Chabbi,S., Anane,N., Messaoud,T., Gouider,R. and Belal,S.
Novel presenilin 1 mutation (p.I83T) in Tunisian family with early-onset Alzheimer's disease
Neurobiol Aging (2015) 36, e9-e11. PubMed Europe PubMed DOI M
Araki,W. and Tamaoka,A.
Amyloid beta-protein and lipid rafts: focused on biogenesis and catabolism
Front Biosci (Landmark Ed) (2015) 20, 314-324. PubMed Europe PubMed DOI V
Bai,X.C., Yan,C., Yang,G., Lu,P., Ma,D., Sun,L., Zhou,R., Scheres,S.H. and Shi,Y.
An atomic structure of human gamma-secretase
Nature (2015) 525, 212-217. PubMed Europe PubMed DOI S
Bai,X.C., Rajendra,E., Yang,G., Shi,Y. and Scheres,S.H.
Sampling the conformational space of the catalytic subunit of human gamma-secretase
elife (2015) 4 PubMed Europe PubMed DOI S I
Bonds,J.A., Kuttner-Hirshler,Y., Bartolotti,N., Tobin,M.K., Pizzi,M., Marr,R. and Lazarov,O.
Presenilin-1 dependent neurogenesis regulates hippocampal learning and memory
PLoS ONE (2015) 10, e0131266-e0131266. PubMed Europe PubMed DOI PMC EPMC
Brautigam,H., Moreno,C.L., Steele,J.W., Bogush,A., Dickstein,D.L., Kwok,J.B., Schofield,P.R., Thinakaran,G., Mathews,P.M., Hof,P.R., Gandy,S. and Ehrlich,M.E.
Physiologically generated presenilin 1 lacking exon 8 fails to rescue brain PS1-/- phenotype and forms complexes with wildtype PS1 and nicastrin
Sci Rep (2015) 5, 17042-17042. PubMed Europe PubMed DOI PMC EPMC M
Chen,W.T., Hsieh,Y.F., Huang,Y.J., Lin,C.C., Lin,Y.T., Liu,Y.C., Lien,C.C. and Cheng,I.H.
G206D Mutation of presenilin-1 reduces Pen2 interaction, increases Abeta42/Abeta40 ratio and elevates ER Ca(2+) accumulation
Mol Neurobiol (2015) 52, 1835-1849. PubMed Europe PubMed DOI M
Chu,J., Li,J.G., Joshi,Y.B., Giannopoulos,P.F., Hoffman,N.E., Madesh,M. and Pratico,D.
Gamma secretase-activating protein is a substrate for caspase-3: implications for Alzheimer's disease
Biol Psychiatry (2015) 77, 720-728. PubMed Europe PubMed DOI
D'Avanzo,C., Sliwinski,C., Wagner,S.L., Tanzi,R.E., Kim,D.Y. and Kovacs,D.M.
gamma-Secretase modulators reduce endogenous amyloid beta42 levels in human neural progenitor cells without altering neuronal differentiation
FASEB J (2015) 29, 3335-3341. PubMed Europe PubMed DOI
De Strooper,B. and Chavez Gutierrez,L.
Learning by failing: ideas and concepts to tackle gamma-secretases in Alzheimer's disease and beyond
Annu Rev Pharmacol Toxicol (2015) 55, 419-437. PubMed Europe PubMed DOI I
Deng,H., Lv,L., Li,Y., Zhang,C., Meng,F., Pu,Y., Xiao,J., Qian,L., Zhao,W., Liu,Q., Zhang,D., Wang,Y., Zhang,H., He,Y. and Zhu,J.
The miR-193a-3p regulated PSEN1 gene suppresses the multi-chemoresistance of bladder cancer
Biochim Biophys Acta (2015) 1852, 520-528. PubMed Europe PubMed DOI
Duggan,S.P., Yan,R. and McCarthy,J.V.
A ubiquitin-binding CUE domain in presenilin-1 enables interaction with K63-linked polyubiquitin chains
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Elad,N., De Strooper,B., Lismont,S., Hagen,W., Veugelen,S., Arimon,M., Horre,K., Berezovska,O., Sachse,C. and Chavez-Gutierrez,L.
The dynamic conformational landscape of gamma-secretase
J Cell Sci (2015) 128, 589-598. PubMed Europe PubMed DOI S
Fischer,C., Zultanski,S.L., Zhou,H., Methot,J.L., Shah,S., Hayashi,I., Hughes,B.L., Moxham,C.M., Bays,N.W., Smotrov,N., Hill,A.D., Pan,B.S., Wu,Z., Moy,L.Y., Tanga,F., Kenific,C., Cruz,J.C., Walker,D., Bouthillette,M., Nikov,G.N., Deshmukh,S.V., Jeliazkova-Mecheva,V.V., Diaz,D., Michener,M.S., Cook,J.J., Munoz,B. and Shearman,M.S.
Discovery of novel triazolobenzazepinones as gamma-secretase modulators with central Abeta42 lowering in rodents and rhesus monkeys
Bioorg Med Chem Lett (2015) 25, 3488-3494. PubMed Europe PubMed DOI
Fleisher,A.S., Chen,K., Quiroz,Y.T., Jakimovich,L.J., Gutierrez Gomez,M., Langois,C.M., Langbaum,J.B., Roontiva,A., Thiyyagura,P., Lee,W., Ayutyanont,N., Lopez,L., Moreno,S., Munoz,C., Tirado,V., Acosta-Baena,N., Fagan,A.M., Giraldo,M., Garcia,G., Huentelman,M.J., Tariot,P.N., Lopera,F. and Reiman,E.M.
Associations between biomarkers and age in the presenilin 1 E280A autosomal dominant Alzheimer disease kindred: a cross-sectional study
JAMA Neurol (2015) 72, 316-324. PubMed Europe PubMed DOI M
Jiang,H.Y., Li,G.D., Dai,S.X., Bi,R., Zhang,D.F., Li,Z.F., Xu,X.F., Zhou,T.C., Yu,L. and Yao,Y.G.
Identification of PSEN1 mutations p.M233L and p.R352C in Han Chinese families with early-onset familial Alzheimer's disease
Neurobiol Aging (2015) 36, e3-e6. PubMed Europe PubMed DOI M
Kamp,F., Winkler,E., Trambauer,J., Ebke,A., Fluhrer,R. and Steiner,H.
Intramembrane proteolysis of beta-amyloid precursor protein by gamma-secretase is an unusually slow process
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Kang,Y., Melcher,K. and Xu,H.E.
The cryo-electron microscopy structure of gamma-secretase: towards complex assembly, substrate recognition and a catalytic mechanism
Natl Sci Rev (2015) 2, 4-5. PubMed Europe PubMed DOI PMC EPMC S
Kong,R., Chang,S., Xia,W. and Wong,S.T.
Molecular dynamics simulation study reveals potential substrate entry path into gamma-secretase/presenilin-1
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Kosik,K.S., Munoz,C., Lopez,L., Arcila,M.L., Garcia,G., Madrigal,L., Moreno,S., Rios Romenets,S., Lopez,H., Gutierrez,M., Langbaum,J.B., Cho,W., Suliman,S., Tariot,P.N., Ho,C., Reiman,E.M. and Lopera,F.
Homozygosity of the autosomal dominant Alzheimer disease presenilin 1 E280A mutation
Neurology (2015) 84, 206-208. PubMed Europe PubMed DOI M
MacPherson,S.E., Parra,M.A., Moreno,S., Lopera,F. and Della Sala,S.
Dual memory task impairment in E280A presenilin-1 mutation carriers
J Alzheimers Dis (2015) 44, 481-492. PubMed Europe PubMed DOI M
Marinangeli,C., Tasiaux,B., Opsomer,R., Hage,S., Sodero,A.O., Dewachter,I., Octave,J.N., Smith,S.O., Constantinescu,S.N. and Kienlen-Campard,P.
Presenilin transmembrane domain 8 conserved AxxxAxxxG motifs are required for the activity of the gamma-secretase complex
J Biol Chem (2015) 290, 7169-7184. PubMed Europe PubMed DOI
Matz,A., Halamoda-Kenzaoui,B., Hamelin,R., Mosser,S., Alattia,J.R., Dimitrov,M., Moniatte,M. and Fraering,P.C.
Identification of new Presenilin-1 phosphosites: implication for gamma-secretase activity and Abeta production
J Neurochem (2015) 133, 409-421. PubMed Europe PubMed DOI
Methot,J.L., Fischer,C., Li,C., Rivkin,A., Ahearn,S.P., Brown,W.C., Kattar,S., Kelley,E., Mampreian,D.M., Schell,A., Rosenau,A., Zhou,H., Ball,R., Deshmukh,S.V., Jeliazkova-Mecheva,V.V., Diaz,D., Moy,L.Y., Kenific,C.M., Moxham,C., Shah,S., Nuthall,H., Szewczak,A.A., Hill,A., Hughes,B., Smotrov,N., Munoz,B., Miller,T.A. and Shearman,M.S.
Potent benzoazepinone gamma-secretase modulators with improved bioavailability
Bioorg Med Chem Lett (2015) 25, 3495-3500. PubMed Europe PubMed DOI
Muchnik,C., Olivar,N., Dalmasso,M.C., Azurmendi,P.J., Liberczuk,C., Morelli,L. and Brusco,L.I.
Identification of PSEN2 mutation p.N141I in Argentine pedigrees with early-onset familial Alzheimer's disease
Neurobiol Aging (2015) 36, 2674-2677. PubMed Europe PubMed DOI M
Pasqualon,T., Pruessmeyer,J., Jankowski,V., Babendreyer,A., Groth,E., Schumacher,J., Koenen,A., Weidenfeld,S., Schwarz,N., Denecke,B., Jahr,H., Dreymueller,D., Jankowski,J. and Ludwig,A.
A cytoplasmic C-terminal fragment of syndecan-1 is generated by sequential proteolysis and antagonizes syndecan-1 dependent lung tumor cell migration
Oncotarget (2015) 6, 31295-31312. PubMed Europe PubMed DOI
Pellowska,M., Stein,C., Pohland,M., Merk,D., Klein,J., Eckert,G.P., Schubert-Zsilavecz,M. and Wurglics,M.
Pharmacokinetic properties of MH84, a gamma-secretase modulator with PPARgamma agonistic activity
J Pharm Biomed Anal (2015) 102, 417-424. PubMed Europe PubMed DOI
Pettersson,M., Johnson,D.S., Humphrey,J.M., Butler,T.W., Am Ende,C.W., Fish,B.A., Green,M.E., Kauffman,G.W., Mullins,P.B., O'Donnell,C.J., Stepan,A.F., Stiff,C.M., Subramanyam,C., Tran,T.P., Vetelino,B.C., Yang,E., Xie,L., Bales,K.R., Pustilnik,L.R., Steyn,S.J., Wood,K.M. and Verhoest,P.R.
Design of pyridopyrazine-1,6-dione gamma-secretase modulators that align potency, MDR efflux ratio, and metabolic stability
ACS Med Chem Lett (2015) 6, 596-601. PubMed Europe PubMed DOI PMC EPMC
Pettersson,M., Johnson,D.S., Humphrey,J.M., Am Ende,C.W., Evrard,E., Efremov,I., Kauffman,G.W., Stepan,A.F., Stiff,C.M., Xie,L., Bales,K.R., Hajos-Korcsok,E., Murrey,H.E., Pustilnik,L.R., Steyn,S.J., Wood,K.M. and Verhoest,P.R.
Discovery of indole-derived pyridopyrazine-1,6-dione gamma-secretase modulators that target presenilin
Bioorg Med Chem Lett (2015) 25, 908-913. PubMed Europe PubMed DOI
Roeber,S., Muller-Sarnowski,F., Kress,J., Edbauer,D., Kuhlmann,T., Tuttelmann,F., Schindler,C., Winter,P., Arzberger,T., Muller,U., Danek,A. and Kretzschmar,H.A.
Three novel presenilin 1 mutations marking the wide spectrum of age at onset and clinical patterns in familial Alzheimer's disease
J Neural Transm (Vienna) (2015) 122, 1715-1719. PubMed Europe PubMed DOI M
Sun,L., Zhao,L., Yang,G., Yan,C., Zhou,R., Zhou,X., Xie,T., Zhao,Y., Wu,S., Li,X. and Shi,Y.
Structural basis of human gamma-secretase assembly
Proc Natl Acad Sci U S A (2015) 112, 6003-6008. PubMed Europe PubMed DOI
Svedruzic,Z.M., Popovic,K. and Sendula-Jengic,V.
Decrease in catalytic capacity of gamma-secretase can facilitate pathogenesis in sporadic and familial Alzheimer's disease
Mol Cell Neurosci (2015) 67, 55-65. PubMed Europe PubMed DOI M
Takagi-Niidome,S., Sasaki,T., Osawa,S., Sato,T., Morishima,K., Cai,T., Iwatsubo,T. and Tomita,T.
Cooperative roles of hydrophilic loop 1 and the C-terminus of presenilin 1 in the substrate-gating mechanism of gamma-secretase
J Neurosci (2015) 35, 2646-2656. PubMed Europe PubMed DOI
Takai,T., Hoashi,Y., Tomata,Y., Morimoto,S., Nakamura,M., Watanabe,T., Igari,T. and Koike,T.
Discovery of novel 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine derivatives as gamma-secretase modulators
Bioorg Med Chem Lett (2015) 25, 4245-4249. PubMed Europe PubMed DOI
Takei,N., Sobu,Y., Kimura,A., Urano,S., Piao,Y., Araki,Y., Taru,H., Yamamoto,T., Hata,S., Nakaya,T. and Suzuki,T.
Cytoplasmic fragment of alcadein alpha generated by regulated intramembrane proteolysis enhances amyloid beta-protein precursor (APP) transport into the late secretory pathway and facilitates APP cleavage
J Biol Chem (2015) 290, 987-995. PubMed Europe PubMed DOI
Teranishi,Y., Inoue,M., Yamamoto,N.G., Kihara,T., Wiehager,B., Ishikawa,T., Winblad,B., Schedin-Weiss,S., Frykman,S. and Tjernberg,L.O.
Proton myo-inositol cotransporter is a novel gamma-secretase associated protein that regulates Abeta production without affecting Notch cleavage
FEBS J (2015) 282, 3438-3451. PubMed Europe PubMed DOI
Walter,J.
Twenty years of presenilins-important proteins in health and disease
Mol Med (2015) 21 Suppl 1, S41-S48. PubMed Europe PubMed DOI PMC EPMC V
Wan,J., Li,Y.-X. and Zheng,W.-H.
Research progress in spatial structure and modulators of gamma-secretase
Chin J Pharmacol Toxicol (2015) 29, 979-985. DOI V
Weissmiller,A.M., Natera-Naranjo,O., Reyna,S.M., Pearn,M.L., Zhao,X., Nguyen,P., Cheng,S., Goldstein,L.S., Tanzi,R.E., Wagner,S.L., Mobley,W.C. and Wu,C.
A gamma-secretase inhibitor, but not a gamma-secretase modulator, induced defects in BDNF axonal trafficking and signaling: evidence for a role for APP
PLoS ONE (2015) 10, e0118379-e0118379. PubMed Europe PubMed DOI PMC EPMC
Wolfe,M.S.
Cutting in on a secretase pas de deux
Cell Res (2015) 25, 1091-1092. PubMed Europe PubMed DOI
Xia,D., Watanabe,H., Wu,B., Lee,S.H., Li,Y., Tsvetkov,E., Bolshakov,V.Y., Shen,J. and Kelleher,R.J.3.
Presenilin-1 knockin mice reveal loss-of-function mechanism for familial Alzheimer's disease
Neuron (2015) 85, 967-981. PubMed Europe PubMed DOI M
Zahs,K.R. and Ashe,K.H.
More than a FAD: the in vivo effects of disease-linked presenilin-1 mutations
Neuron (2015) 85, 893-895. PubMed Europe PubMed DOI M
Zhao,Z., Pissarnitski,D.A., Josien,H.B., Wu,W.L., Xu,R., Li,H., Clader,J.W., Burnett,D.A., Terracina,G., Hyde,L., Lee,J., Song,L., Zhang,L. and Parker,E.M.
Discovery of a novel, potent spirocyclic series of gamma-secretase inhibitors
J Med Chem (2015) 58, 8806-8817. PubMed Europe PubMed DOI I

2014

Acx,H., Chavez-Gutierrez,L., Serneels,L., Lismont,S., Benurwar,M., Elad,N. and De Strooper,B.
Signature amyloid beta profiles are produced by different gamma-secretase complexes
J Biol Chem (2014) 289, 4346-4355. PubMed Europe PubMed DOI
Ballard,T., Murrey,H.E., Geoghegan,K.F., Am Ende,C.W. and Johnson,D.S.
Investigating gamma-secretase protein interactions in live cells using active site-directed clickable dual-photoaffinity probes
MedChemComm (2014) 5, 321-327. DOI I
Bhadoriya,K.S., Sharma,M.C., Sharma,S., Jain,S.V. and Avchar,M.H.
An approach to design potent anti-Alzheimer's agents by 3D-QSAR studies on fused 5,6-bicyclic heterocycles as gamma-secretase modulators using kNN-MFA methodology
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Bolduc,D.M. and Wolfe,M.S.
Structure of nicastrin unveils secrets of gamma-secretase
Proc Natl Acad Sci U S A (2014) 111, 14643-14644. PubMed Europe PubMed DOI S
Cornejo-Olivas,M.R., Yu,C.E., Mazzetti,P., Mata,I.F., Meza,M., Lindo-Samanamud,S., Leverenz,J.B. and Bird,T.D.
Clinical and molecular studies reveal a PSEN1 mutation (L153V) in a Peruvian family with early-onset Alzheimer's disease
Neurosci Lett (2014) 563, 140-143. PubMed Europe PubMed DOI M
De Strooper,B.
Lessons from a failed gamma-secretase Alzheimer trial
Cell (2014) 159, 721-726. PubMed Europe PubMed DOI I
Deng,B., Lian,Y., Wang,X., Zeng,F., Jiao,B., Wang,Y.R., Liang,C.R., Liu,Y.H., Bu,X.L., Yao,X.Q., Zhu,C., Shen,L., Zhou,H.D., Zhang,T. and Wang,Y.J.
Identification of a novel mutation in the presenilin 1 gene in a Chinese Alzheimer's disease family
Neurotox Res (2014) 26, 211-215. PubMed Europe PubMed DOI M
Dolzhanskaya,N., Gonzalez,M.A., Sperziani,F., Stefl,S., Messing,J., Wen,G.Y., Alexov,E., Zuchner,S. and Velinov,M.
A novel p.Leu(381)Phe mutation in presenilin 1 is associated with very early onset and unusually fast progressing dementia as well as lysosomal inclusions typically seen in Kufs disease
J Alzheimers Dis (2014) 39, 23-27. PubMed Europe PubMed DOI M
Gai,J.W., Wahafu,W., Hsieh,Y.C., Liu,M., Zhang,L., Li,S.W., Zhang,B., He,Q., Guo,H. and Jin,J.
Inhibition of presenilins attenuates proliferation and invasion in bladder cancer cells through multiple pathways
Urol Oncol (2014) 32, 36-25. PubMed Europe PubMed DOI I
Gertsik,N., Ballard,T.E., Am Ende,C.W., Johnson,D.S. and Li,Y.-M.
Development of CBAP-BPyne, a probe for gamma-secretase and presenilinase
MedChemComm (2014) 5, 338-341. PubMed Europe PubMed DOI I
Gertsik,N., Chiu,D. and Li,Y.M.
Complex regulation of gamma-secretase: from obligatory to modulatory subunits
Front Aging Neurosci (2014) 6, 342-342. PubMed Europe PubMed DOI PMC EPMC
Groot,A.J., Habets,R., Yahyanejad,S., Hodin,C.M., Reiss,K., Saftig,P., Theys,J. and Vooijs,M.
Regulated proteolysis of NOTCH2 and NOTCH3 receptors by ADAM10 and presenilins
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Smolarkiewicz,M., Skrzypczak,T. and Wojtaszek,P.
The very many faces of presenilins and the gamma-secretase complex
Protoplasma (2013) 250, 997-1011. PubMed Europe PubMed DOI V
Takagi-Niidome,S., Osawa,S., Tomita,T. and Iwatsubo,T.
Inhibition of gamma-secretase activity by a monoclonal antibody against the extracellular hydrophilic loop of presenilin 1
Biochemistry (2013) 52, 61-69. PubMed Europe PubMed DOI
Thathiah,A., Horre,K., Snellinx,A., Vandewyer,E., Huang,Y., Ciesielska,M., De Kloe,G., Munck,S. and De Strooper,B.
beta-Arrestin 2 regulates Abeta generation and gamma-secretase activity in Alzheimer's disease
Nat Med (2013) 19, 43-49. PubMed Europe PubMed DOI
Tiedt,H.O., Lueschow,A., Winter,P. and Muller,U.
Previously not recognized deletion in presenilin-1 (p.Leu174del.) in a patient with early-onset familial Alzheimer's disease
Neurosci Lett (2013) 544, 115-118. PubMed Europe PubMed DOI M
Toyn,J.H., Rowley,A., Matsuoka,Y., Tomita,T. and Imbimbo,B.P.
gamma-Secretase pharmacology: What pharmacology will work for Alzheimer's disease?
Int J Alzheimers Dis (2013) 2013, 849128-849128. PubMed Europe PubMed DOI PMC EPMC I
Wilson,L. and Lardelli,M.
The development of an in vivo gamma-secretase assay using zebrafish embryos
J Alzheimers Dis (2013) 36, 521-534. PubMed Europe PubMed DOI
Wolfe,M.S.
Alzheimer's gamma-secretase under arrestin
Nat Med (2013) 19, 22-24. PubMed Europe PubMed DOI
Wu,W.L., Asberom,T., Bara,T., Bennett,C., Burnett,D.A., Clader,J., Domalski,M., Greenlee,W.J., Josien,H., McBriar,M., Rajagopalan,M., Vicarel,M., Xu,R., Hyde,L.A., Del Vecchio,R.A., Cohen-Williams,M.E., Song,L., Lee,J., Terracina,G., Zhang,Q., Nomeir,A., Parker,E.M. and Zhang,L.
Structure activity relationship studies of tricyclic bispyran sulfone gamma-secretase inhibitors
Bioorg Med Chem Lett (2013) 23, 844-849. PubMed Europe PubMed DOI I
Wu,W.L., Sasikumar,T.K., Domalski,M.S., Qiang,L., Burnett,D.A., Clader,J., Greenlee,W.J., Chan,T.M., Lee,J. and Zhang,L.
A-ring modification of SCH 900229 and related chromene sulfone gamma-secretase inhibitors
Bioorg Med Chem Lett (2013) 23, 850-853. PubMed Europe PubMed DOI I
Ye,X.M., Konradi,A.W., Sun,M., Yuan,S., Aubele,D.L., Dappen,M., Dressen,D., Garofalo,A.W., Jagodzinski,J.J., Latimer,L., Probst,G.D., Sham,H.L., Wone,D., Xu,Y.Z., Ness,D., Brigham,E., Kwong,G.T., Willtis,C., Tonn,G., Goldbach,E., Quinn,K.P., Zhang,H.H., Sauer,J.M., Bova,M. and Basi,G.S.
Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious gamma-secretase inhibitors
Bioorg Med Chem Lett (2013) 23, 996-1000. PubMed Europe PubMed DOI I
Yngve,U., Paulsen,K., MacSari,I., Sundstrom,M., Santangelo,E., Linde,C., Bogar,K., Lake,F., Besidski,Y., Malmborg,J., Stromberg,K., Appelkvist,P., Radesater,A.C., Olsson,F., Bergstrom,D., Klintenberg,R. and Arvidsson,P.I.
Triazolopyrimidinones as gamma-secretase modulators: Structure-activity relationship, modulator profile, and in vivo profiling
MedChemComm (2013) 4, 422-431. DOI
Zhang,S., Zhang,M., Cai,F. and Song,W.
Biological function of presenilin and its role in AD pathogenesis
Transl Neurodegener (2013) 2, 15-15. PubMed Europe PubMed DOI PMC EPMC

2012

Adeniji,A.O., Wells,R.M. and Adejare,A.
Syntheses and in-vitro evaluation of novel adamantane based gamma-secretase inhibitors
Curr Med Chem (2012) 19, 2458-2471. PubMed Europe PubMed I
Bischoff,F., Berthelot,D., De Cleyn,M., Macdonald,G., Minne,G., Oehlrich,D., Pieters,S., Surkyn,M., Trabanco,A.A., Tresadern,G., Van Brandt,S., Velter,I., Zaja,M., Borghys,H., Masungi,C., Mercken,M. and Gijsen,H.J.
Design and synthesis of a novel series of bicyclic heterocycles as potent gamma-secretase modulators
J Med Chem (2012) 55, 9089-9106. PubMed Europe PubMed DOI
Borgegard,T., Jureus,A., Olsson,F., Rosqvist,S., Sabirsh,A., Rotticci,D., Paulsen,K., Klintenberg,R., Yan,H., Waldman,M., Stromberg,K., Nord,J., Johansson,J., Regner,A., Parpal,S., Malinowsky,D., Radesater,A.C., Li,T., Singh,R., Eriksson,H. and Lundkvist,J.
First and second generation gamma-secretase modulators (GSMs) modulate amyloid-beta (Abeta) peptide production through different mechanisms
J Biol Chem (2012) 287, 11810-11819. PubMed Europe PubMed DOI I
Borroni,B., Pilotto,A., Bonvicini,C., Archetti,S., Alberici,A., Lupi,A., Gennarelli,M. and Padovani,A.
Atypical presentation of a novel Presenilin 1 R377W mutation: Sporadic, late-onset Alzheimer Disease with epilepsy and frontotemporal atrophy
Neurol Sci (2012) 33, 375-378. PubMed Europe PubMed DOI M
Cacquevel,M., Aeschbach,L., Houacine,J. and Fraering,P.C.
Alzheimer's disease-linked mutations in presenilin-1 result in a drastic loss of activity in purified gamma-secretase complexes
PLoS ONE (2012) 7, e35133-e35133. PubMed Europe PubMed DOI PMC EPMC M
Chau,D.M., Crump,C.J., Villa,J.C., Scheinberg,D.A. and Li,Y.M.
Familial Alzheimer disease presenilin-1 mutations alter the active site conformation of gamma-secretase
J Biol Chem (2012) 287, 17288-17296. PubMed Europe PubMed DOI M
Chavez-Gutierrez,L., Bammens,L., Benilova,I., Vandersteen,A., Benurwar,M., Borgers,M., Lismont,S., Zhou,L., Van Cleynenbreugel,S., Esselmann,H., Wiltfang,J., Serneels,L., Karran,E., Gijsen,H., Schymkowitz,J., Rousseau,F., Broersen,K. and De Strooper,B.
The mechanism of gamma-secretase dysfunction in familial Alzheimer disease
EMBO J (2012) 31, 2261-2274. PubMed Europe PubMed DOI M
Close,J., Heidebrecht,R., Jr., Hendrix,J., Li,C., Munoz,B., Surdi,L., Kattar,S., Tempest,P., Moses,P., Geng,X., Hughes,B., Smotrov,N., Moxham,C., Chapnick,J., Kariv,I., Nikov,G., Burke,J.E., Deshmukh,S., Jeliazkova-Mecheva,V., Leach,J.K., Diaz,D., Xu,L., Yang,Z., Kwei,G., Moy,L., Shah,S., Tanga,F., Kenefic,C., Savage,D., Shearman,M., Ball,R.G., McNevin,M.J., Markarewicz,A. and Miller,T.
Lead optimization of 4,4-biaryl piperidine amides as gamma-secretase inhibitors
Bioorg Med Chem Lett (2012) 22, 3203-3207. PubMed Europe PubMed DOI I
Crump,C.J., Am Ende,C.W., Eric Ballard,T., Pozdnyakov,N., Pettersson,M., Chau,D.M., Bales,K.R., Li,Y.M. and Johnson,D.S.
Development of clickable active site-directed photoaffinity probes for gamma-secretase
Bioorg Med Chem Lett (2012) 22, 2997-3000. PubMed Europe PubMed DOI I
De Strooper,B., Iwatsubo,T. and Wolfe,M.S.
Presenilins and gamma-secretase: structure, function, and role in Alzheimer disease
Cold Spring Harb Perspect Med (2012) 2, a006304-a006304. PubMed Europe PubMed DOI PMC EPMC
Findeis,M.A., Schroeder,F., McKee,T.D., Yager,D., Fraering,P.C., Creaser,S.P., Austin,W.F., Clardy,J., Wang,R., Selkoe,D. and Eckman,C.B.
Discovery of a novel pharmacological and structural class of gamma secretase modulators derived from the extract of Actaea racemosa
ACS Chem Neurosci (2012) 3, 941-951. PubMed Europe PubMed DOI PMC EPMC
Fischer,C., Zultanski,S.L., Zhou,H., Methot,J.L., Shah,S., Nuthall,H., Hughes,B.L., Smotrov,N., Hill,A., Szewczak,A.A., Moxham,C.M., Bays,N., Middleton,R.E., Munoz,B. and Shearman,M.S.
Triazoloamides as potent gamma-secretase modulators with reduced hERG liability
Bioorg Med Chem Lett (2012) 22, 3140-3146. PubMed Europe PubMed DOI
Fuller,N.O., Hubbs,J.L., Austin,W.F., Creaser,S.P., McKee,T.D., Loureiro,R.M.B., Tate,B., Xia,W., Ives,J.L., Findeis,M.A. and Bronk,B.S.
Initial optimization of a new series of gamma-secretase modulators derived from a triterpene glycoside
ACS Med Chem Lett (2012) 3, 908-913. PubMed Europe PubMed DOI
Gijsen,H.J. and Mercken,M.
gamma-Secretase modulators: can we combine potency with safety?
Int J Alzheimers Dis (2012) 2012, 295207-295207. PubMed Europe PubMed DOI PMC EPMC
Golde,T.E., Ran,Y. and Felsenstein,K.M.
Shifting a complex debate on gamma-secretase cleavage and Alzheimer's disease
EMBO J (2012) 31, 2237-2239. PubMed Europe PubMed DOI M V
Hayashi,I., Takatori,S., Urano,Y., Miyake,Y., Takagi,J., Sakata-Yanagimoto,M., Iwanari,H., Osawa,S., Morohashi,Y., Li,T., Wong,P.C., Chiba,S., Kodama,T., Hamakubo,T., Tomita,T. and Iwatsubo,T.
Neutralization of the gamma-secretase activity by monoclonal antibody against extracellular domain of nicastrin
Oncogene (2012) 31, 787-798. PubMed Europe PubMed DOI
Honarnejad,K. and Herms,J.
Presenilins: role in calcium homeostasis
Int J Biochem Cell Biol (2012) 44, 1983-1986. PubMed Europe PubMed DOI V
Huang,X., Zhou,W., Liu,X., Li,H., Sun,G., Mandal,M., Vicarel,M., Zhu,X., Bennett,C., McCraken,T., Pissarnitski,D., Zhao,Z., Cole,D., Gallo,G., Zhu,Z., Palani,A., Aslanian,R., Clader,J., Czarniecki,M., Greenlee,W., Burnett,D., Cohen-Williams,M., Hyde,L., Song,L., Zhang,L., Chu,I. and Buevich,A.
Synthesis and SAR studies of fused oxadiazines as gamma-secretase modulators for treatment of Alzheimer's disease
ACS Med Chem Lett (2012) 3, 931-935. PubMed Europe PubMed DOI
Hubbs,J.L., Fuller,N.O., Austin,W.F., Shen,R., Creaser,S.P., McKee,T.D., Loureiro,R.M., Tate,B., Xia,W., Ives,J. and Bronk,B.S.
Optimization of a natural product-based class of gamma-secretase modulators
J Med Chem (2012) 55, 9270-9282. PubMed Europe PubMed DOI
Jumpertz,T., Rennhack,A., Ness,J., Baches,S., Pietrzik,C.U., Bulic,B. and Weggen,S.
Presenilin is the molecular target of acidic gamma-secretase modulators in living cells
PLoS ONE (2012) 7, e30484-e30484. PubMed Europe PubMed DOI PMC EPMC
Kandimalla,R.J., Wani,W.Y., Bk,B. and Gill,K.D.
siRNA against presenilin 1 (PS1) down regulates amyloid beta 42 production in IMR-32 cells
J Biomed Sci (2012) 19, 2-2. PubMed Europe PubMed DOI
Kerchner,G.A. and Holbrook,K.
Novel presenilin-1 Y159F sequence variant associated with early-onset Alzheimer's disease
Neurosci Lett (2012) 531, 142-144. PubMed Europe PubMed DOI M
Kim,J., Bagyinszky,E., Chang,Y.H., Choe,G., Choi,B.O., An,S.S. and Kim,S.
A novel PSEN1 H163P mutation in a patient with early-onset Alzheimer's disease: clinical, neuroimaging, and neuropathological findings
Neurosci Lett (2012) 530, 109-114. PubMed Europe PubMed DOI M
Kolb,E.A., Gorlick,R., Keir,S.T., Maris,J.M., Lock,R., Carol,H., Kurmasheva,R.T., Reynolds,C.P., Kang,M.H., Wu,J., Houghton,P.J. and Smith,M.A.
Initial testing (stage 1) by the pediatric preclinical testing program of RO4929097, a gamma-secretase inhibitor targeting notch signaling
Pediatr Blood Cancer (2012) 58, 815-818. PubMed Europe PubMed DOI I
Lebedeva,E., Stingl,J.C., Thal,D.R., Ghebremedhin,E., Strauss,J., Ozer,E., Bertram,L., von Einem,B., Tumani,H., Otto,M., Riepe,M.W., Hogel,J., Ludolph,A.C. and von Arnim,C.A.
Genetic variants in PSEN2 and correlation to CSF beta-amyloid42 levels in AD
Neurobiol Aging (2012) 33, 201-218. PubMed Europe PubMed DOI M
Mao,G., Cui,M.Z., Li,T., Jin,Y. and Xu,X.
Pen-2 is dispensable for endoproteolysis of presenilin 1, and nicastrin-Aph subcomplex is important for both gamma-secretase assembly and substrate recruitment
J Neurochem (2012) 123, 837-844. PubMed Europe PubMed DOI
Parker,M.F., Barten,D.M., Bergstrom,C.P., Bronson,J.J., Corsa,J.A., Dee,M.F., Gai,Y., Guss,V.L., Higgins,M.A., Keavy,D.J., Loo,A., Mate,R.A., Marcin,L.R., McElhone,K.E., Polson,C.T., Roberts,S.B. and Macor,J.E.
2-(N-Benzyl-N-phenylsulfonamido)alkyl amide derivatives as gamma-secretase inhibitors
Bioorg Med Chem Lett (2012) 22, 6828-6831. PubMed Europe PubMed DOI I
Pettersson,M., Johnson,D.S., Subramanyam,C., Bales,K.R., Am Ende,C.W., Fish,B.A., Green,M.E., Kauffman,G.W., Lira,R., Mullins,P.B., Navaratnam,T., Sakya,S.M., Stiff,C.M., Tran,T.P., Vetelino,B.C., Xie,L., Zhang,L., Pustilnik,L.R., Wood,K.M. and O'Donnell,C.J.
Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active gamma-secretase modulators
Bioorg Med Chem Lett (2012) 22, 2906-2911. PubMed Europe PubMed DOI I
Rennhack,A., Jumpertz,T., Ness,J., Baches,S., Pietrzik,C.U., Weggen,S. and Bulic,B.
Synthesis of a potent photoreactive acidic gamma-secretase modulator for target identification in cells
Bioorg Med Chem (2012) 20, 6523-6532. PubMed Europe PubMed DOI
Rogers,K., Felsenstein,K.M., Hrdlicka,L., Tu,Z., Albayya,F., Lee,W., Hopp,S., Miller,M.J., Spaulding,D., Yang,Z., Hodgdon,H., Nolan,S., Wen,M., Costa,D., Blain,J.F., Freeman,E., De Strooper,B., Vulsteke,V., Scrocchi,L., Zetterberg,H., Portelius,E., Hutter-Paier,B., Havas,D., Ahlijanian,M., Flood,D., Leventhal,L., Shapiro,G., Patzke,H., Chesworth,R. and Koenig,G.
Modulation of gamma-secretase by EVP-0015962 reduces amyloid deposition and behavioral deficits in Tg2576 mice
Mol Neurodegener (2012) 7, 61-61. PubMed Europe PubMed DOI
St George-Hyslop,P. and Fraser,P.E.
Assembly of the presenilin gamma-/epsilon-secretase complex
J Neurochem (2012) 120 Suppl 1, 84-88. PubMed Europe PubMed DOI
Stepan,A.F., Subramanyam,C., Efremov,I.V., Dutra,J.K., O'Sullivan,T.J., Dirico,K.J., McDonald,W.S., Won,A., Dorff,P.H., Nolan,C.E., Becker,S.L., Pustilnik,L.R., Riddell,D.R., Kauffman,G.W., Kormos,B.L., Zhang,L., Lu,Y., Capetta,S.H., Green,M.E., Karki,K., Sibley,E., Atchison,K.P., Hallgren,A.J., Oborski,C.E., Robshaw,A.E., Sneed,B. and O'Donnell,C.J.
Application of the bicyclo[1.1.1]pentane motif as a nonclassical phenyl ring bioisostere in the design of a potent and orally active gamma-secretase inhibitor
J Med Chem (2012) 55, 3414-3424. PubMed Europe PubMed DOI I
Sun,Z.Y., Asberom,T., Bara,T., Bennett,C., Burnett,D., Chu,I., Clader,J., Cohen-Williams,M., Cole,D., Czarniecki,M., Durkin,J., Gallo,G., Greenlee,W., Josien,H., Huang,X., Hyde,L., Jones,N., Kazakevich,I., Li,H., Liu,X., Lee,J., MacCoss,M., Mandal,M.B., McCracken,T., Nomeir,A., Mazzola,R., Palani,A., Parker,E.M., Pissarnitski,D.A., Qin,J., Song,L., Terracina,G., Vicarel,M., Voigt,J., Xu,R., Zhang,L., Zhang,Q., Zhao,Z., Zhu,X. and Zhu,Z.
Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious gamma-secretase modulators in vivo
J Med Chem (2012) 55, 489-502. PubMed Europe PubMed DOI
Svedruzic,Z.M., Popovic,K., Smoljan,I. and Sendula-Jengic,V.
Modulation of gamma-secretase activity by multiple enzyme-substrate interactions: implications in pathogenesis of Alzheimer's disease
PLoS ONE (2012) 7, e32293-e32293. PubMed Europe PubMed DOI PMC EPMC
Takami,M. and Funamoto,S.
gamma-Secretase-Dependent Proteolysis of Transmembrane Domain of Amyloid Precursor Protein: Successive Tri- and Tetrapeptide Release in Amyloid beta-Protein Production
Int J Alzheimers Dis (2012) 2012, 591392-591392. PubMed Europe PubMed DOI PMC EPMC P
Takeo,K., Watanabe,N., Tomita,T. and Iwatsubo,T.
Contribution of the gamma-secretase subunits to the formation of catalytic pore of presenilin 1 protein
J Biol Chem (2012) 287, 25834-25843. PubMed Europe PubMed DOI
Tomita,T.
Structure-function relationship of gamma-secretase
Mol Neurodegener (2012) 7 Suppl 1, L5-L5. PMC EPMC
Wagner,S.L., Tanzi,R.E., Mobley,W.C. and Galasko,D.
Potential use of gamma-secretase modulators in the treatment of Alzheimer disease
Arch Neurol (2012) 69, 1255-1258. PubMed Europe PubMed DOI
Wanngren,J., Ottervald,J., Parpal,S., Portelius,E., Stromberg,K., Borgegard,T., Klintenberg,R., Jureus,A., Blomqvist,J., Blennow,K., Zetterberg,H., Lundkvist,J., Rosqvist,S. and Karlstrom,H.
Second generation gamma-secretase modulators exhibit different modulation of Notch beta and Abeta production
J Biol Chem (2012) 287, 32640-32650. PubMed Europe PubMed DOI I
Wolfe,M.S.
gamma-Secretase inhibitors and modulators for Alzheimer's disease
J Neurochem (2012) 120 Suppl 1, 89-98. PubMed Europe PubMed DOI V I
Wolfe,M.S.
Presenilin 1
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Wolfe,M.S.
Processive proteolysis by gamma-secretase and the mechanism of Alzheimer's disease
Biol Chem (2012) 393, 899-905. PubMed Europe PubMed DOI M
Wolfe,M.S.
gamma-Secretase as a target for Alzheimer's disease
Adv Pharmacol (2012) 64, 127-153. PubMed Europe PubMed DOI V
Wu,W.L., Domalski,M., Burnett,D.A., Josien,H., Bara,T., Rajagopalan,M., Xu,R., Clader,J., Greenlee,W.J., Brunskill,A., Hyde,L.A., Del Vecchio,R.A., Cohen-Williams,M.E., Song,L., Lee,J., Terracina,G., Zhang,Q., Nomeir,A., Parker,E.M. and Zhang,L.
Discovery of SCH 900229, a potent presenilin 1 selective gamma-secretase inhibitor for the treatment of Alzheimer's disease
ACS Med Chem Lett (2012) 3, 892-896. PubMed Europe PubMed DOI I
Zettl,H., Ness,J., Hahnke,V., Beher,D., Jumpertz,T., Saric,A., Baumann,K., Pietrzik,C.U., Bulic,B., Schneider,G. and Weggen,S.
Discovery of gamma-secretase modulators with a novel activity profile by text-based virtual screening
ACS Chem Biol (2012) 7, 1488-1495. PubMed Europe PubMed DOI

2011

Antonell,A., Balasa,M., Oliva,R., Llado,A., Bosch,B., Fabregat,N., Fortea,J., Molinuevo,J.L. and Sanchez-Valle,R.
A novel PSEN1 gene mutation (L235R) associated with familial early-onset Alzheimer's disease
Neurosci Lett (2011) 496, 40-42. PubMed Europe PubMed DOI M
Arcaroli,J.J., Dasari,A., Messersmith,W.A. and Jimeno,A.
gamma-Secretase inhibitors in solid tumor malignancies
Drugs Future (2011) 36, 677-689. DOI I
Aubele,D.L., Truong,A.P., Dressen,D.B., Probst,G.D., Bowers,S., Mattson,M.N., Semko,C.M., Sun,M., Garofalo,A.W., Konradi,A.W., Sham,H.L., Zmolek,W., Wong,K., Goldbach,E., Quinn,K.P., Sauer,J.M., Brigham,E.F., Wallace,W., Nguyen,L., Bova,M.P., Hemphill,S.S. and Basi,G.
Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent gamma-secretase inhibitors
Bioorg Med Chem Lett (2011) 21, 5791-5794. PubMed Europe PubMed DOI I
Barrett,P.J., Sanders,C.R., Kaufman,S.A., Michelsen,K. and Jordan,J.B.
NSAID-based gamma-secretase modulators do not bind to the amyloid-beta polypeptide
Biochemistry (2011) 50, 10328-10342. PubMed Europe PubMed DOI I
Barthet,G., Shioi,J., Shao,Z., Ren,Y., Georgakopoulos,A. and Robakis,N.K.
Inhibitors of gamma-secretase stabilize the complex and differentially affect processing of amyloid precursor protein and other substrates
FASEB J (2011) 25, 2937-2946. PubMed Europe PubMed DOI I
Blair,C.R., Stone,J.B. and Wells,R.G.
The type III TGF-beta receptor betaglycan transmembrane-cytoplasmic domain fragment is stable after ectodomain cleavage and is a substrate of the intramembrane protease gamma-secretase
Biochim Biophys Acta (2011) 1813, 332-339. PubMed Europe PubMed DOI I
Borgegard,T., Minidis,A., Jureus,A., Malmborg,J., Rosqvist,S., Gruber,S., Almqvist,H., Yan,H., Bogstedt,A., Olsson,F., Dahlstrom,J., Ray,C., Narhi,K., Malinowsky,D., Hagstrom,E., Jin,S., Malmberg,A., Lendahl,U. and Lundkvist,J.
In vivo analysis using a presenilin-1-specific inhibitor: presenilin1-containing lambda-secretase complexes mediate the majority of CNS Abeta production in the mouse
Alzheimer's Dis Res J (2011) 3, 29-45. I
Brodney,M.A., Auperin,D.D., Becker,S.L., Bronk,B.S., Brown,T.M., Coffman,K.J., Finley,J.E., Hicks,C.D., Karmilowicz,M.J., Lanz,T.A., Liston,D., Liu,X., Martin,B.A., Nelson,R.B., Nolan,C.E., Oborski,C.E., Parker,C.P., Richter,K.E., Pozdnyakov,N., Sahagan,B.G., Schachter,J.B., Sokolowski,S.A., Tate,B., Van Deusen,J.W., Wood,D.E. and Wood,K.M.
Diamide amino-imidazoles: a novel series of gamma-secretase inhibitors for the treatment of Alzheimer's disease
Bioorg Med Chem Lett (2011) 21, 2631-2636. PubMed Europe PubMed DOI I
Brodney,M.A., Auperin,D.D., Becker,S.L., Bronk,B.S., Brown,T.M., Coffman,K.J., Finley,J.E., Hicks,C.D., Karmilowicz,M.J., Lanz,T.A., Liston,D., Liu,X., Martin,B.A., Nelson,R.B., Nolan,C.E., Oborski,C.E., Parker,C.P., Richter,K.E., Pozdnyakov,N., Sahagan,B.G., Schachter,J.B., Sokolowski,S.A., Tate,B., Wood,D.E., Wood,K.M., Van Deusen,J.W. and Zhang,L.
Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as gamma-secretase inhibitors: discovery of PF-3084014
Bioorg Med Chem Lett (2011) 21, 2637-2640. PubMed Europe PubMed DOI I
Bulic,B., Ness,J., Hahn,S., Rennhack,A., Jumpertz,T. and Weggen,S.
Chemical biology, molecular mechanism and clinical perspective of gamma-secretase modulators in Alzheimer's disease
Curr Neuropharmacol (2011) 9, 598-622. PubMed Europe PubMed DOI V
Church,A., Prescott,J., Lillis,S., Rees,J., Chance,P., Williamson,K. and Morris,H.R.
A novel presenilin 1 mutation, I202F occurring at a previously predicted pathogenic site causing autosomal dominant Alzheimer's disease
Neurobiol Aging (2011) 32, 556-556. PubMed Europe PubMed DOI M
Crump,C.J., Fish,B.A., Castro,S.V., Chau,D.M., Gertsik,N., Ahn,K., Stiff,C., Pozdnyakov,N., Bales,K.R., Johnson,D.S. and Li,Y.M.
Piperidine acetic acid based gamma-secretase modulators directly bind to Presenilin-1
ACS Chem Neurosci (2011) 2, 705-710. PubMed Europe PubMed DOI PMC EPMC
Crump,C.J., Johnson,D.S. and Li,Y.M.
Target of gamma-secretase modulators, presenilin marks the spot
EMBO J (2011) 30, 4696-4698. PubMed Europe PubMed DOI
Ebke,A., Luebbers,T., Fukumori,A., Shirotani,K., Haass,C., Baumann,K. and Steiner,H.
Novel gamma-secretase enzyme modulators directly target presenilin protein
J Biol Chem (2011) 286, 37181-37186. PubMed Europe PubMed DOI
Haapasalo,A. and Kovacs,D.M.
The many substrates of presenilin/gamma-secretase
J Alzheimers Dis (2011) 25, 3-28. PubMed Europe PubMed DOI V
Hamblett,C.L., Shah,S., Heidebrecht,R. and Munoz,B.
gamma-Secretase inhibition: an overview of development of inhibitors for the treatment of Alzheimer's disease
Aspartic Acid Proteases as Therapeutic Targets (2011) 45, 353-390. DOI I
Han,W., Ji,T., Wang,L., Yan,L., Wang,H., Luo,Z., Mei,B. and Su,J.
Abnormalities in periodontal and salivary tissues in conditional presenilin 1 and presenilin 2 double knockout mice
Mol Cell Biochem (2011) 347, 13-20. PubMed Europe PubMed DOI K
Ho,A. and Shen,J.
Presenilins in synaptic function and disease
Trends Mol Med (2011) 17, 617-624. PubMed Europe PubMed DOI V
Imbimbo,B.P. and Giardina,G.A.
gamma-Secretase inhibitors and modulators for the treatment of Alzheimer's disease: disappointments and hopes
Curr Top Med Chem (2011) 11, 1555-1570. PubMed Europe PubMed DOI V I
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The gamma-secretase modulator CHF5074 reduces the accumulation of native hyperphosphorylated tau in a transgenic mouse model of Alzheimer's disease
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Presenilin-1 mutation Alzheimer's disease: a genetic epilepsy syndrome?
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Identification of presenilin 1-selective gamma-secretase inhibitors with reconstituted gamma-secretase complexes
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Lleo,A. and Saura,C.A.
gamma-Secretase substrates and their implications for drug development in Alzheimer's disease
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Lubbers,T., Flohr,A., Jolidon,S., David-Pierson,P., Jacobsen,H., Ozmen,L. and Baumann,K.
Aminothiazoles as gamma-secretase modulators
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Lundkvist,J. and Lendahl,U.
gamma-Secretase: an unusual enzyme with many possible disease targets, including Alzheimer's disease
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Presenilins mediate efficient proteolysis via the autophagosome-lysosome system
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Amino-caprolactam gamma-secretase inhibitors showing potential for the treatment of Alzheimer's disease
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Oehlrich,D., Berthelot,D.J. and Gijsen,H.J.
gamma-Secretase modulators as potential disease modifying anti-Alzheimer's drugs
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Phenylpiperidine-type gamma-secretase modulators target the transmembrane domain 1 of presenilin 1
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Panza,F., Frisardi,V., Solfrizzi,V., Imbimbo,B.P., Logroscino,G., Santamato,A., Greco,A., Seripa,D. and Pilotto,A.
Interacting with gamma-secretase for treating Alzheimer's disease: from inhibition to modulation
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Peng,H., Talreja,T., Xin,Z., Cuervo,J.H., Kumaravel,G., Humora,M.J., Xu,L., Rohde,E., Gan,L., Jung,M.Y., Shackett,M.N., Chollate,S., Dunah,A.W., Snodgrass-Belt,P.A., Arnold,H.M., Taveras,A.G., Rhodes,K.J. and Scannevin,R.H.
Discovery of BIIB042, a potent, selective, and orally bioavailable gamma-secretase modulator
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Variant Alzheimer disease with spastic paraparesis: a rare presenilin-1 mutation
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Novel gamma-secretase modulators: a review of patents from 2008 to 2010
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Dissociation between the processivity and total activity of gamma-secretase: implications for the mechanism of Alzheimer's disease-causing presenilin mutations
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Structure of gamma-secretase and its trimeric pre-activation intermediate by single-particle electron microscopy
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Saura,C.A., Servian-Morilla,E. and Scholl,F.G.
Presenilin/gamma-secretase regulates neurexin processing at synapses
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Scholl,M., Almkvist,O., Axelman,K., Stefanova,E., Wall,A., Westman,E., Langstrom,B., Lannfelt,L., Graff,C. and Nordberg,A.
Glucose metabolism and PIB binding in carriers of a His163Tyr presenilin 1 mutation
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Stepan,A.F., Karki,K., McDonald,W.S., Dorff,P.H., Dutra,J.K., Dirico,K.J., Won,A., Subramanyam,C., Efremov,I.V., O'Donnell,C.J., Nolan,C.E., Becker,S.L., Pustilnik,L.R., Sneed,B., Sun,H., Lu,Y., Robshaw,A.E., Riddell,D., O'Sullivan,T.J., Sibley,E., Capetta,S., Atchison,K., Hallgren,A.J., Miller,E., Wood,A. and Obach,R.S.
Metabolism-directed design of oxetane-containing arylsulfonamide derivatives as gamma-secretase inhibitors
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Su,J., Tang,H. and McKittrick,B.A.
Stereoselective synthesis of C-6 hydroxy tricyclic sulfone as a gamma-secretase inhibitor
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Synthesis and SAR study of tricyclic sulfones as gamma-secretase inhibitors: C-6 and C-8 positions
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Van Broeck,B., Chen,J.M., Treton,G., Desmidt,M., Hopf,C., Ramsden,N., Karran,E., Mercken,M. and Rowley,A.
Chronic treatment with a novel gamma-secretase modulator, JNJ-40418677, inhibits amyloid plaque formation in a mouse model of Alzheimer's disease
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Clinical phenotype of G206D mutation in the presenilin 1 gene in pathologically confirmed familial Alzheimer's disease
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SAR of tricyclic sulfones as gamma-secretase inhibitors
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Comparison of presenilin 1 and presenilin 2 gamma-secretase activities using a yeast reconstitution system
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Presenilin-based transgenic models of Alzheimer's dementia
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Zhu,Y., Obregon,D., Hou,H., Giunta,B., Erhart,J., Fernandez,F., Mori,T., Nikolic,W., Zhao,Y., Morgan,D., Town,T. and Tan,J.
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2010

Ahn,K., Shelton,C.C., Tian,Y., Zhang,X., Gilchrist,M.L., Sisodia,S.S. and Li,Y.M.
Activation and intrinsic gamma-secretase activity of presenilin 1
Proc Natl Acad Sci U S A (2010) 107, 21435-21440. PubMed Europe PubMed DOI
Augelli-Szafran,C.E., Wei,H.X., Lu,D., Zhang,J., Gu,Y., Yang,T., Osenkowski,P., Ye,W. and Wolfe,M.S.
Discovery of Notch-sparing gamma-secretase inhibitors
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Basi,G.S., Hemphill,S., Brigham,E.F., Liao,A., Aubele,D.L., Baker,J., Barbour,R., Bova,M., Chen,X.H., Dappen,M.S., Eichenbaum,T., Goldbach,E., Hawkinson,J., Lawler Herbold,R., Hu,K., Hui,T., Jagodzinski,J.J., Keim,P.S., Kholodenko,D., Latimer,L.H., Lee,M., Marugg,J., Mattson,M.N., McCauley,S., Miller,J.L., Motter,R., Mutter,L., Neitzel,M.L., Ni,H., Nguyen,L., Quinn,K., Ruslim,L., Semko,C.M., Shapiro,P., Smith,J., Soriano,F., Szoke,B., Tanaka,K., Tang,P., Tucker,J.A., Ye,X.M., Yu,M., Wu,J., Zu,Y.Z., Garofalo,A.W., Sauer,J.M., Konradi,A.W., Ness,D., Shopp,G., Pleiss,M.A., Freedman,S.B. and Schenk,D.
Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease
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Behbahani,H., Pavlov,P.F., Wiehager,B., Nishimura,T., Winblad,B. and Ankarcrona,M.
Association of Omi/HtrA2 with gamma-secretase in mitochondria
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Bergmans,B.A. and De Strooper,B.
gamma-Secretases: from cell biology to therapeutic strategies
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Boyles,R.S., Lantz,K.M., Poertner,S., Georges,S.J. and Andres,A.J.
Presenilin controls CBP levels in the adult Drosophila central nervous system
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Bruni,A.C., Bernardi,L., Colao,R., Rubino,E., Smirne,N., Frangipane,F., Terni,B., Curcio,S.A., Mirabelli,M., Clodomiro,A., Di Lorenzo,R., Maletta,R., Anfossi,M., Gallo,M., Geracitano,S., Tomaino,C., Muraca,M.G., Leotta,A., Lio,S.G., Pinessi,L., Rainero,I., Sorbi,S., Nee,L., Milan,G., Pappata,S., Postiglione,A., Abbamondi,N., Forloni,G., St George Hyslop,P., Rogaeva,E., Bugiani,O., Giaccone,G., Foncin,J.F., Spillantini,M.G. and Puccio,G.
Worldwide distribution of PSEN1 Met146Leu mutation: a large variability for a founder mutation
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Caldwell,J.P., Bennett,C.E., McCracken,T.M., Mazzola,R.D., Bara,T., Buevich,A., Burnett,D.A., Chu,I., Cohen-Williams,M., Josein,H., Hyde,L., Lee,J., McKittrick,B., Song,L., Terracina,G., Voigt,J., Zhang,L. and Zhu,Z.
Iminoheterocycles as gamma-secretase modulators
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Coen,K. and Annaert,W.
Presenilins: how much more than gamma-secretase?!
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Czerwinski,A., Valenzuela,F., Afonine,P., Dauter,M. and Dauter,Z.
N-{N-[2-(3,5-Difluorophenyl)acetyl]-(S)-alanyl}-(S)-phenylglycine tert-butyl ester (DAPT): an inhibitor of gamma-secretase, revealing fine electronic and hydrogen-bonding features
Acta Crystallogr C (2010) 66, o585-o588. PubMed Europe PubMed DOI I
De Strooper,B., Vassar,R. and Golde,T.
The secretases: enzymes with therapeutic potential in Alzheimer disease
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De Strooper,B. and Annaert,W.
Novel research horizons for presenilins and gamma-secretases in cell biology and disease
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Elder,G.A., Gama Sosa,M.A., De Gasperi,R., Dickstein,D.L. and Hof,P.R.
Presenilin transgenic mice as models of Alzheimer's disease
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Masking of transmembrane-based retention signals controls ER export of gamma-secretase
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Franberg,J., Karlstrom,H., Winblad,B., Tjernberg,L.O. and Frykman,S.
gamma-Secretase dependent production of intracellular domains is reduced in adult compared to embryonic rat brain membranes
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Frykman,S., Hur,J.Y., Franberg,J., Aoki,M., Winblad,B., Nahalkova,J., Behbahani,H. and Tjernberg,L.O.
Synaptic and endosomal localization of active gamma-secretase in rat brain
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Fukumori,A., Fluhrer,R., Steiner,H. and Haass,C.
Three-amino acid spacing of presenilin endoproteolysis suggests a general stepwise cleavage of gamma-secretase-mediated intramembrane proteolysis
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Gama Sosa,M.A., Gasperi,R.D., Rocher,A.B., Wang,A.C., Janssen,W.G., Flores,T., Perez,G.M., Schmeidler,J., Dickstein,D.L., Hof,P.R. and Elder,G.A.
Age-related vascular pathology in transgenic mice expressing presenilin 1-associated familial Alzheimer's disease mutations
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Gomez-Tortosa,E., Barquero,S., Baron,M., Gil-Neciga,E., Castellanos,F., Zurdo,M., Manzano,S., Munoz,D.G., Jimenez-Huete,A., Rabano,A., Sainz,M.J., Guerrero,R., Gobernado,I., Perez-Perez,J. and Jimenez-Escrig,A.
Clinical-genetic correlations in familial Alzheimer's disease caused by presenilin 1 mutations
J Alzheimers Dis (2010) 19, 873-884. PubMed Europe PubMed DOI M
Gong,P., Vetrivel,K.S., Nguyen,P.D., Meckler,X., Cheng,H., Kounnas,M.Z., Wagner,S.L., Parent,A.T. and Thinakaran,G.
Mutation analysis of the presenilin 1 N-terminal domain reveals a broad spectrum of gamma-secretase activity toward amyloid precursor protein and other substrates
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Hall,A., Elliott,R.L., Giblin,G.M., Hussain,I., Musgrave,J., Naylor,A., Sasse,R. and Smith,B.
Piperidine-derived gamma-secretase modulators
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He,G., Luo,W., Li,P., Remmers,C., Netzer,W.J., Hendrick,J., Bettayeb,K., Flajolet,M., Gorelick,F., Wennogle,L.P. and Greengard,P.
Gamma-secretase activating protein is a therapeutic target for Alzheimer's disease
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Heilig,E.A., Xia,W., Shen,J. and Kelleher,R.J., III
A presenilin-1 mutation identified in familial Alzheimer disease with cotton wool plaques causes a nearly complete loss of gamma-secretase activity
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Hieke,M., Ness,J., Steri,R., Dittrich,M., Greiner,C., Werz,O., Baumann,K., Schubert-Zsilavecz,M., Weggen,S. and Zettl,H.
Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity
J Med Chem (2010) 53, 4691-4700. PubMed Europe PubMed DOI
Huang,X., Aslanian,R., Zhou,W., Zhu,X., Qin,J., Greenlee,W., Zhu,Z., Zhang,L., Hyde,L., Chu,I., Cohen-Williams,M. and Palani,A.
The discovery of pyridone and pyridazone heterocycles as gamma-secretase modulators
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Imbimbo,B.P., Giardino,L., Sivilia,S., Giuliani,A., Gusciglio,M., Pietrini,V., Del Giudice,E., D'Arrigo,A., Leon,A., Villetti,G. and Calza,L.
CHF5074, a novel gamma-secretase modulator, restores hippocampal neurogenesis potential and reverses contextual memory deficit in a transgenic mouse model of Alzheimer's disease
J Alzheimers Dis (2010) 20, 159-173. PubMed Europe PubMed DOI I
Jorissen,E. and De Strooper,B.
Gamma-secretase and the intramembrane proteolysis of Notch
Curr Top Dev Biol (2010) 92, 201-230. PubMed Europe PubMed DOI V
Kelleher,R.J., III and Shen,J.
Genetics. Gamma-secretase and human disease
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Kim,H.J., Kim,H.Y., Ki,C.S. and Kim,S.H.
Presenilin 1 gene mutation (M139I) in a patient with an early-onset Alzheimer's disease: clinical characteristics and genetic identification
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Kounnas,M.Z., Danks,A.M., Cheng,S., Tyree,C., Ackerman,E., Zhang,X., Ahn,K., Nguyen,P., Comer,D., Mao,L., Yu,C., Pleynet,D., Digregorio,P.J., Velicelebi,G., Stauderman,K.A., Comer,W.T., Mobley,W.C., Li,Y.M., Sisodia,S.S., Tanzi,R.E. and Wagner,S.L.
Modulation of gamma-secretase reduces beta-amyloid deposition in a transgenic mouse model of Alzheimer's disease
Neuron (2010) 67, 769-780. PubMed Europe PubMed DOI
Kurosumi,M., Nishio,Y., Osawa,S., Kobayashi,H., Iwatsubo,T., Tomita,T. and Miyachi,H.
Novel Notch-sparing gamma-secretase inhibitors derived from a peroxisome proliferator-activated receptor agonist library
Bioorg Med Chem Lett (2010) 20, 5282-5285. PubMed Europe PubMed DOI I
Lanz,T.A., Wood,K.M., Richter,K.E., Nolan,C.E., Becker,S.L., Pozdnyakov,N., Martin,B.A., Du,P., Oborski,C.E., Wood,D.E., Brown,T.M., Finley,J.E., Sokolowski,S.A., Hicks,C.D., Coffman,K.J., Geoghegan,K.F., Brodney,M.A., Liston,D. and Tate,B.
Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014
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Lee,J.H., Yu,W.H., Kumar,A., Lee,S., Mohan,P.S., Peterhoff,C.M., Wolfe,D.M., Martinez-Vicente,M., Massey,A.C., Sovak,G., Uchiyama,Y., Westaway,D., Cuervo,A.M. and Nixon,R.A.
Lysosomal proteolysis and autophagy require presenilin 1 and are disrupted by Alzheimer-related PS1 mutations
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Lessard,C.B., Wagner,S.L. and Koo,E.H.
And four equals one: presenilin takes the gamma-secretase role by itself
Proc Natl Acad Sci U S A (2010) 107, 21236-21237. PubMed Europe PubMed DOI
Li,H., Xu,R., Cole,D., Clader,J.W., Greenlee,W.J., Nomeir,A.A., Song,L. and Zhang,L.
Design, synthesis, and structure-activity relationship studies of N-arylsulfonyl morpholines as gamma-secretase inhibitors
Bioorg Med Chem Lett (2010) 20, 6606-6609. PubMed Europe PubMed DOI I
Llado,A., Sanchez-Valle,R., Rey,M.J., Mercadal,P., Almenar,C., Lopez-Villegas,D., Fortea,J. and Molinuevo,J.L.
[New mutation in the PSEN1 (E120G) gene associated with early onset Alzheimer's disease]
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Mattson,M.N., Neitzel,M.L., Quincy,D.A., Semko,C.M., Garofalo,A.W., Keim,P.S., Konradi,A.W., Pleiss,M.A., Sham,H.L., Brigham,E.F., Goldbach,E.G., Zhang,H., Sauer,J.M. and Basi,G.S.
Discovery of sulfonamide-pyrazole gamma-secretase inhibitors
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Mitsuishi,Y., Hasegawa,H., Matsuo,A., Araki,W., Suzuki,T., Tagami,S., Okochi,M., Takeda,M., Roepman,R. and Nishimura,M.
Human CRB2 inhibits gamma-secretase cleavage of amyloid precursor protein by binding to the presenilin complex
J Biol Chem (2010) 285, 14920-14931. PubMed Europe PubMed DOI
Panza,F., Frisardi,V., Imbimbo,B.P., Capurso,C., Logroscino,G., Sancarlo,D., Seripa,D., Vendemiale,G., Pilotto,A. and Solfrizzi,V.
Review: gamma-secretase inhibitors for the treatment of Alzheimer's disease: the current state
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Perez-Revuelta,B.I., Fukumori,A., Lammich,S., Yamasaki,A., Haass,C. and Steiner,H.
Requirement for small side chain residues within the GxGD-motif of presenilin for gamma-secretase substrate cleavage
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Placanica,L., Chien,J.W. and Li,Y.M.
Characterization of an atypical gamma-secretase complex from hematopoietic origin
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Rivkin,A., Ahearn,S.P., Chichetti,S.M., Kim,Y.R., Li,C., Rosenau,A., Kattar,S.D., Jung,J., Shah,S., Hughes,B.L., Crispino,J.L., Middleton,R.E., Szewczak,A.A., Munoz,B. and Shearman,M.S.
Piperazinyl pyrimidine derivatives as potent gamma-secretase modulators
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Rivkin,A., Ahearn,S.P., Chichetti,S.M., Hamblett,C.L., Garcia,Y., Martinez,M., Hubbs,J.L., Reutershan,M.H., Daniels,M.H., Siliphaivanh,P., Otte,K.M., Li,C., Rosenau,A., Surdi,L.M., Jung,J., Hughes,B.L., Crispino,J.L., Nikov,G.N., Middleton,R.E., Moxham,C.M., Szewczak,A.A., Shah,S., Moy,L.Y., Kenific,C.M., Tanga,F., Cruz,J.C., Andrade,P., Angagaw,M.H., Shomer,N.H., Miller,T., Munoz,B. and Shearman,M.S.
Purine derivatives as potent gamma-secretase modulators
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Ross,J.S. and Imbimbo,B.P.
Are gamma-secretase inhibitors detrimental for Alzheimer's disease patients?
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Sasikumar,T.K., Qiang,L., Burnett,D.A., Cole,D., Xu,R., Li,H., Greenlee,W.J., Clader,J., Zhang,L. and Hyde,L.
Tricyclic sulfones as orally active gamma-secretase inhibitors: synthesis and structure-activity relationship studies
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Sasikumar,T.K., Burnett,D.A., Asberom,T., Wu,W.L., Bennett,C., Cole,D., Xu,R., Greenlee,W.J., Clader,J., Zhang,L. and Hyde,L.
Tetracyclic sulfones as potent gamma-secretase inhibitors: synthesis and structure-activity relationship studies
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Small,D.H., Klaver,D.W. and Foa,L.
Presenilins and the gamma-secretase: still a complex problem
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Sobhanifar,S., Schneider,B., Lohr,F., Gottstein,D., Ikeya,T., Mlynarczyk,K., Pulawski,W., Ghoshdastider,U., Kolinski,M., Filipek,S., Guntert,P., Bernhard,F. and Dotsch,V.
Structural investigation of the C-terminal catalytic fragment of presenilin 1
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St George-Hyslop,P. and Schmitt-Ulms,G.
Alzheimer's disease: selectively tuning gamma-secretase
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Fluorinated piperidine acetic acids as gamma-secretase modulators
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Stempfle,D., Kanwar,R., Loewer,A., Fortini,M.E. and Merdes,G.
In vivo reconstitution of gamma-secretase in Drosophila results in substrate specificity
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Takagi,S., Tominaga,A., Sato,C., Tomita,T. and Iwatsubo,T.
Participation of transmembrane domain 1 of presenilin 1 in the catalytic pore structure of the gamma-secretase
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Teng,L., Zhao,J., Wang,F., Ma,L. and Pei,G.
A GPCR/secretase complex regulates beta- and gamma-secretase specificity for Abeta production and contributes to AD pathogenesis
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Teranishi,Y., Hur,J.Y., Welander,H., Franberg,J., Aoki,M., Winblad,B., Frykman,S. and Tjernberg,L.O.
Affinity pulldown of gamma-secretase and associated proteins from human and rat brain
J Cell Mol Med (2010) 14, 2675-2686. PubMed Europe PubMed DOI
Tian,Y., Bassit,B., Chau,D. and Li,Y.M.
An APP inhibitory domain containing the Flemish mutation residue modulates gamma-secretase activity for Abeta production
Nat Struct Mol Biol (2010) 17, 151-158. PubMed Europe PubMed DOI
Uemura,K., Farner,K.C., Hashimoto,T., Nasser-Ghodsi,N., Wolfe,M.S., Koo,E.H., Hyman,B.T. and Berezovska,O.
Substrate docking to gamma-secretase allows access of gamma-secretase modulators to an allosteric site
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Verkhratsky,A. and Rodriguez,J.J.
The Achilles heel of gamma-secretase: can we contain Alzheimer's disease by reducing synthesis of beta-amyloid?
Acta Pharmacol Sin (2010) 31, 1407-1408. PubMed Europe PubMed DOI
Wanngren,J., Franberg,J., Svensson,A.I., Laudon,H., Olsson,F., Winblad,B., Liu,F., Naslund,J., Lundkvist,J. and Karlstrom,H.
The large hydrophilic loop of presenilin 1 is important for regulating gamma-secretase complex assembly and dictating the amyloid beta peptide (Abeta) profile without affecting Notch processing
J Biol Chem (2010) 285, 8527-8536. PubMed Europe PubMed DOI
Watanabe,N., Image Image,I.I., Takagi,S., Image Image,I.I., Tominaga,A., Image Image,I., Tomita,T., Image Image,I.I., Iwatsubo,T. and Image Image,I.
Functional analysis of the transmembrane domains of presenilin 1: participation of transmembrane domains 2 and 6 in the formation of initial substrate-binding site of gamma-secretase
J Biol Chem (2010) 285, 19738-19746. PubMed Europe PubMed DOI
Wei,P., Walls,M., Qiu,M., Ding,R., Denlinger,R.H., Wong,A., Tsaparikos,K., Jani,J.P., Hosea,N., Sands,M., Randolph,S. and Smeal,T.
Evaluation of selective gamma-secretase inhibitor PF-03084014 for its antitumor efficacy and gastrointestinal safety to guide optimal clinical trial design
Mol Cancer Ther (2010) 9, 1618-1628. PubMed Europe PubMed DOI I
Weyand,N.J., Calton,C.M., Higashi,D.L., Kanack,K.J. and So,M.
Presenilin/gamma-secretase cleaves CD46 in response to Neisseria infection
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Wines-Samuelson,M., Schulte,E.C., Smith,M.J., Aoki,C., Liu,X., Kelleher,R.J., III and Shen,J.
Characterization of age-dependent and progressive cortical neuronal degeneration in presenilin conditional mutant mice
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Wolfe,M.S.
Structure, mechanism and inhibition of gamma-secretase and presenilin-like proteases
Biol Chem (2010) 391, 839-847. PubMed Europe PubMed DOI V
Wu,F., Schweizer,C., Rudinskiy,N., Taylor,D.M., Kazantsev,A., Luthi-Carter,R. and Fraering,P.C.
Novel gamma-secretase inhibitors uncover a common nucleotide-binding site in JAK3, SIRT2, and PS1
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Xu,R., Cole,D., Asberom,T., Bara,T., Bennett,C., Burnett,D.A., Clader,J., Domalski,M., Greenlee,W., Hyde,L., Josien,H., Li,H., McBriar,M., McKittrick,B., McPhail,A.T., Pissarnitski,D., Qiang,L., Rajagopalan,M., Sasikumar,T., Su,J., Tang,H., Wu,W.L., Zhang,L. and Zhao,Z.
Design and synthesis of tricyclic sulfones as gamma-secretase inhibitors with greatly reduced Notch toxicity
Bioorg Med Chem Lett (2010) 20, 2591-2596. PubMed Europe PubMed DOI I
Ye,X.M., Konradi,A.W., Smith,J., Xu,Y.Z., Dressen,D., Garofalo,A.W., Marugg,J., Sham,H.L., Truong,A.P., Jagodzinski,J., Pleiss,M., Zhang,H., Goldbach,E., Sauer,J.M., Brigham,E., Bova,M. and Basi,G.S.
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors
Bioorg Med Chem Lett (2010) 20, 2195-2199. PubMed Europe PubMed DOI I
Ye,X.M., Konradi,A.W., Smith,J., Aubele,D.L., Garofalo,A.W., Marugg,J., Neitzel,M.L., Semko,C.M., Sham,H.L., Sun,M., Truong,A.P., Wu,J., Zhang,H., Goldbach,E., Sauer,J.M., Brigham,E.F., Bova,M. and Basi,G.S.
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors (Part II)
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Zhang,C., Browne,A., Kim,D.Y. and Tanzi,R.E.
Familial Alzheimer's disease mutations in presenilin 1 do not alter levels of the secreted amyloid-beta protein precursor generated by beta-secretase cleavage
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Zhang,Y.W. and Xu,H.
Substrate check of gamma-secretase
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Zhao,G., Liu,Z., Ilagan,M.X. and Kopan,R.
gamma-Secretase composed of PS1/Pen2/Aph1a can cleave Notch and amyloid precursor protein in the absence of nicastrin
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Zhou,H., Zhou,S., Walian,P.J. and Jap,B.K.
Dependency of gamma-secretase complex activity on the structural integrity of the bilayer
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2009

Baumann,S., Hottecke,N., Schubenel,R., Baumann,K. and Schmidt,B.
NSAID-derived gamma-secretase modulators. Part III: membrane anchoring
Bioorg Med Chem Lett (2009) 19, 6986-6990. PubMed Europe PubMed DOI I
Belbin,O., Beaumont,H., Warden,D., Smith,A.D., Kalsheker,N. and Morgan,K.
PSEN1 polymorphisms alter the rate of cognitive decline in sporadic Alzheimer's disease patients
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Bloch,L., Sineshchekova,O., Reichenbach,D., Reiss,K., Saftig,P., Kuro-o,M. and Kaether,C.
Klotho is a substrate for alpha-, beta- and gamma-secretase
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Bowers,S., Probst,G.D., Truong,A.P., Hom,R.K., Konradi,A.W., Sham,H.L., Garofalo,A.W., Wong,K., Goldbach,E., Quinn,K.P., Sauer,J.M., Wallace,W., Nguyen,L., Hemphill,S.S., Bova,M.P. and Basi,G.S.
N-Bridged bicyclic sulfonamides as inhibitors of gamma-secretase
Bioorg Med Chem Lett (2009) 19, 6952-6956. PubMed Europe PubMed DOI I
Cole,D.C., Stock,J.R., Kreft,A.F., Antane,M., Aschmies,S.H., Atchison,K.P., Casebier,D.S., Comery,T.A., Diamantidis,G., Ellingboe,J.W., Harrison,B.L., Hu,Y., Jin,M., Kubrak,D.M., Lu,P., Mann,C.W., Martone,R.L., Moore,W.J., Oganesian,A., Riddell,D.R., Sonnenberg-Reines,J., Sun,S.C., Wagner,E., Wang,Z., Woller,K.R., Xu,Z., Zhou,H. and Jacobsen,J.S.
(S)-N-(5-Chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol a Notch-1-sparing gamma-secretase inhibitor
Bioorg Med Chem Lett (2009) 19, 926-929. PubMed Europe PubMed DOI I
Cuc,H.T., Seo,J.B., Choi,J.K., Kim,W.T., Park,S.J., Lee,D.W., Kim,Y.S., Fortini,M.E. and Koh,Y.H.
Generation and characterization of monoclonal antibodies specific to Drosophila presenilin
Hybridoma (Larchmt) (2009) 28, 215-220. PubMed Europe PubMed DOI
Dries,D.R., Shah,S., Han,Y.H., Yu,C., Yu,S., Shearman,M.S. and Yu,G.
Glu-333 of nicastrin directly participates in gamma-secretase activity
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Foveau,B., Ancot,F., Leroy,C., Petrelli,A., Reiss,K., Vingtdeux,V., Giordano,S., Fafeur,V. and Tulasne,D.
Down-regulation of the Met receptor tyrosine kinase by presenilin-dependent regulated intramembrane proteolysis
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Futai,E., Yagishita,S. and Ishiura,S.
Nicastrin is dispensable for gamma-secretase protease activity in the presence of specific presenilin mutations
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Ha,Y.
Structure and mechanism of intramembrane protease
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Hamaguchi,T., Morinaga,A., Tsukie,T., Kuwano,R. and Yamada,M.
A novel presenilin 1 mutation (L282F) in familial Alzheimer's disease
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Hass,M.R., Sato,C., Kopan,R. and Zhao,G.
Presenilin: RIP and beyond
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Holloway,M.K., Hunt,P. and McGaughey,G.B.
Structure and modeling in the design of beta- and gamma-secretase inhibitors
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Imamura,Y., Watanabe,N., Umezawa,N., Iwatsubo,T., Kato,N., Tomita,T. and Higuchi,T.
Inhibition of gamma-secretase activity by helical beta-peptide foldamers
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Imbimbo,B.P., Hutter-Paier,B., Villetti,G., Facchinetti,F., Cenacchi,V., Volta,R., Lanzillotta,A., Pizzi,M. and Windisch,M.
CHF5074, a novel gamma-secretase modulator, attenuates brain beta-amyloid pathology and learning deficit in a mouse model of Alzheimer's disease
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Inoue,E., Deguchi-Tawarada,M., Togawa,A., Matsui,C., Arita,K., Katahira-Tayama,S., Sato,T., Yamauchi,E., Oda,Y. and Takai,Y.
Synaptic activity prompts gamma-secretase-mediated cleavage of EphA4 and dendritic spine formation
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Jiang,X., Zhang,D., Shi,J., Chen,Y., Zhang,P. and Mei,B.
Increased inflammatory response both in brain and in periphery in presenilin 1 and presenilin 2 conditional double knock-out mice
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Josien,H., Bara,T., Rajagopalan,M., Clader,J.W., Greenlee,W.J., Favreau,L., Hyde,L.A., Nomeir,A.A., Parker,E.M., Song,L., Zhang,L. and Zhang,Q.
Novel orally active morpholine N-arylsulfonamides gamma-secretase inhibitors with low CYP 3A4 liability
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Julian,J., Dharmaraj,N. and Carson,D.D.
MUC1 is a substrate for gamma-secretase
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Kang,J.H., Kim,B.S., Uhm,T.G., Lee,S.H., Lee,G.R., Park,C.S. and Chung,I.Y.
gamma-Secretase inhibitor reduces allergic pulmonary inflammation by modulating Th1 and Th2 responses
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Keown,L.E., Collins,I., Cooper,L.C., Harrison,T., Madin,A., Mistry,J., Reilly,M., Shaimi,M., Welch,C.J., Clarke,E.E., Lewis,H.D., Wrigley,J.D., Best,J.D., Murray,F. and Shearman,M.S.
Novel orally bioavailable gamma-secretase inhibitors with excellent in vivo activity
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Kopan,R. and Ilagan,M.X.
The canonical Notch signaling pathway: unfolding the activation mechanism
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Kreft,A.F., Martone,R. and Porte,A.
Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease
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Krishnaswamy,S., Verdile,G., Groth,D., Kanyenda,L. and Martins,R.N.
The structure and function of Alzheimer's gamma secretase enzyme complex
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Genotype-phenotype relationships of presenilin-1 mutations in Alzheimer's disease: an update
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Toward structural elucidation of the gamma-secretase complex
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Accurate determination of carboxyl-terminal fragment of presenilin 1 in various tissues from rat and cell lines
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Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties
Cancer Res (2009) 69, 7672-7680. PubMed Europe PubMed DOI I
McCarthy,J.V., Twomey,C. and Wujek,P.
Presenilin-dependent regulated intramembrane proteolysis and gamma-secretase activity
Cell Mol Life Sci (2009) 66, 1534-1555. PubMed Europe PubMed DOI V
McLeod,J., Curtis,N., Lewis,H.D., Good,M.A., Fagan,M.J. and Genever,P.G.
Gamma-secretase-dependent cleavage of amyloid precursor protein regulates osteoblast behavior
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Minogue,A.M., Stubbs,A.K., Frigerio,C.S., Boland,B., Fadeeva,J.V., Tang,J., Selkoe,D.J. and Walsh,D.M.
gamma-Secretase processing of APLP1 leads to the production of a p3-like peptide that does not aggregate and is not toxic to neurons
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Newman,M., Tucker,B., Nornes,S., Ward,A. and Lardelli,M.
Altering presenilin gene activity in zebrafish embryos causes changes in expression of genes with potential involvement in Alzheimer's disease pathogenesis
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Osenkowski,P., Li,H., Ye,W., Li,D., Aeschbach,L., Fraering,P.C., Wolfe,M.S., Selkoe,D.J. and Li,H.
Cryoelectron microscopy structure of purified gamma-secretase at 12 A resolution
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Placanica,L., Tarassishin,L., Yang,G., Peethumnongsin,E., Kim,S.H., Zheng,H., Sisodia,S.S. and Li,Y.M.
Pen2 and presenilin-1 modulate the dynamic equilibrium of presenilin-1 and presenilin-2 gamma-secretase complexes
J Biol Chem (2009) 284, 2967-2977. PubMed Europe PubMed DOI PMC EPMC
Pu,J., Kreft,A.F., Aschmies,S.H., Atchison,K.P., Berkowitz,J., Caggiano,T.J., Chlenov,M., Diamantidis,G., Harrison,B.L., Hu,Y., Huryn,D., Steven Jacobsen,J., Jin,M., Lipinski,K., Lu,P., Martone,R.L., Morris,K., Sonnenberg-Reines,J., Riddell,D.R., Sabalski,J., Sun,S.C., Wagner,E., Wang,Y., Xu,Z., Zhou,H. and Resnick,L.
Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors
Bioorg Med Chem (2009) 17, 4708-4717. PubMed Europe PubMed DOI I
Rao,S.S., O'Neil,J., Liberator,C.D., Hardwick,J.S., Dai,X., Zhang,T., Tyminski,E., Yuan,J., Kohl,N.E., Richon,V.M., Van der Ploeg,L.H., Carroll,P.M., Draetta,G.F., Look,A.T., Strack,P.R. and Winter,C.G.
Inhibition of Notch signaling by gamma secretase inhibitor engages the RB pathway and elicits cell cycle exit in T-cell acute lymphoblastic leukemia cells
Cancer Res (2009) 69, 3060-3068. PubMed Europe PubMed DOI T I
Sala Frigerio,C., Kukar,T.L., Fauq,A., Engel,P.C., Golde,T.E. and Walsh,D.M.
An NSAID-like compound, FT-9, preferentially inhibits gamma-secretase cleavage of the amyloid precursor protein compared to its effect on amyloid precursor-like protein 1
Biochemistry (2009) 48, 10894-10904. PubMed Europe PubMed DOI I
Sammi,T., Silakari,O. and Ravikumar,M.
Three-dimensional quantitative structure-activity relationship (3D-QSAR) studies of various benzodiazepine analogues of gamma-secretase inhibitors
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Shelton,C.C., Tian,Y., Shum,D., Radu,C., Djaballah,H. and Li,Y.M.
A miniaturized 1536-well format gamma-secretase assay
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Shelton,C.C., Zhu,L., Chau,D., Yang,L., Wang,R., Djaballah,H., Zheng,H. and Li,Y.M.
Modulation of gamma-secretase specificity using small molecule allosteric inhibitors
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Shideman,C.R., Reinardy,J.L. and Thayer,S.A.
gamma-Secretase activity modulates store-operated Ca2+ entry into rat sensory neurons
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Singh,R., Barman,A. and Prabhakar,R.
Computational insights into aspartyl protease activity of presenilin 1 (PS1) generating Alzheimer amyloid beta-peptides (Abeta40 and Abeta42)
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Takami,M., Nagashima,Y., Sano,Y., Ishihara,S., Morishima-Kawashima,M., Funamoto,S. and Ihara,Y.
gamma-Secretase: successive tripeptide and tetrapeptide release from the transmembrane domain of beta-carboxyl terminal fragment
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Tolia,A. and De Strooper,B.
Structure and function of gamma-secretase
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Secretase inhibitors and modulators for Alzheimer's disease treatment
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Truong,A.P., Aubele,D.L., Probst,G.D., Neitzel,M.L., Semko,C.M., Bowers,S., Dressen,D., Hom,R.K., Konradi,A.W., Sham,H.L., Garofalo,A.W., Keim,P.S., Wu,J., Dappen,M.S., Wong,K., Goldbach,E., Quinn,K.P., Sauer,J.M., Brigham,E.F., Wallace,W., Nguyen,L., Hemphill,S.S., Bova,M.P., Bard,F., Yednock,T.A. and Basi,G.
Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors
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Uemura,K., Lill,C.M., Li,X., Peters,J.A., Ivanov,A., Fan,Z., DeStrooper,B., Bacskai,B.J., Hyman,B.T. and Berezovska,O.
Allosteric modulation of PS1/gamma-secretase conformation correlates with amyloid beta(42/40) ratio
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Wakabayashi,T., Craessaerts,K., Bammens,L., Bentahir,M., Borgions,F., Herdewijn,P., Staes,A., Timmerman,E., Vandekerckhove,J., Rubinstein,E., Boucheix,C., Gevaert,K. and De Strooper,B.
Analysis of the gamma-secretase interactome and validation of its association with tetraspanin-enriched microdomains
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Wang,L.F., Zhang,R. and Xie,X.
Development of a high-throughput assay for screening of gamma-secretase inhibitor with endogenous human, mouse or drosophila gamma-secretase
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Winkler,E., Hobson,S., Fukumori,A., Dumpelfeld,B., Luebbers,T., Baumann,K., Haass,C., Hopf,C. and Steiner,H.
Purification, pharmacological modulation, and biochemical characterization of interactors of endogenous human gamma-secretase
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Wolfe,M.S.
gamma-Secretase in biology and medicine
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Wolfe,M.S.
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Yang,G., Yin,Y.I., Chun,J., Shelton,C.C., Ouerfelli,O. and Li,Y.M.
Stereo-controlled synthesis of novel photoreactive gamma-secretase inhibitors
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Yokoshima,S., Abe,Y., Watanabe,N., Kita,Y., Kan,T., Iwatsubo,T., Tomita,T. and Fukuyama,T.
Development of photoaffinity probes for gamma-secretase equipped with a nitrobenzenesulfonamide-type cleavable linker
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Zhang,C., Wu,B., Beglopoulos,V., Wines-Samuelson,M., Zhang,D., Dragatsis,I., Sudhof,T.C. and Shen,J.
Presenilins are essential for regulating neurotransmitter release
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2008

Abramowski,D., Wiederhold,K.H., Furrer,U., Jaton,A.L., Neuenschwander,A., Runser,M.J., Danner,S., Reichwald,J., Ammaturo,D., Staab,D., Stoeckli,M., Rueeger,H., Neumann,U. and Staufenbiel,M.
Dynamics of Abeta turnover and deposition in different beta-amyloid precursor protein transgenic mouse models following gamma-secretase inhibition
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Batelli,S., Albani,D., Prato,F., Polito,L., Franceschi,M., Gavazzi,A. and Forloni,G.
Early-onset Alzheimer disease in an Italian family with presenilin-1 double mutation E318G and G394V
Alzheimer Dis Assoc Disord (2008) 22, 184-187. PubMed Europe PubMed DOI M
Beel,A.J. and Sanders,C.R.
Substrate specificity of gamma-secretase and other intramembrane proteases
Cell Mol Life Sci (2008) 65, 1311-1334. PubMed Europe PubMed DOI PMC EPMC V P
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Gamma-secretase modulation and its promise for Alzheimer's disease: a rationale for drug discovery
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Bergstrom,C.P., Sloan,C.P., Lau,W.Y., Smith,D.W., Zheng,M., Hansel,S.B., Polson,C.T., Corsa,J.A., Barten,D.M., Felsenstein,K.M. and Roberts,S.B.
Carbamate-appended N-alkylsulfonamides as inhibitors of gamma-secretase
Bioorg Med Chem Lett (2008) 18, 464-468. PubMed Europe PubMed DOI I
Bergstrom,C.P., Sloan,C.P., Wang,H.H., Parker,M.F., Smith,D.W., Zheng,M., Hansel,S.B., Polson,C.T., Barber,L.E., Bursuker,I., Guss,V.L., Corsa,J.A., Barten,D.M., Felsenstein,K.M. and Roberts,S.B.
Nitrogen-appended N-alkylsulfonamides as inhibitors of gamma-secretase
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Boeras,D.I., Granic,A., Padmanabhan,J., Crespo,N.C., Rojiani,A.M. and Potter,H.
Alzheimer's presenilin 1 causes chromosome missegregation and aneuploidy
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Boo,J.H., Sohn,J.H., Kim,J.E., Song,H. and Mook-Jung,I.
Rac1 changes the substrate specificity of gamma-secretase between amyloid precursor protein and Notch1
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Boulton,M.E., Cai,J. and Grant,M.B.
gamma-Secretase: a multifaceted regulator of angiogenesis
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Boulton,M.E., Cai,J., Grant,M.B. and Zhang,Y.
Gamma-secretase regulates VEGFR-1 signalling in vascular endothelium and RPE
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The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression
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Cacquevel,M., Aeschbach,L., Osenkowski,P., Li,D., Ye,W., Wolfe,M.S., Li,H., Selkoe,D.J. and Fraering,P.C.
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Kogoshi,H., Sato,T., Koyama,T., Nara,N. and Tohda,S.
gamma-Secretase inhibitors suppress the growth of leukemia and lymphoma cells
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Konishi,J., Kawaguchi,K.S., Vo,H., Haruki,N., Gonzalez,A., Carbone,D.P. and Dang,T.P.
gamma-Secretase inhibitor prevents Notch3 activation and reduces proliferation in human lung cancers
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Kuzuya,A., Uemura,K., Kitagawa,N., Aoyagi,N., Kihara,T., Ninomiya,H., Ishiura,S., Takahashi,R. and Shimohama,S.
Presenilin 1 is involved in the maturation of beta-site amyloid precursor protein-cleaving enzyme 1 (BACE1)
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Laras,Y., Sheha,M., Pietrancosta,N. and Kraus,J.L.
Thiazolamide-ascorbic acid conjugate: a gamma-secretase inhibitor with enhanced blood-brain barrier permeation
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The Alzheimer's disease-associated gamma-secretase complex: functional domains in the presenilin 1 protein
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Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors
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Li,T., Wen,H., Brayton,C., Laird,F.M., Ma,G., Peng,S., Placanica,L., Wu,T.C., Crain,B.J., Price,D.L., Eberhart,C.G. and Wong,P.C.
Moderate reduction of gamma-secretase attenuates amyloid burden and limits mechanism-based liabilities
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Li,T., Wen,H., Brayton,C., Das,P., Smithson,L.A., Fauq,A., Fan,X., Crain,B.J., Price,D.L., Golde,T.E., Eberhart,C.G. and Wong,P.C.
Epidermal growth factor receptor and notch pathways participate in the tumor suppressor function of gamma-secretase
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Liao,Y.F., Wang,B.J., Hsu,W.M., Lee,H., Liao,C.Y., Wu,S.Y., Cheng,H.T. and Hu,M.K.
Unnatural amino acid-substituted (hydroxyethyl)urea peptidomimetics inhibit gamma-secretase and promote the neuronal differentiation of neuroblastoma cells
Mol Pharmacol (2007) 71, 588-601. PubMed Europe PubMed DOI I
Lundkvist,J. and Naslund,J.
gamma-Secretase: a complex target for Alzheimer's disease
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Madsen,L.B., Thomsen,B., Larsen,K., Bendixen,C., Holm,I.E., Fredholm,M., Jorgensen,A.L. and Nielsen,A.L.
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Narlawar,R., Perez Revuelta,B.I., Baumann,K., Schubenel,R., Haass,C., Steiner,H. and Schmidt,B.
N-Substituted carbazolyloxyacetic acids modulate Alzheimer associated gamma-secretase
Bioorg Med Chem Lett (2007) 17, 176-182. PubMed Europe PubMed DOI I
Narlawar,R., Baumann,K., Czech,C. and Schmidt,B.
Conversion of the LXR-agonist TO-901317 - from inverse to normal modulation of gamma-secretase by addition of a carboxylic acid and a lipophilic anchor
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Olson,R.E. and Marcin,L.R.
Chapter 3 Secretase Inhibitors and Modulators for the Treatment of Alzheimer's Disease
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N-(5-Chloro-2-(hydroxymethyl)-N-alkyl-arylsulfonamides as gamma-secretase inhibitors
Bioorg Med Chem Lett (2007) 17, 4432-4436. PubMed Europe PubMed DOI I
Parker,M.F., Bronson,J.J., Barten,D.M., Corsa,J.A., Du,W., Felsenstein,K.M., Guss,V.L., Izzarelli,D., Loo,A., McElhone,K.E., Marcin,L.R., Padmanabha,R., Pak,R., Polson,C.T., Toyn,J.H., Varma,S., Wang,J., Wong,V., Zheng,M. and Roberts,S.B.
Amino-caprolactam derivatives as gamma-secretase inhibitors
Bioorg Med Chem Lett (2007) 17, 5790-5795. PubMed Europe PubMed DOI I
Parks,A.L. and Curtis,D.
Presenilin diversifies its portfolio
Trends Genet (2007) 23, 140-150. PubMed Europe PubMed DOI V
Peters,J.U., Galley,G., Jacobsen,H., Czech,C., David-Pierson,P., Kitas,E.A. and Ozmen,L.
Novel orally active, dibenzazepinone-based gamma-secretase inhibitors
Bioorg Med Chem Lett (2007) 17, 5918-5923. PubMed Europe PubMed DOI I
Pissarnitski,D.A., Asberom,T., Bara,T.A., Buevich,A.V., Clader,J.W., Greenlee,W.J., Guzik,H.S., Josien,H.B., Li,W., McEwan,M., McKittrick,B.A., Nechuta,T.L., Parker,E.M., Sinning,L., Smith,E.M., Song,L., Vaccaro,H.A., Voigt,J.H., Zhang,L., Zhang,Q. and Zhao,Z.
2,6-Disubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors
Bioorg Med Chem Lett (2007) 17, 57-62. PubMed Europe PubMed DOI I
Prager,K., Wang-Eckhardt,L., Fluhrer,R., Killick,R., Barth,E., Hampel,H., Haass,C. and Walter,J.
A structural switch of presenilin 1 by glycogen synthase kinase 3beta-mediated phosphorylation regulates the interaction with beta-catenin and its nuclear signaling
J Biol Chem (2007) 282, 14083-14093. PubMed Europe PubMed DOI
Prasad,C.V., Zheng,M., Vig,S., Bergstrom,C., Smith,D.W., Gao,Q., Yeola,S., Polson,C.T., Corsa,J.A., Guss,V.L., Loo,A., Wang,J., Sleczka,B.G., Dangler,C., Robertson,B.J., Hendrick,J.P., Roberts,S.B. and Barten,D.M.
Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4- oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheimer's disease
Bioorg Med Chem Lett (2007) 17, 4006-4011. PubMed Europe PubMed DOI I
Raman,A., Lin,X., Suri,M., Hewitt,M., Constantinescu,C.S. and Phillips,M.F.
A presenilin 1 mutation (Arg278Ser) associated with early onset Alzheimer's disease and spastic paraparesis
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Ren,Z., Schenk,D., Basi,G.S. and Shapiro,I.P.
Amyloid beta-protein precursor juxtamembrane domain regulates specificity of gamma-secretase-dependent cleavages
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Repetto,E., Yoon,I.S., Zheng,H. and Kang,D.E.
Presenilin 1 regulates epidermal growth factor receptor turnover and signaling in the endosomal-lysosomal pathway
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Sato,T., Diehl,T.S., Narayanan,S., Funamoto,S., Ihara,Y., De Strooper,B., Steiner,H., Haass,C. and Wolfe,M.S.
Active gamma-secretase complexes contain only one of each component
J Biol Chem (2007) 282, 33985-33993. PubMed Europe PubMed DOI
Selkoe,D.J. and Wolfe,M.S.
Presenilin: running with scissors in the membrane
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[YEAR:9-1-2007]Shen,J. and Kelleher,R.J., III
The presenilin hypothesis of Alzheimer's disease: evidence for a loss-of-function pathogenic mechanism
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Shih,I. and Wang,T.L.
Notch signaling, gamma-secretase inhibitors, and cancer therapy
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Shimojo,M., Sahara,N., Murayama,M., Ichinose,H. and Takashima,A.
Decreased Abeta secretion by cells expressing familial Alzheimer's disease-linked mutant presenilin 1
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Shirotani,K., Tomioka,M., Kremmer,E., Haass,C. and Steiner,H.
Pathological activity of familial Alzheimer's disease-associated mutant presenilin can be executed by six different gamma-secretase complexes
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Shrimpton,A.E., Schelper,R.L., Linke,R.P., Hardy,J., Crook,R., Dickson,D.W., Ishizawa,T. and Davis,R.L.
A presenilin 1 mutation (L420R) in a family with early onset Alzheimer disease, seizures and cotton wool plaques, but not spastic paraparesis
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Spasic,D., Raemaekers,T., Dillen,K., Declerck,I., Baert,V., Serneels,L., Fullekrug,J. and Annaert,W.
Rer1p competes with APH-1 for binding to nicastrin and regulates gamma-secretase complex assembly in the early secretory pathway
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Villegas,A., Castaneda,M.M., Arias,L.F., Vieco,B., Lopera,F. and Bedoya,G.
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gamma-Secretase modulators
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When loss is gain: reduced presenilin proteolytic function leads to increased Abeta42/Abeta40. Talking Point on the role of presenilin mutations in Alzheimer disease
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Xiong,K., Clough,R.W., Luo,X.G., Struble,R.G., Li,Y.M. and Yan,X.X.
[3H]-L-685,458 as a radiotracer that maps gamma-secretase complex in the rat brain: relevance to Abeta genesis and presence of active presenilin-1 components
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Yang,M.G., Shi,J.L., Modi,D.P., Wells,J., Cochran,B.M., Wolf,M.A., Thompson,L.A., Ramanjulu,M.M., Roach,A.H., Zaczek,R., Robertson,D.W., Wexler,R.R. and Olson,R.E.
Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent gamma-secretase inhibitors
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Yin,Y.I., Bassit,B., Zhu,L., Yang,X., Wang,C. and Li,Y.M.
gamma-Secretase substrate concentration modulates the Abeta42/Abeta40 ratio: implications for Alzheimer disease
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Zhang,Y.W., Wang,R., Liu,Q., Zhang,H., Liao,F.F. and Xu,H.
Presenilin/gamma-secretase-dependent processing of beta-amyloid precursor protein regulates EGF receptor expression
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Zhao,G., Tan,J., Mao,G., Cui,M.Z. and Xu,X.
The same gamma-secretase accounts for the multiple intramembrane cleavages of APP
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Zhou,S., Zhou,H., Walian,P.J. and Jap,B.K.
Regulation of gamma-secretase activity in Alzheimer's disease
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2006

[YEAR:7-5-2006]Arumugam,T.V., Chan,S.L., Jo,D.G., Yilmaz,G., Tang,S.C., Cheng,A., Gleichmann,M., Okun,E., Dixit,V.D., Chigurupati,S., Mughal,M.R., Ouyang,X., Miele,L., Magnus,T., Poosala,S., Granger,D.N. and Mattson,M.P.
Gamma secretase-mediated Notch signaling worsens brain damage and functional outcome in ischemic stroke
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Avram,S., Milac,A.L., Mihailescu,D.F., Dabu,A. and Flonta,M.L.
Computer-aided drug design applied to beta and gamma secretase inhibitors - perspectives for new Alzheimer disease therapy
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[YEAR:9-1-2006]Bentahir,M., Nyabi,O., Verhamme,J., Tolia,A., Horre,K., Wiltfang,J., Esselmann,H. and De Strooper,B.
Presenilin clinical mutations can affect gamma-secretase activity by different mechanisms
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[YEAR:27-1-2006]Best,J.D., Jay,M.T., Otu,F., Churcher,I., Reilly,M., Morentin-Gutierrez,P., Pattison,C., Harrison,T., Shearman,M.S. and Atack,J.R.
In vivo characterization of Abeta(40) changes in brain and cerebrospinal fluid using the novel gamma-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1, 1-trifluoromethanesulfonamide (MRK-560) in the rat
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[YEAR:21-11-2006]Chandu,D., Huppert,S.S. and Kopan,R.
Analysis of transmembrane domain mutants is consistent with sequential cleavage of Notch by gamma-secretase
J Neurochem (21-11-2006) 96, 228-235. PubMed Europe PubMed DOI
[YEAR:27-4-2006]Chen,F., Hasegawa,H., Schmitt-Ulms,G., Kawarai,T., Bohm,C., Katayama,T., Gu,Y., Sanjo,N., Glista,M., Rogaeva,E., Wakutani,Y., Pardossi-Piquard,R., Ruan,X., Tandon,A., Checler,F., Marambaud,P., Hansen,K., Westaway,D., St George-Hyslop,P. and Fraser,P.
TMP21 is a presenilin complex component that modulates gamma-secretase but not epsilon-secretase activity
Nature (27-4-2006) 440, 1208-1212. PubMed Europe PubMed DOI
[YEAR:2-11-2006]Churcher,I., Beher,D., Best,J.D., Castro,J.L., Clarke,E.E., Gentry,A., Harrison,T., Hitzel,L., Kay,E., Kerrad,S., Lewis,H.D., Morentin-Gutierrez,P., Mortishire-Smith,R., Oakley,P.J., Reilly,M., Shaw,D.E., Shearman,M.S., Teall,M.R., Williams,S. and Wrigley,J.D.
4-Substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors
Bioorg Med Chem Lett (2-11-2006) 16, 280-284. PubMed Europe PubMed DOI I
[YEAR:11-8-2006]Clarke,E.E., Churcher,I., Ellis,S., Wrigley,J.D., Lewis,H.D., Harrison,T., Shearman,M.S. and Beher,D.
Intra- or intercomplex binding to the gamma-secretase enzyme. A model to differentiate inhibitor classes
J Biol Chem (11-8-2006) 281, 31279-31289. PubMed Europe PubMed DOI I
[YEAR:25-10-2006]Coolen,M.W., van Loo,K.M., van Bakel,N.N., Ellenbroek,B.A., Cools,A.R. and Martens,G.J.
Reduced Aph-1b expression causes tissue- and substrate-specific changes in gamma-secretase activity in rats with a complex phenotype
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[YEAR:5-4-2006]Deng,Y., Tarassishin,L., Kallhoff,V., Peethumnongsin,E., Wu,L., Li,Y.M. and Zheng,H.
Deletion of presenilin 1 hydrophilic loop sequence leads to impaired gamma-secretase activity and exacerbated amyloid pathology
J Neurosci (5-4-2006) 26, 3845-3854. PubMed Europe PubMed DOI
Dewji,N.N.
Presenilin structure in mechanisms leading to Alzheimer's disease
J Alzheimers Dis (2006) 10, 277-290. PubMed Europe PubMed
El Mouedden,M., Vandermeeren,M., Meert,T. and Mercken,M.
Reduction of Abeta levels in the Sprague Dawley rat after oral administration of the functional gamma-secretase inhibitor, DAPT: a novel non-transgenic model for Abeta production inhibitors
Curr Pharm Des (2006) 12, 671-676. PubMed Europe PubMed DOI I
Evin,G., Sernee,M.F. and Masters,C.L.
Inhibition of gamma-secretase as a therapeutic intervention for Alzheimer's disease: prospects, limitations and strategies
CNS Drugs (2006) 20, 351-372. PubMed Europe PubMed DOI I
[YEAR:18-4-2006]Fukumori,A., Okochi,M., Tagami,S., Jiang,J., Itoh,N., Nakayama,T., Yanagida,K., Ishizuka-Katsura,Y., Morihara,T., Kamino,K., Tanaka,T., Kudo,T., Tanii,H., Ikuta,A., Haass,C. and Takeda,M.
Presenilin-dependent gamma-secretase on plasma membrane and endosomes is functionally distinct
Biochemistry (18-4-2006) 45, 4907-4914. PubMed Europe PubMed DOI
[YEAR:9-6-2006]Fuwa,H., Hiromoto,K., Takahashi,Y., Yokoshima,S., Kan,T., Fukuyama,T., Iwatsubo,T., Tomita,T. and Natsugari,H.
Synthesis of biotinylated photoaffinity probes based on arylsulfonamide gamma-secretase inhibitors
Bioorg Med Chem Lett (9-6-2006) 16, 4184-4189. PubMed Europe PubMed DOI I
[YEAR:10-2-2006]Herl,L., Lleo,A., Thomas,A.V., Nyborg,A.C., Jansen,K., Golde,T.E., Hyman,B.T. and Berezovska,O.
Detection of presenilin-1 homodimer formation in intact cells using fluorescent lifetime imaging microscopy
Biochem Biophys Res Commun (10-2-2006) 340, 668-674. PubMed Europe PubMed DOI
Herranz,H., Stamataki,E., Feiguin,F. and Milan,M.
Self-refinement of Notch activity through the transmembrane protein Crumbs: modulation of gamma-secretase activity
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3-Substituted gem-cyclohexane sulfone based gamma-secretase inhibitors for Alzheimer's disease: conformational analysis and biological activity
Bioorg Med Chem Lett (5-5-2006) 16, 3839-3842. PubMed Europe PubMed DOI I
Kaether,C., Haass,C. and Steiner,H.
Assembly, trafficking and function of gamma-secretase
Neurodegener Dis (2006) 3, 275-283. PubMed Europe PubMed DOI
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Equimolar production of amyloid beta-protein and amyloid precursor protein intracellular domain from beta-carboxyl-terminal fragment by gamma-secretase
J Biol Chem (4-4-2006) 281, 14776-14786. PubMed Europe PubMed DOI
[YEAR:25-4-2006]Keller,P.C., Tomita,T., Hayashi,I., Chandu,D., Weber,J.D., Cistola,D.P. and Kopan,R.
A faster migrating variant masquerades as NICD when performing in vitro gamma-secretase assays with bacterially expressed notch substrates
Biochemistry (25-4-2006) 45, 5351-5358. PubMed Europe PubMed DOI PMC EPMC A
[YEAR:20-6-2006]Kornilova,A.Y., Kim,J., Laudon,H. and Wolfe,M.S.
Deducing the transmembrane domain organization of presenilin-1 in gamma-secretase by cysteine disulfide cross-linking
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[YEAR:4-11-2006]Larner,A.J. and Doran,M.
Clinical phenotypic heterogeneity of Alzheimer's disease associated with mutations of the presenilin-1 gene
J Neurol (4-11-2006) 253, 139-158. PubMed Europe PubMed DOI M
[YEAR:2-5-2006]Lazarov,V.K., Fraering,P.C., Ye,W., Wolfe,M.S., Selkoe,D.J. and Li,H.
Electron microscopic structure of purified, active gamma-secretase reveals an aqueous intramembrane chamber and two pores
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[YEAR:28-3-2006]Morohashi,Y., Kan,T., Tominari,Y., Fuwa,H., Okamura,Y., Watanabe,N., Sato,C., Natsugari,H., Fukuyama,T., Iwatsubo,T. and Tomita,T.
C-terminal fragment of presenilin is the molecular target of a dipeptidic gamma-secretase-specific inhibitor DAPT (N-[N-(3,5-difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester)
J Biol Chem (28-3-2006) 281, 14670-14676. PubMed Europe PubMed DOI I
[YEAR:28-12-2006]Narlawar,R., Perez Revuelta,B.I., Haass,C., Steiner,H., Schmidt,B. and Baumann,K.
Scaffold of the cyclooxygenase-2 (COX-2) inhibitor carprofen provides Alzheimer gamma-secretase modulators
J Med Chem (28-12-2006) 49, 7588-7591. PubMed Europe PubMed DOI
Ni,Y., Zhao,X., Bao,G., Zou,L., Teng,L., Wang,Z., Song,M., Xiong,J., Bai,Y. and Pei,G.
Activation of beta2-adrenergic receptor stimulates gamma-secretase activity and accelerates amyloid plaque formation
Nat Med (2006) 12, 1390-1396. PubMed Europe PubMed DOI
Nyborg,A.C., Ladd,T.B., Zwizinski,C.W., Lah,J.J. and Golde,T.E.
Sortilin, SorCS1b, and SorLA Vps10p sorting receptors, are novel gamma-secretase substrates
Mol Neurodegener (2006) 1, 3-3. PubMed Europe PubMed DOI PMC EPMC
[YEAR:5-5-2006]Ogura,T., Mio,K., Hayashi,I., Miyashita,H., Fukuda,R., Kopan,R., Kodama,T., Hamakubo,T., Iwastubo,T., Tomita,T. and Sato,C.
Three-dimensional structure of the gamma-secretase complex
Biochem Biophys Res Commun (5-5-2006) 343, 525-534. PubMed Europe PubMed DOI
[YEAR:30-5-2006]Oh,Y.S. and Turner,R.J.
Protease digestion indicates that endogenous presenilin 1 is present in at least two physical forms
Biochem Biophys Res Commun (30-5-2006) 346, 330-334. PubMed Europe PubMed DOI
[YEAR:15-11-2006]Sato,C., Morohashi,Y., Tomita,T. and Iwatsubo,T.
Structure of the catalytic pore of gamma-secretase probed by the accessibility of substituted cysteines
J Neurosci (15-11-2006) 26, 12081-12088. PubMed Europe PubMed DOI
Schmidt,B., Baumann,S., Braun,H.A. and Larbig,G.
Inhibitors and modulators of beta- and gamma-secretase
Curr Top Med Chem (2006) 6, 377-392. PubMed Europe PubMed DOI I
[YEAR:1-6-2006]Shaw,D., Best,J., Dinnell,K., Nadin,A., Shearman,M., Pattison,C., Peachey,J., Reilly,M., Williams,B., Wrigley,J. and Harrison,T.
3,4-Fused cyclohexyl sulfones as gamma-secretase inhibitors
Bioorg Med Chem Lett (1-6-2006) 16, 3073-3077. PubMed Europe PubMed DOI I
Shiraishi,H., Marutani,T., Wang,H.Q., Maeda,Y., Kurono,Y., Takashima,A., Araki,W., Nishimura,M., Yanagisawa,K. and Komano,H.
Reconstitution of gamma-secretase by truncated presenilin (PS) fragments revealed that PS C-terminal transmembrane domain is critical for formation of gamma-secretase complex
Genes Cells (2006) 11, 83-93. PubMed Europe PubMed DOI
[YEAR:28-2-2006]Siemers,E.R., Quinn,J.F., Kaye,J., Farlow,M.R., Porsteinsson,A., Tariot,P., Zoulnouni,P., Galvin,J.E., Holtzman,D.M., Knopman,D.S., Satterwhite,J., Gonzales,C., Dean,R.A. and May,P.C.
Effects of a gamma-secretase inhibitor in a randomized study of patients with Alzheimer disease
Neurology (28-2-2006) 66, 602-604. PubMed Europe PubMed DOI I
[YEAR:14-7-2006]Spasic,D., Tolia,A., Dillen,K., Baert,V., De Strooper,B., Vrijens,S. and Annaert,W.
Presenilin-1 maintains a nine-transmembrane topology throughout the secretory pathway
J Biol Chem (14-7-2006) 281, 26569-26577. PubMed Europe PubMed DOI
[YEAR:29-10-2006]Stachel,S.J., Coburn,C.A., Steele,T.G., Crouthamel,M.C., Pietrak,B.L., Lai,M.T., Holloway,M.K., Munshi,S.K., Graham,S.L. and Vacca,J.P.
Conformationally biased P3 amide replacements of beta-secretase inhibitors
Bioorg Med Chem Lett (29-10-2006) 16, 641-644. PubMed Europe PubMed DOI I
[YEAR:3-8-2006]Steiner,H., Than,M., Bode,W. and Haass,C.
Pore-forming scissors? A first structural glimpse of gamma-secretase
Trends Biochem Sci (3-8-2006) 31, 491-493. PubMed Europe PubMed DOI S
[YEAR:6-5-2006]Takahashi,Y., Fuwa,H., Kaneko,A., Sasaki,M., Yokoshima,S., Koizumi,H., Takebe,T., Kan,T., Iwatsubo,T., Tomita,T., Natsugari,H. and Fukuyama,T.
Novel gamma-secretase inhibitors discovered by library screening of in-house synthetic natural product intermediates
Bioorg Med Chem Lett (6-5-2006) 16, 3813-3816. PubMed Europe PubMed DOI I
[YEAR:9-2-2006]Thompson,L.A., Liauw,A.Y., Ramanjulu,M.M., Kasireddy-Polam,P., Mercer,S.E., Maduskuie,T.P., Glicksman,M., Roach,A.H., Meredith,J.E., Liu,R.Q., Combs,A.P., Higaki,J.N., Cordell,B., Seiffert,D., Zaczek,R.C., Robertson,D.W. and Olson,R.E.
Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors
Bioorg Med Chem Lett (9-2-2006) 16, 2357-2363. PubMed Europe PubMed DOI I
Tolia,A., Chavez-Gutierrez,L. and De Strooper,B.
Contribution of presenilin transmembrane domains 6 and 7 to a water-containing cavity in the gamma-secretase complex
J Biol Chem (2006) 281, 27633-27642. PubMed Europe PubMed DOI
Tomita,T. and Iwatsubo,T.
gamma-Secretase as a therapeutic target for treatment of Alzheimer's disease
Curr Pharm Des (2006) 12, 661-670. PubMed Europe PubMed DOI
Tomita,T., Tanaka,S., Morohashi,Y. and Iwatsubo,T.
Presenilin-dependent intramembrane cleavage of ephrin-B1
Mol Neurodegener (2006) 1, 2-2. PubMed Europe PubMed DOI PMC EPMC
[YEAR:23-11-2006]Wang,J., Beher,D., Nyborg,A.C., Shearman,M.S., Golde,T.E. and Goate,A.
C-terminal PAL motif of presenilin and presenilin homologues required for normal active site conformation
J Neurochem (23-11-2006) 96, 218-227. PubMed Europe PubMed DOI I
[YEAR:4-7-2006]Wolfe,M.S.
The gamma-secretase complex: membrane-embedded proteolytic ensemble
Biochemistry (4-7-2006) 45, 7931-7939. PubMed Europe PubMed DOI V
Wolfe,M.S.
Alzheimer protease hitches a ride
Nat Med (2006) 12, 1352-1354. PubMed Europe PubMed DOI
Wolfe,M.S.
Presenilin/gamma-secretase as a therapeutic target
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[YEAR:28-3-2006]Yagishita,S., Morishima-Kawashima,M., Tanimura,Y., Ishiura,S. and Ihara,Y.
DAPT-Induced intracellular accumulations of longer amyloid beta-proteins: further implications for the mechanism of intramembrane cleavage by gamma-secretase
Biochemistry (28-3-2006) 45, 3952-3960. PubMed Europe PubMed DOI I
[YEAR:5-4-2006]Yamasaki,A., Eimer,S., Okochi,M., Smialowska,A., Kaether,C., Baumeister,R., Haass,C. and Steiner,H.
The GxGD motif of presenilin contributes to catalytic function and substrate identification of gamma-secretase
J Neurosci (5-4-2006) 26, 3821-3828. PubMed Europe PubMed DOI
[YEAR:27-4-2006]Zhang,M., Haapasalo,A., Kim,D.Y., Ingano,L.A., Pettingell,W.H. and Kovacs,D.M.
Presenilin/gamma-secretase activity regulates protein clearance from the endocytic recycling compartment
FASEB J (27-4-2006) 20, 1176-1178. PubMed Europe PubMed DOI

2005

[YEAR:15-2-2005]Anderson,J.J., Holtz,G., Baskin,P.P., Turner,M., Rowe,B., Wang,B., Kounnas,M.Z., Lamb,B.T., Barten,D., Felsenstein,K., McDonald,I., Srinivasan,K., Munoz,B. and Wagner,S.L.
Reductions in beta-amyloid concentrations in vivo by the gamma-secretase inhibitors BMS-289948 and BMS-299897
Biochem Pharmacol (15-2-2005) 69, 689-698. PubMed Europe PubMed DOI I
[YEAR:27-9-2005]Barten,D.M., Guss,V.L., Corsa,J.A., Loo,A., Hansel,S.B., Zheng,M., Munoz,B., Srinivasan,K., Wang,B., Robertson,B.J., Polson,C.T., Wang,J., Roberts,S.B., Hendrick,J.P., Anderson,J.J., Loy,J.K., Denton,R., Verdoorn,T.A., Smith,D.W. and Felsenstein,K.M.
Dynamics of {beta}-amyloid reductions in brain, cerebrospinal fluid, and plasma of {beta}-amyloid precursor protein transgenic mice treated with a {gamma}-secretase inhibitor
J Pharmacol Exp Ther (27-9-2005) 312, 635-643. PubMed Europe PubMed DOI I
[YEAR:2-3-2005]Best,J.D., Jay,M.T., Otu,F., Ma,J., Nadin,A., Ellis,S., Lewis,H.D., Pattison,C., Reilly,M., Harrison,T., Shearman,M.S., Williamson,T.L. and Atack,J.R.
Quantitative measurement of changes in amyloid-beta(40) in the rat brain and cerebrospinal fluid following treatment with the gamma-secretase inhibitor LY-411575 [N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-ox o-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide]
J Pharmacol Exp Ther (2-3-2005) 313, 902-908. PubMed Europe PubMed DOI I
Brunkan,A.L. and Goate,A.M.
Presenilin function and gamma-secretase activity
J Neurochem (2005) 93, 769-792. PubMed Europe PubMed DOI V
Brunkan,A.L., Martinez,M., Walker,E.S. and Goate,A.M.
Presenilin endoproteolysis is an intramolecular cleavage
Mol Cell Neurosci (2005) 29, 65-73. PubMed Europe PubMed DOI
Brunkan,A.L., Martinez,M., Wang,J., Walker,E.S. and Goate,A.M.
A domain at the C-terminus of PS1 is required for presenilinase and gamma-secretase activities
J Neurochem (2005) 92, 1158-1169. PubMed Europe PubMed DOI
[YEAR:10-12-2005]Capell,A., Beher,D., Prokop,S., Steiner,H., Kaether,C., Shearman,M.S. and Haass,C.
Gamma-secretase complex assembly within the early secretory pathway
J Biol Chem (10-12-2005) 280, 6471-6478. PubMed Europe PubMed DOI
Churcher,I. and Beher,D.
Gamma-secretase as a therapeutic target for the treatment of Alzheimer's disease
Curr Pharm Des (2005) 11, 3363-3382. PubMed Europe PubMed DOI V
[YEAR:29-11-2005]Chyung,J.H., Raper,D.M. and Selkoe,D.J.
gamma-Secretase exists on the plasma membrane as an intact complex that accepts substrates and effects intramembrane cleavage
J Biol Chem (29-11-2005) 280, 4383-4392. PubMed Europe PubMed DOI
[YEAR:2-3-2005]Cowan,J.W., Wang,X., Guan,R., He,K., Jiang,J., Baumann,G., Black,R.A., Wolfe,M.S. and Frank,S.J.
Growth hormone receptor is a target for presenilin-dependent gamma-secretase cleavage
J Biol Chem (2-3-2005) 280, 19331-19342. PubMed Europe PubMed DOI I
[YEAR:12-8-2005]De Strooper,B.
Nicastrin: gatekeeper of the gamma-secretase complex
Cell (12-8-2005) 122, 318-320. PubMed Europe PubMed DOI
[YEAR:19-10-2005]Fraering,P.C., Ye,W., LaVoie,M.J., Ostaszewski,B.L., Selkoe,D.J. and Wolfe,M.S.
gamma-Secretase substrate selectivity can be modulated directly via interaction with a nucleotide-binding site
J Biol Chem (19-10-2005) 280, 41987-41996. PubMed Europe PubMed DOI PMC EPMC
Grimwood,S., Hogg,J., Jay,M.T., Lad,A.M., Lee,V., Murray,F., Peachey,J., Townend,T., Vithlani,M., Beher,D., Shearman,M.S. and Hutson,P.H.
Determination of guinea-pig cortical gamma-secretase activity ex vivo following the systemic administration of a gamma-secretase inhibitor
Neuropharmacology (2005) 48, 1002-1011. PubMed Europe PubMed DOI I
[YEAR:1-4-2005]Gundersen,E., Fan,K., Haas,K., Huryn,D., Steven Jacobsen,J., Kreft,A., Martone,R., Mayer,S., Sonnenberg-Reines,J., Sun,S.C. and Zhou,H.
Molecular-modeling based design, synthesis, and activity of substituted piperidines as gamma-secretase inhibitors
Bioorg Med Chem Lett (1-4-2005) 15, 1891-1894. PubMed Europe PubMed DOI I
Hansson,E.M., Stromberg,K., Bergstedt,S., Yu,G., Naslund,J., Lundkvist,J. and Lendahl,U.
Aph-1 interacts at the cell surface with proteins in the active gamma-secretase complex and membrane-tethered Notch
J Neurochem (2005) 92, 1010-1020. PubMed Europe PubMed DOI
Henricson,A., Kall,L. and Sonnhammer,E.L.
A novel transmembrane topology of presenilin based on reconciling experimental and computational evidence
FEBS J (2005) 272, 2727-2733. PubMed Europe PubMed DOI
Hoke,D.E., Tan,J.L., Ilaya,N.T., Culvenor,J.G., Smith,S.J., White,A.R., Masters,C.L. and Evin,G.M.
In vitro gamma-secretase cleavage of the Alzheimer's amyloid precursor protein correlates to a subset of presenilin complexes and is inhibited by zinc
FEBS J (2005) 272, 5544-5557. PubMed Europe PubMed DOI
Hu,M.K., Liao,Y.F., Wang,B.J., Huang,S.Y. and Liao,C.Y.
gamma-Secretase inhibition of dipeptide-based aldehydes with optimized N-terminal building blocks
Chin Pharm J (2005) 57, 89-98. I
Huppert,S.S., Ilagan,M.X., De Strooper,B. and Kopan,R.
Analysis of Notch function in presomitic mesoderm suggests a gamma-secretase-independent role for presenilins in somite differentiation
Dev Cell (2005) 8, 677-688. PubMed Europe PubMed DOI
[YEAR:29-3-2005]Kim,H., Ki,H., Park,H.S. and Kim,K.
Presenilin-1 D257A and D385A mutants fail to cleave Notch in their endoproteolyzed forms, but only presenilin-1 D385A mutant can restore its gamma-secretase activity with the compensatory overexpression of normal C-terminal fragment
J Biol Chem (29-3-2005) 280, 22462-22472. PubMed Europe PubMed DOI
[YEAR:10-11-2005]Kim,S.H. and Sisodia,S.S.
A sequence within the first transmembrane domain of PEN-2 is critical for PEN-2-mediated endoproteolysis of presenilin 1
J Biol Chem (10-11-2005) 280, 1992-2001. PubMed Europe PubMed DOI
[YEAR:1-3-2005]Kornilova,A.Y., Bihel,F., Das,C. and Wolfe,M.S.
The initial substrate-binding site of gamma-secretase is located on presenilin near the active site
Proc Natl Acad Sci U S A (1-3-2005) 102, 3230-3235. PubMed Europe PubMed DOI PMC EPMC
[YEAR:21-2-2005]Laras,Y., Quelever,G., Garino,C., Pietrancosta,N., Sheha,M., Bihel,F., Wolfe,M.S. and Kraus,J.L.
Substituted thiazolamide coupled to a redox delivery system: a new gamma-secretase inhibitor with enhanced pharmacokinetic profile
Org Biomol Chem (21-2-2005) 3, 612-618. PubMed Europe PubMed DOI I
[YEAR:25-7-2005]Laudon,H., Hansson,E.M., Melen,K., Bergman,A., Farmery,M.R., Winblad,B., Lendahl,U., von Heijne,G. and Naslund,J.
A nine-transmembrane domain topology for presenilin 1
J Biol Chem (25-7-2005) 280, 35352-35360. PubMed Europe PubMed DOI
[YEAR:17-1-2005]Lewis,S.J., Smith,A.L., Neduvelil,J.G., Stevenson,G.I., Lindon,M.J., Jones,A.B., Shearman,M.S., Beher,D., Clarke,E., Best,J.D., Peachey,J.E., Harrison,T. and Castro,J.L.
A novel series of potent gamma-secretase inhibitors based on a benzobicyclo[4.2.1]nonane core
Bioorg Med Chem Lett (17-1-2005) 15, 373-378. PubMed Europe PubMed DOI I
[YEAR:21-6-2005]Mastrangelo,P., Mathews,P.M., Chishti,M.A., Schmidt,S.D., Gu,Y., Yang,J., Mazzella,M.J., Coomaraswamy,J., Horne,P., Strome,B., Pelly,H., Levesque,G., Ebeling,C., Jiang,Y., Nixon,R.A., Rozmahel,R., Fraser,P.E., St George-Hyslop,P., Carlson,G.A. and Westaway,D.
Dissociated phenotypes in presenilin transgenic mice define functionally distinct gamma-secretases
Proc Natl Acad Sci U S A (21-6-2005) 102, 8972-8977. PubMed Europe PubMed DOI PMC EPMC
Nakaya,Y., Yamane,T., Shiraishi,H., Wang,H.Q., Matsubara,E., Sato,T., Dolios,G., Wang,R., De Strooper,B., Shoji,M., Komano,H., Yanagisawa,K., Ihara,Y., Fraser,P., St George-Hyslop,P. and Nishimura,M.
Random mutagenesis of presenilin-1 identifies novel mutants exclusively generating long amyloid beta-peptides
J Biol Chem (2005) 280, 19070-19077. PubMed Europe PubMed DOI I
[YEAR:6-9-2005]Oh,Y.S. and Turner,R.J.
Topology of the C-terminal fragment of human presenilin 1
Biochemistry (6-9-2005) 44, 11821-11828. PubMed Europe PubMed DOI
[YEAR:20-4-2005]Oh,Y.S. and Turner,R.J.
Evidence that the COOH terminus of human presenilin 1 is located in extracytoplasmic space
Am J Physiol Cell Physiol (20-4-2005) 289, C576-C581. PubMed Europe PubMed DOI PMC EPMC
[YEAR:19-5-2005]Pardossi-Piquard,R., Petit,A., Kawarai,T., Sunyach,C., Alves da Costa,C., Vincent,B., Ring,S., D'Adamio,L., Shen,J., Muller,U., St George Hyslop,P. and Checler,F.
Presenilin-dependent transcriptional control of the Abeta-degrading enzyme neprilysin by intracellular domains of betaAPP and APLP
Neuron (19-5-2005) 46, 541-554. PubMed Europe PubMed DOI
Pollack,S.J. and Lewis,H.
Secretase inhibitors for Alzheimer's disease: challenges of a promiscuous protease
Curr Opin Investig Drugs (2005) 6, 35-47. PubMed Europe PubMed V
Prokop,S., Haass,C. and Steiner,H.
Length and overall sequence of the PEN-2 C-terminal domain determines its function in the stabilization of presenilin fragments
J Neurochem (2005) 94, 57-62. PubMed Europe PubMed DOI
Qi-Takahara,Y., Morishima-Kawashima,M., Tanimura,Y., Dolios,G., Hirotani,N., Horikoshi,Y., Kametani,F., Maeda,M., Saido,T.C., Wang,R. and Ihara,Y.
Longer forms of amyloid beta protein: implications for the mechanism of intramembrane cleavage by gamma-secretase
J Neurosci (2005) 25, 436-445. PubMed Europe PubMed DOI I
[YEAR:7-7-2005]Quelever,G., Kachidian,P., Melon,C., Garino,C., Laras,Y., Pietrancosta,N., Sheha,M. and Louis Kraus,J.
Enhanced delivery of gamma-secretase inhibitor DAPT into the brain via an ascorbic acid mediated strategy
Org Biomol Chem (7-7-2005) 3, 2450-2457. PubMed Europe PubMed DOI I
Raemaekers,T., Esselens,C. and Annaert,W.
Presenilin 1: more than just gamma-secretase
Biochem Soc Trans (2005) 33, 559-562. PubMed Europe PubMed DOI
[YEAR:1-3-2005]Ravi Keerti,A., Ashok Kumar,B., Parthasarathy,T. and Uma,V.
QSAR studies - potent benzodiazepine gamma-secretase inhibitors
Bioorg Med Chem (1-3-2005) 13, 1873-1878. PubMed Europe PubMed DOI I
[YEAR:4-2-2005]Saito,S. and Araki,W.
Expression profiles of two human APH-1 genes and their roles in formation of presenilin complexes
Biochem Biophys Res Commun (4-2-2005) 327, 18-22. PubMed Europe PubMed DOI
[YEAR:1-2-2005]Serneels,L., Dejaegere,T., Craessaerts,K., Horre,K., Jorissen,E., Tousseyn,T., Hebert,S., Coolen,M., Martens,G., Zwijsen,A., Annaert,W., Hartmann,D. and De Strooper,B.
Differential contribution of the three Aph1 genes to gamma-secretase activity in vivo
Proc Natl Acad Sci U S A (1-2-2005) 102, 1719-1724. PubMed Europe PubMed DOI PMC EPMC
[YEAR:12-8-2005]Shah,S., Lee,S.F., Tabuchi,K., Hao,Y.H., Yu,C., LaPlant,Q., Ball,H., Dann,C.E., III, Sudhof,T. and Yu,G.
Nicastrin functions as a gamma-secretase-substrate receptor
Cell (12-8-2005) 122, 435-447. PubMed Europe PubMed DOI
[YEAR:26-7-2005]Sparey,T., Beher,D., Best,J., Biba,M., Castro,J.L., Clarke,E., Hannam,J., Harrison,T., Lewis,H., Madin,A., Shearman,M., Sohal,B., Tsou,N., Welch,C. and Wrigley,J.
Cyclic sulfamide gamma-secretase inhibitors
Bioorg Med Chem Lett (26-7-2005) 15, 4212-4216. PubMed Europe PubMed DOI I
[YEAR:31-8-2005]Stromberg,K., Hansson,E.M., Laudon,H., Bergstedt,S., Naslund,J., Lundkvist,J. and Lendahl,U.
gamma-Secretase complexes containing N- and C-terminal fragments of different presenilin origin retain normal gamma-secretase activity
J Neurochem (31-8-2005) 95, 880-890. PubMed Europe PubMed DOI
[YEAR:16-5-2005]Teall,M., Oakley,P., Harrison,T., Shaw,D., Kay,E., Elliott,J., Gerhard,U., Castro,J.L., Shearman,M., Ball,R.G. and Tsou,N.N.
Aryl sulfones: a new class of gamma-secretase inhibitors
Bioorg Med Chem Lett (16-5-2005) 15, 2685-2688. PubMed Europe PubMed DOI I
[YEAR:16-2-2005]Urano,Y., Hayashi,I., Isoo,N., Reid,P.C., Shibasaki,Y., Noguchi,N., Tomita,T., Iwatsubo,T., Hamakubo,T. and Kodama,T.
Association of active gamma-secretase complex with lipid rafts
J Lipid Res (16-2-2005) 46, 904-912. PubMed Europe PubMed DOI
[YEAR:16-6-2005]van Es,J.H., van Gijn,M.E., Riccio,O., van den Born,M., Vooijs,M., Begthel,H., Cozijnsen,M., Robine,S., Winton,D.J., Radtke,F. and Clevers,H.
Notch/gamma-secretase inhibition turns proliferative cells in intestinal crypts and adenomas into goblet cells
Nature (16-6-2005) 435, 959-963. PubMed Europe PubMed DOI
[YEAR:3-3-2005]Vidal,G.A., Naresh,A., Marrero,L. and Jones,F.E.
Presenilin-dependent gamma-secretase processing regulates multiple ERBB4/HER4 activities
J Biol Chem (3-3-2005) 280, 19777-19783. PubMed Europe PubMed DOI
[YEAR:18-10-2005]Watanabe,N., Tomita,T., Sato,C., Kitamura,T., Morohashi,Y. and Iwatsubo,T.
Pen-2 is incorporated into the gamma-secretase complex through binding to transmembrane domain 4 of presenilin 1
J Biol Chem (18-10-2005) 280, 41967-41975. PubMed Europe PubMed DOI
[YEAR:3-8-2005]Wen,P.H., De Gasperi,R., Sosa,M.A., Rocher,A.B., Friedrich,V.L., Jr., Hof,P.R. and Elder,G.A.
Selective expression of presenilin 1 in neural progenitor cells rescues the cerebral hemorrhages and cortical lamination defects in presenilin 1-null mutant mice
Development (3-8-2005) 132, 3873-3883. PubMed Europe PubMed DOI PMC EPMC K
[YEAR:1-6-2005]Wiley,J.C., Hudson,M., Kanning,K.C., Schecterson,L.C. and Bothwell,M.
Familial Alzheimer's disease mutations inhibit gamma-secretase-mediated liberation of beta-amyloid precursor protein carboxy-terminal fragment
J Neurochem (1-6-2005) 94, 1189-1201. PubMed Europe PubMed DOI
Wong,H.K., Sakurai,T., Oyama,F., Kaneko,K., Wada,K., Miyazaki,H., Kurosawa,M., De Strooper,B., Saftig,P. and Nukina,N.
beta Subunits of voltage-gated sodium channels are novel substrates of beta-site amyloid precursor protein-cleaving enzyme (BACE1) and gamma-secretase
J Biol Chem (2005) 280, 23009-23017. PubMed Europe PubMed DOI
[YEAR:21-12-2005]Wrigley,J.D., Schurov,I., Nunn,E.J., Martin,A.C., Clarke,E.E., Ellis,S., Bonnert,T.P., Shearman,M.S. and Beher,D.
Functional overexpression of gamma-secretase reveals protease-independent trafficking functions and a critical role of lipids for protease activity
J Biol Chem (21-12-2005) 280, 12523-12535. PubMed Europe PubMed DOI
[YEAR:22-3-2005]Zhang,L., Lee,J., Song,L., Sun,X., Shen,J., Terracina,G. and Parker,E.M.
Characterization of the reconstituted gamma-secretase complex from Sf9 cells co-expressing presenilin 1, nicastrin, aph-1a, and pen-2
Biochemistry (22-3-2005) 44, 4450-4457. PubMed Europe PubMed DOI
[YEAR:11-2-2005]Zhang,Y.W., Luo,W.J., Wang,H., Lin,P., Vetrivel,K.S., Liao,F., Li,F., Wong,P.C., Farquhar,M.G., Thinakaran,G. and Xu,H.
Nicastrin is critical for stability and trafficking but not association of other presenilin/gamma-secretase components
J Biol Chem (11-2-2005) 280, 17020-17026. PubMed Europe PubMed DOI PMC EPMC
[YEAR:24-5-2005]Zhou,S., Zhou,H., Walian,P.J. and Jap,B.K.
CD147 is a regulatory subunit of the gamma-secretase complex in Alzheimer's disease amyloid beta-peptide production
Proc Natl Acad Sci U S A (24-5-2005) 102, 7499-7504. PubMed Europe PubMed DOI PMC EPMC

2004

[YEAR:16-12-2004]Bakshi,P. and Wolfe,M.S.
Stereochemical analysis of (hydroxyethyl)urea peptidomimetic inhibitors of gamma-secretase
J Med Chem (16-12-2004) 47, 6485-6489. PubMed Europe PubMed DOI I
[YEAR:1-9-2004]Beglopoulos,V., Sun,X., Saura,C.A., Lemere,C.A., Kim,R.D. and Shen,J.
Reduced beta-amyloid production and increased inflammatory responses in presenilin conditional knock-out mice
J Biol Chem (1-9-2004) 279, 46907-46914. PubMed Europe PubMed DOI K
[YEAR:10-8-2004]Beher,D., Clarke,E.E., Wrigley,J.D., Martin,A.C., Nadin,A., Churcher,I. and Shearman,M.S.
Selected non-steroidal anti-inflammatory drugs and their derivatives target gamma-secretase at a novel site. Evidence for an allosteric mechanism
J Biol Chem (10-8-2004) 279, 43419-43426. PubMed Europe PubMed DOI
[YEAR:20-8-2004]Bergman,A., Laudon,H., Winblad,B., Lundkvist,J. and Naslund,J.
The extreme C terminus of presenilin 1 is essential for gamma-secretase complex assembly and activity
J Biol Chem (20-8-2004) 279, 45564-45572. PubMed Europe PubMed DOI
[YEAR:29-7-2004]Bihel,F., Das,C., Bowman,M.J. and Wolfe,M.S.
Discovery of a subnanomolar helical D-tridecapeptide inhibitor of gamma-secretase
J Med Chem (29-7-2004) 47, 3931-3933. PubMed Europe PubMed DOI I
Carter,T.L., Verdile,G., Groth,D., Bogush,A., Thomas,S., Shen,P., Fraser,P.E., Mathews,P., Nixon,R.A., Ehrlich,M.E., Kwok,J.B., St George-Hyslop,P., Schofield,P., Li,Y., Yang,A., Martins,R.N. and Gandy,S.
Alzheimer amyloid precursor aspartyl proteinase activity in CHAPSO homogenates of Spodoptera frugiperda cells
Alzheimer Dis Assoc Disord (2004) 18, 261-263. PubMed Europe PubMed E
[YEAR:25-6-2004]Cervantes,S., Saura,C.A., Pomares,E., Gonzalez-Duarte,R. and Marfany,G.
Functional implications of the presenilin dimerization: reconstitution of gamma-secretase activity by assembly of a catalytic site at the dimer interface of two catalytically inactive presenilins
J Biol Chem (25-6-2004) 279, 36519-36529. PubMed Europe PubMed DOI
Dominguez,D.I., Hartmann,D. and De Strooper,B.
BACE1 and presenilin: two unusual aspartyl proteases involved in Alzheimer's disease
Neurodegener Dis (2004) 1, 168-174. PubMed Europe PubMed DOI
[YEAR:21-6-2004]Edbauer,D., Kaether,C., Steiner,H. and Haass,C.
Co-expression of nicastrin and presenilin rescues a loss of function mutant of APH-1
J Biol Chem (21-6-2004) 279, 37311-37315. PubMed Europe PubMed DOI
[YEAR:19-4-2004]Esler,W.P., Das,C. and Wolfe,M.S.
Probing pockets S2-S4' of the gamma-secretase active site with (hydroxyethyl)urea peptidomimetics
Bioorg Med Chem Lett (19-4-2004) 14, 1935-1938. PubMed Europe PubMed DOI
[YEAR:25-5-2004]Feng,R., Wang,H., Wang,J., Shrom,D., Zeng,X. and Tsien,J.Z.
Forebrain degeneration and ventricle enlargement caused by double knockout of Alzheimer's presenilin-1 and presenilin-2
Proc Natl Acad Sci U S A (25-5-2004) 101, 8162-8167. PubMed Europe PubMed DOI PMC EPMC
[YEAR:20-1-2004]Fraering,P.C., LaVoie,M.J., Ye,W., Ostaszewski,B.L., Kimberly,W.T., Selkoe,D.J. and Wolfe,M.S.
Detergent-dependent dissociation of active gamma-secretase reveals an interaction between Pen-2 and PS1-NTF and offers a model for subunit organization within the complex
Biochemistry (20-1-2004) 43, 323-333. PubMed Europe PubMed DOI
[YEAR:3-8-2004]Fraering,P.C., Ye,W., Strub,J.M., Dolios,G., LaVoie,M.J., Ostaszewski,B.L., Van Dorsselaer,A., Wang,R., Selkoe,D.J. and Wolfe,M.S.
Purification and characterization of the human gamma-secretase complex
Biochemistry (3-8-2004) 43, 9774-9789. PubMed Europe PubMed DOI I
[YEAR:30-4-2004]Gu,Y., Sanjo,N., Chen,F., Hasegawa,H., Petit,A., Ruan,X., Li,W., Shier,C., Kawarai,T., Schmitt-Ulms,G., Westaway,D., St George-Hyslop,P. and Fraser,P.E.
The presenilin proteins are components of multiple membrane-bound complexes that have different biological activities
J Biol Chem (30-4-2004) 279, 31329-31336. PubMed Europe PubMed DOI
[YEAR:4-8-2004]Gupta,S., Singh,R., Datta,P., Zhang,Z., Orr,C., Lu,Z., Dubois,G., Zervos,A.S., Meisler,M.H., Srinivasula,S.M., Fernandes-Alnemri,T. and Alnemri,E.S.
The C-terminal tail of presenilin regulates Omi/HtrA2 protease activity
J Biol Chem (4-8-2004) 279, 45844-45854. PubMed Europe PubMed DOI
[YEAR:28-9-2004]Hansson,C.A., Frykman,S., Farmery,M.R., Tjernberg,L.O., Nilsberth,C., Pursglove,S.E., Ito,A., Winblad,B., Cowburn,R.F., Thyberg,J. and Ankarcrona,M.
Nicastrin, presenilin, APH-1, and PEN-2 form active gamma-secretase complexes in mitochondria
J Biol Chem (28-9-2004) 279, 51654-51660. PubMed Europe PubMed DOI I
Harrison,T., Churcher,I. and Beher,D.
gamma-Secretase as a target for drug intervention in Alzheimer's disease
Curr Opin Drug Discov Devel (2004) 7, 709-719. PubMed Europe PubMed V
[YEAR:23-6-2004]Hayashi,I., Urano,Y., Fukuda,R., Isoo,N., Kodama,T., Hamakubo,T., Tomita,T. and Iwatsubo,T.
Selective reconstitution and recovery of functional gamma-secretase complex on budded baculovirus particles
J Biol Chem (23-6-2004) 279, 38040-38046. PubMed Europe PubMed DOI
[YEAR:8-12-2004]Kaether,C., Capell,A., Edbauer,D., Winkler,E., Novak,B., Steiner,H. and Haass,C.
The presenilin C-terminus is required for ER-retention, nicastrin-binding and gamma-secretase activity
EMBO J (8-12-2004) 23, 4738-4748. PubMed Europe PubMed DOI PMC EPMC
Kilb,W., Hartmann,D., Saftig,P. and Luhmann,H.J.
Altered morphological and electrophysiological properties of Cajal-Retzius cells in cerebral cortex of embryonic presenilin-1 knockout mice
Eur J Neurosci (2004) 20, 2749-2756. PubMed Europe PubMed DOI K
[YEAR:29-9-2004]Kim,S.H., Yin,Y.I., Li,Y.M. and Sisodia,S.S.
Evidence that assembly of an active gamma-secretase complex occurs in the early compartments of the secretory pathway
J Biol Chem (29-9-2004) 279, 48615-48619. PubMed Europe PubMed DOI
[YEAR:25-5-2004]Knappenberger,K.S., Tian,G., Ye,X., Sobotka-Briner,C., Ghanekar,S.V., Greenberg,B.D. and Scott,C.W.
Mechanism of gamma-secretase cleavage activation: is gamma-secretase regulated through autoinhibition involving the presenilin-1 exon 9 loop?
Biochemistry (25-5-2004) 43, 6208-6218. PubMed Europe PubMed DOI I
Kopan,R. and Ilagan,M.X.
Gamma-secretase: proteasome of the membrane?
Nat Rev Mol Cell Biol (2004) 5, 499-504. PubMed Europe PubMed DOI
Landman,N. and Kim,T.W.
Got RIP? Presenilin-dependent intramembrane proteolysis in growth factor receptor signaling
Cytokine Growth Factor Rev (2004) 15, 337-351. PubMed Europe PubMed DOI
[YEAR:12-1-2004]Lanz,T.A., Hosley,J.D., Adams,W.J. and Merchant,K.M.
Studies of Abeta pharmacodynamics in the brain, cerebrospinal fluid, and plasma in young (plaque-free) Tg2576 mice using the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo -6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY-411575)
J Pharmacol Exp Ther (12-1-2004) 309, 49-55. PubMed Europe PubMed DOI I
Larbig,G., Zall,A. and Schmidt,B.
Inhibitors designed for presenilin 1 by means of aspartic acid activation
Helv Chim Acta (2004) 87, 2334-2340. I
[YEAR:29-3-2004]Laudon,H., Karlstrom,H., Mathews,P.M., Farmery,M.R., Gandy,S.E., Lundkvist,J., Lendahl,U. and Naslund,J.
Functional domains in presenilin 1: the Tyr-288 residue controls gamma-secretase activity and endoproteolysis
J Biol Chem (29-3-2004) 279, 23925-23932. PubMed Europe PubMed DOI
[YEAR:6-2-2004]Lee,S.F., Shah,S., Yu,C., Wigley,W.C., Li,H., Lim,M., Pedersen,K., Han,W., Thomas,P., Lundkvist,J., Hao,Y.H. and Yu,G.
A conserved GXXXG motif in APH-1 is critical for assembly and activity of the gamma-secretase complex
J Biol Chem (6-2-2004) 279, 4144-4152. PubMed Europe PubMed DOI
Lleo,A., Berezovska,O., Herl,L., Raju,S., Deng,A., Bacskai,B.J., Frosch,M.P., Irizarry,M. and Hyman,B.T.
Nonsteroidal anti-inflammatory drugs lower Abeta42 and change presenilin 1 conformation
Nat Med (2004) 10, 1065-1066. PubMed Europe PubMed DOI
Menendez,M.
Pathological and clinical heterogeneity of presenilin 1 gene mutations
J Alzheimers Dis (2004) 6, 475-482. PubMed Europe PubMed M V
Pan,Y., Lin,M.H., Tian,X., Cheng,H.T., Gridley,T., Shen,J. and Kopan,R.
gamma-Secretase functions through Notch signaling to maintain skin appendages but is not required for their patterning or initial morphogenesis
Dev Cell (2004) 7, 731-743. PubMed Europe PubMed DOI
[YEAR:18-11-2004]Popescu,B.O., Cedazo-Minguez,A., Benedikz,E., Nishimura,T., Winblad,B., Ankarcrona,M. and Cowburn,R.F.
gamma-Secretase activity of presenilin 1 regulates acetylcholine muscarinic receptor-mediated signal transduction
J Biol Chem (18-11-2004) 279, 6455-6464. PubMed Europe PubMed DOI I
[YEAR:19-4-2004]Prasad,C.V., Wallace,O.B., Noonan,J.W., Sloan,C.P., Lau,W., Vig,S., Parker,M.F., Smith,D.W., Hansel,S.B., Polson,C.T., Barten,D.M., Felsenstein,K.M. and Roberts,S.B.
Hydroxytriamides as potent gamma-secretase inhibitors
Bioorg Med Chem Lett (19-4-2004) 14, 1917-1921. PubMed Europe PubMed DOI I
[YEAR:5-7-2004]Prasad,C.V., Vig,S., Smith,D.W., Gao,Q., Polson,C.T., Corsa,J.A., Guss,V.L., Loo,A., Barten,D.M., Zheng,M., Felsenstein,K.M. and Roberts,S.B.
2,3-Benzodiazepin-1,4-diones as peptidomimetic inhibitors of gamma-secretase
Bioorg Med Chem Lett (5-7-2004) 14, 3535-3538. PubMed Europe PubMed DOI I
[YEAR:23-3-2004]Prokop,S., Shirotani,K., Edbauer,D., Haass,C. and Steiner,H.
Requirement of PEN-2 for stabilization of the presenilin N-/C-terminal fragment heterodimer within the gamma-secretase complex
J Biol Chem (23-3-2004) 279, 23255-23261. PubMed Europe PubMed DOI
[YEAR:8-4-2004]Saura,C.A., Choi,S.Y., Beglopoulos,V., Malkani,S., Zhang,D., Shankaranarayana Rao,B.S., Chattarji,S., Kelleher,R.J., III, Kandel,E.R., Duff,K., Kirkwood,A. and Shen,J.
Loss of presenilin function causes impairments of memory and synaptic plasticity followed by age-dependent neurodegeneration
Neuron (8-4-2004) 42, 23-36. PubMed Europe PubMed DOI K
[YEAR:5-10-2004]Scheper,W., Zwart,R. and Baas,F.
Alternative splicing in the N-terminus of Alzheimer's presenilin 1
Neurogenetics (5-10-2004) 5, 223-227. PubMed Europe PubMed DOI R
Shiraishi,H., Sai,X., Wang,H.Q., Maeda,Y., Kurono,Y., Nishimura,M., Yanagisawa,K. and Komano,H.
PEN-2 enhances gamma-cleavage after presenilin heterodimer formation
J Neurochem (2004) 90, 1402-1413. PubMed Europe PubMed DOI
Siman,R. and Salidas,S.
Gamma-secretase subunit composition and distribution in the presenilin wild-type and mutant mouse brain
Neuroscience (2004) 129, 615-628. PubMed Europe PubMed DOI
Steiner,H.
Uncovering gamma-secretase
Curr Alzheimer Res (2004) 1, 175-181. PubMed Europe PubMed V
Tomita,T. and Iwatsubo,T.
The inhibition of gamma-secretase as a therapeutic approach to Alzheimer's disease
Drug News Perspect (2004) 17, 321-325. PubMed Europe PubMed DOI I
[YEAR:2-3-2004]Verdile,G., Groth,D., Mathews,P.M., St George-Hyslop,P., Fraser,P.E., Ramabhadran,T.V., Kwok,J.B., Schofield,P.R., Carter,T., Gandy,S. and Martins,R.N.
Baculoviruses expressing the human familial Alzheimer's disease presenilin 1 mutation lacking exon 9 increase levels of an amyloid beta-like protein in Sf9 cells
Mol Psychiatry (2-3-2004) 9, 594-602. PubMed Europe PubMed DOI
[YEAR:22-10-2004]Vetrivel,K.S., Cheng,H., Lin,W., Sakurai,T., Li,T., Nukina,N., Wong,P.C., Xu,H. and Thinakaran,G.
Association of gamma-secretase with lipid rafts in post-Golgi and endosome membranes
J Biol Chem (22-10-2004) 279, 44945-44954. PubMed Europe PubMed DOI PMC EPMC
[YEAR:4-10-2004]Vooijs,M., Schroeter,E.H., Pan,Y., Blandford,M. and Kopan,R.
Ectodomain shedding and intramembrane cleavage of mammalian notch proteins is not regulated through oligomerization
J Biol Chem (4-10-2004) 279, 50864-50873. PubMed Europe PubMed DOI
Wang,J., Brunkan,A.L., Hecimovic,S., Walker,E. and Goate,A.
Conserved "PAL" sequence in presenilins is essential for gamma-secretase activity, but not required for formation or stabilization of gamma-secretase complexes
Neurobiol Dis (2004) 15, 654-666. PubMed Europe PubMed DOI
[YEAR:23-11-2004]Wen,P.H., De Gasperi,R., Gama Sosa,M.A. and Elder,G.A.
Neural progenitor cells do not differentiate prematurely in presenilin-1 null mutant mice
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Wolfe,M.S.
Presenilins
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[YEAR:6-1-2004]Wong,G.T., Manfra,D., Poulet,F.M., Zhang,Q., Josien,H., Bara,T., Engstrom,L., Pinzon-Ortiz,M., Fine,J.S., Lee,H.J., Zhang,L., Higgins,G.A. and Parker,E.M.
Chronic treatment with the gamma-secretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation
J Biol Chem (6-1-2004) 279, 12876-12882. PubMed Europe PubMed DOI I
Wrigley,J.D., Nunn,E.J., Nyabi,O., Clarke,E.E., Hunt,P., Nadin,A., De Strooper,B., Shearman,M.S. and Beher,D.
Conserved residues within the putative active site of gamma-secretase differentially influence enzyme activity and inhibitor binding
J Neurochem (2004) 90, 1312-1320. PubMed Europe PubMed DOI
[YEAR:13-10-2004]Zhao,G., Mao,G., Tan,J., Dong,Y., Cui,M.Z., Kim,S.H. and Xu,X.
Identification of a new presenilin-dependent zeta-cleavage site within the transmembrane domain of amyloid precursor protein
J Biol Chem (13-10-2004) 279, 50647-50650. PubMed Europe PubMed DOI

2003

Baulac,S., LaVoie,M.J., Kimberly,W.T., Strahle,J., Wolfe,M.S., Selkoe,D.J. and Xia,W.
Functional gamma-secretase complex assembly in Golgi/trans-Golgi network: interactions among presenilin, nicastrin, Aph1, Pen-2, and gamma-secretase substrates
Neurobiol Dis (2003) 14, 194-204. PubMed Europe PubMed DOI
[YEAR:15-7-2003]Beher,D., Fricker,M., Nadin,A., Clarke,E.E., Wrigley,J.D., Li,Y.M., Culvenor,J.G., Masters,C.L., Harrison,T. and Shearman,M.S.
In vitro characterization of the presenilin-dependent gamma-secretase complex using a novel affinity ligand
Biochemistry (15-7-2003) 42, 8133-8142. PubMed Europe PubMed DOI
[YEAR:26-12-2003]Capell,A., Kaether,C., Edbauer,D., Shirotani,K., Merkl,S., Steiner,H. and Haass,C.
Nicastrin interacts with gamma-secretase complex components via the N-terminal part of its transmembrane domain
J Biol Chem (26-12-2003) 278, 52519-52523. PubMed Europe PubMed DOI
[YEAR:10-4-2003]De Strooper,B.
Aph-1, Pen-2, and nicastrin with presenilin generate an active gamma-secretase complex
Neuron (10-4-2003) 38, 9-12. PubMed Europe PubMed DOI
Edbauer,D., Winkler,E., Regula,J.T., Pesold,B., Steiner,H. and Haass,C.
Reconstitution of gamma-secretase activity
Nat Cell Biol (2003) 5, 486-488. PubMed Europe PubMed DOI
[YEAR:11-4-2003]Grimm,H.S., Beher,D., Lichtenthaler,S.F., Shearman,M.S., Beyreuther,K. and Hartmann,T.
gamma-Secretase cleavage site specificity differs for intracellular and secretory amyloid beta
J Biol Chem (11-4-2003) 278, 13077-13085. PubMed Europe PubMed DOI
[YEAR:31-1-2003]Hebert,S.S., Godin,C., Tomiyama,T., Mori,H. and Levesque,G.
Dimerization of presenilin-1 in vivo: suggestion of novel regulatory mechanisms leading to higher order complexes
Biochem Biophys Res Commun (31-1-2003) 301, 119-126. PubMed Europe PubMed DOI M
[YEAR:28-2-2003]Ikeuchi,T., Dolios,G., Kim,S.H., Wang,R. and Sisodia,S.S.
Familial Alzheimer disease-linked presenilin 1 variants enhance production of both Abeta 1-40 and Abeta 1-42 peptides that are only partially sensitive to a potent aspartyl protease transition state inhibitor of "gamma-secretase"
J Biol Chem (28-2-2003) 278, 7010-7018. PubMed Europe PubMed DOI I
Ikeuchi,T. and Sisodia,S.S.
The Notch ligands, Delta1 and Jagged2, are substrates for presenilin-dependent "gamma-secretase" cleavage
J Biol Chem (2003) 278, 7751-7754. PubMed Europe PubMed DOI P
[YEAR:14-1-2003]Kimberly,W.T., Esler,W.P., Ye,W., Ostaszewski,B.L., Gao,J., Diehl,T., Selkoe,D.J. and Wolfe,M.S.
Notch and the amyloid precursor protein are cleaved by similar gamma-secretase(s)
Biochemistry (14-1-2003) 42, 137-144. PubMed Europe PubMed DOI
[YEAR:27-5-2003]Kimberly,W.T., LaVoie,M.J., Ostaszewski,B.L., Ye,W., Wolfe,M.S. and Selkoe,D.J.
Gamma-secretase is a membrane protein complex comprised of presenilin, nicastrin, Aph-1, and Pen-2
Proc Natl Acad Sci U S A (27-5-2003) 100, 6382-6387. PubMed Europe PubMed DOI PMC EPMC
[YEAR:9-5-2003]Kornilova,A.Y., Das,C. and Wolfe,M.S.
Differential effects of inhibitors on the gamma-secretase complex. Mechanistic implications
J Biol Chem (9-5-2003) 278, 16470-16473. PubMed Europe PubMed DOI I
[YEAR:20-6-2003]Lai,M.T., Chen,E., Crouthamel,M.C., DiMuzio-Mower,J., Xu,M., Huang,Q., Price,E., Register,R.B., Shi,X.P., Donoviel,D.B., Bernstein,A., Hazuda,D., Gardell,S.J. and Li,Y.M.
Presenilin-1 and presenilin-2 exhibit distinct yet overlapping gamma-secretase activities
J Biol Chem (20-6-2003) 278, 22475-22481. PubMed Europe PubMed DOI
Lanz,T.A., Himes,C.S., Pallante,G., Adams,L., Yamazaki,S., Amore,B. and Merchant,K.M.
The gamma-secretase inhibitor N-[N-(3,5-difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester reduces A beta levels in vivo in plasma and cerebrospinal fluid in young (plaque-free) and aged (plaque-bearing) Tg2576 mice
J Pharmacol Exp Ther (2003) 305, 864-871. PubMed Europe PubMed DOI I
[YEAR:26-9-2003]LaVoie,M.J., Fraering,P.C., Ostaszewski,B.L., Ye,W., Kimberly,W.T., Wolfe,M.S. and Selkoe,D.J.
Assembly of the gamma-secretase complex involves early formation of an intermediate subcomplex of Aph-1 and nicastrin
J Biol Chem (26-9-2003) 278, 37213-37222. PubMed Europe PubMed DOI
[YEAR:5-9-2003]LaVoie,M.J. and Selkoe,D.J.
The Notch ligands, Jagged and Delta, are sequentially processed by alpha-secretase and presenilin/gamma-secretase and release signaling fragments
J Biol Chem (5-9-2003) 278, 34427-34437. PubMed Europe PubMed DOI
[YEAR:24-6-2003]Lewis,H.D., Perez Revuelta,B.I., Nadin,A., Neduvelil,J.G., Harrison,T., Pollack,S.J. and Shearman,M.S.
Catalytic site-directed gamma-secretase complex inhibitors do not discriminate pharmacologically between Notch S3 and beta-APP cleavages
Biochemistry (24-6-2003) 42, 7580-7586. PubMed Europe PubMed DOI I
[YEAR:15-4-2003]Li,T., Ma,G., Cai,H., Price,D.L. and Wong,P.C.
Nicastrin is required for assembly of presenilin/gamma-secretase complexes to mediate Notch signaling and for processing and trafficking of beta-amyloid precursor protein in mammals
J Neurosci (15-4-2003) 23, 3272-3277. PubMed Europe PubMed
[YEAR:5-9-2003]Marambaud,P., Wen,P.H., Dutt,A., Shioi,J., Takashima,A., Siman,R. and Robakis,N.K.
A CBP binding transcriptional repressor produced by the PS1/epsilon-cleavage of N-cadherin is inhibited by PS1 FAD mutations
Cell (5-9-2003) 114, 635-645. PubMed Europe PubMed DOI
[YEAR:6-6-2003]Marlow,L., Canet,R.M., Haugabook,S.J., Hardy,J.A., Lahiri,D.K. and Sambamurti,K.
APH1, PEN2, and nicastrin increase Abeta levels and gamma-secretase activity
Biochem Biophys Res Commun (6-6-2003) 305, 502-509. PubMed Europe PubMed DOI
Medina,M. and Dotti,C.G.
RIPped out by presenilin-dependent gamma-secretase
Cell Signal (2003) 15, 829-841. PubMed Europe PubMed DOI
[YEAR:13-3-2003]Murakami,D., Okamoto,I., Nagano,O., Kawano,Y., Tomita,T., Iwatsubo,T., De Strooper,B., Yumoto,E. and Saya,H.
Presenilin-dependent gamma-secretase activity mediates the intramembranous cleavage of CD44
Oncogene (13-3-2003) 22, 1511-1516. PubMed Europe PubMed DOI
Nakajima,M., Yuasa,S., Ueno,M., Takakura,N., Koseki,H. and Shirasawa,T.
Abnormal blood vessel development in mice lacking presenilin-1
Mech Dev (2003) 120, 657-667. PubMed Europe PubMed DOI
[YEAR:10-9-2003]Nornes,S., Groth,C., Camp,E., Ey,P. and Lardelli,M.
Developmental control of presenilin1 expression, endoproteolysis, and interaction in zebrafish embryos
Exp Cell Res (10-9-2003) 289, 124-132. PubMed Europe PubMed DOI
[YEAR:31-10-2003]Nyabi,O., Bentahir,M., Horre,K., Herreman,A., Gottardi-Littell,N., Van Broeckhoven,C., Merchiers,P., Spittaels,K., Annaert,W. and De Strooper,B.
Presenilins mutated at Asp-257 or Asp-385 restore Pen-2 expression and Nicastrin glycosylation but remain catalytically inactive in the absence of wild type Presenilin
J Biol Chem (31-10-2003) 278, 43430-43436. PubMed Europe PubMed DOI
[YEAR:18-7-2003]Pasternak,S.H., Bagshaw,R.D., Guiral,M., Zhang,S., Ackerley,C.A., Pak,B.J., Callahan,J.W. and Mahuran,D.J.
Presenilin-1, nicastrin, amyloid precursor protein, and gamma-secretase activity are co-localized in the lysosomal membrane
J Biol Chem (18-7-2003) 278, 26687-26694. PubMed Europe PubMed DOI
[YEAR:1-11-2003]Petit,A., Pasini,A., Alves da Costa,C., Ayral,E., Hernandez,J.F., Dumanchin-Njock,C., Phiel,C.J., Marambaud,P., Wilk,S., Farzan,M., Fulcrand,P., Martinez,J., Andrau,D. and Checler,F.
JLK isocoumarin inhibitors: selective gamma-secretase inhibitors that do not interfere with notch pathway in vitro or in vivo
J Neurosci Res (1-11-2003) 74, 370-377. PubMed Europe PubMed DOI I
[YEAR:6-6-2003]Piper,S.C., Amtul,Z., Galinanes-Garcia,L., Howard,V.G., Ziani-Cherif,C., McLendon,C., Rochette,M.J., Fauq,A., Golde,T.E. and Murphy,M.P.
Peptide-based, irreversible inhibitors of gamma-secretase activity
Biochem Biophys Res Commun (6-6-2003) 305, 529-533. PubMed Europe PubMed DOI I
[YEAR:5-9-2003]Rao,V.R. and Finkbeiner,S.
Secrets of a secretase: N-cadherin proteolysis regulates CBP function
Cell (5-9-2003) 114, 533-535. PubMed Europe PubMed DOI
[YEAR:24-4-2003]Scarpa,S., Fuso,A., D'Anselmi,F. and Cavallaro,R.A.
Presenilin 1 gene silencing by S-adenosylmethionine: a treatment for Alzheimer disease?
FEBS Lett (24-4-2003) 541, 145-148. PubMed Europe PubMed DOI
[YEAR:17-10-2003]Schroeter,E.H., Ilagan,M.X., Brunkan,A.L., Hecimovic,S., Li,Y.M., Xu,M., Lewis,H.D., Saxena,M.T., De Strooper,B., Coonrod,A., Tomita,T., Iwatsubo,T., Moore,C.L., Goate,A., Wolfe,M.S., Shearman,M. and Kopan,R.
A presenilin dimer at the core of the gamma-secretase enzyme: insights from parallel analysis of Notch 1 and APP proteolysis
Proc Natl Acad Sci U S A (17-10-2003) 100, 13075-13080. PubMed Europe PubMed DOI PMC EPMC
Selkoe,D. and Kopan,R.
Notch and Presenilin: regulated intramembrane proteolysis links development and degeneration
Annu Rev Neurosci (2003) 26, 565-597. PubMed Europe PubMed DOI
Siman,R. and Velji,J.
Localization of presenilin-nicastrin complexes and gamma-secretase activity to the trans-Golgi network
J Neurochem (2003) 84, 1143-1153. PubMed Europe PubMed DOI
[YEAR:24-6-2003]Six,E., Ndiaye,D., Laabi,Y., Brou,C., Gupta-Rossi,N., Israel,A. and Logeat,F.
The Notch ligand Delta1 is sequentially cleaved by an ADAM protease and gamma-secretase
Proc Natl Acad Sci U S A (24-6-2003) 100, 7638-7643. PubMed Europe PubMed DOI PMC EPMC
[YEAR:15-8-2003]Taniguchi,Y., Kim,S.H. and Sisodia,S.S.
Presenilin-dependent "gamma-secretase" processing of deleted in colorectal cancer (DCC)
J Biol Chem (15-8-2003) 278, 30425-30428. PubMed Europe PubMed DOI
[YEAR:1-8-2003]Tian,G., Ghanekar,S.V., Aharony,D., Shenvi,A.B., Jacobs,R.T., Liu,X. and Greenberg,B.D.
The mechanism of gamma-secretase: multiple inhibitor binding sites for transition state analogs and small molecule inhibitors
J Biol Chem (1-8-2003) 278, 28968-28975. PubMed Europe PubMed DOI I
[YEAR:15-7-2003]Uemura,K., Kitagawa,N., Kohno,R., Kuzuya,A., Kageyama,T., Shibasaki,H. and Shimohama,S.
Presenilin 1 mediates retinoic acid-induced differentiation of SH-SY5Y cells through facilitation of Wnt signaling
J Neurosci Res (15-7-2003) 73, 166-175. PubMed Europe PubMed DOI
Weihofen,A. and Martoglio,B.
Intramembrane-cleaving proteases: controlled liberation of proteins and bioactive peptides
Trends Cell Biol (2003) 13, 71-78. PubMed Europe PubMed DOI
[YEAR:15-7-2003]Xia,W. and Wolfe,M.S.
Intramembrane proteolysis by presenilin and presenilin-like proteases
J Cell Sci (15-7-2003) 116, 2839-2844. PubMed Europe PubMed DOI

2002

Beher,D. and Shearman,M.S.
gamma-Secretase inhibition
Biochem Soc Trans (2002) 30, 534-537. PubMed Europe PubMed DOI I
[YEAR:5-3-2002]Esler,W.P., Kimberly,W.T., Ostaszewski,B.L., Ye,W., Diehl,T.S., Selkoe,D.J. and Wolfe,M.S.
Activity-dependent isolation of the presenilin-gamma-secretase complex reveals nicastrin and a gamma substrate
Proc Natl Acad Sci U S A (5-3-2002) 99, 2720-2725. PubMed Europe PubMed DOI PMC EPMC
Goutte,C., Tsunozaki,M., Hale,V.A. and Priess,J.R.
APH-1 is a multipass membrane protein essential for the Notch signaling pathway in Caenorhabditis elegans embryos
Proc Natl Acad Sci U S A (2002) 99, 775-779. PubMed Europe PubMed DOI PMC EPMC
[YEAR:1-12-2002]Haass,C. and Steiner,H.
Alzheimer disease gamma-secretase: a complex story of GxGD-type presenilin proteases
Trends Cell Biol (1-12-2002) 12, 556-562. PubMed Europe PubMed DOI
[YEAR:1-3-2002]Karlstrom,H., Bergman,A., Lendahl,U., Naslund,J. and Lundkvist,J.
A sensitive and quantitative assay for measuring cleavage of presenilin substrates
J Biol Chem (1-3-2002) 277, 6763-6766. PubMed Europe PubMed DOI A
[YEAR:20-9-2002]Kimberly,W.T., LaVoie,M.J., Ostaszewski,B.L., Ye,W., Wolfe,M.S. and Selkoe,D.J.
Complex N-linked glycosylated nicastrin associates with active gamma-secretase and undergoes tight cellular regulation
J Biol Chem (20-9-2002) 277, 35113-35117. PubMed Europe PubMed DOI
[YEAR:31-1-2002]Kopan,R. and Goate,A.
Aph-2/nicastrin: an essential component of gamma-secretase and regulator of notch signaling and presenilin localization
Neuron (31-1-2002) 33, 321-324. PubMed Europe PubMed DOI
[YEAR:22-11-2002]Lammich,S., Okochi,M., Takeda,M., Kaether,C., Capell,A., Zimmer,A.K., Edbauer,D., Walter,J., Steiner,H. and Haass,C.
Presenilin-dependent intramembrane proteolysis of CD44 leads to the liberation of its intracellular domain and the secretion of an Abeta-like peptide
J Biol Chem (22-11-2002) 277, 44754-44759. PubMed Europe PubMed DOI
[YEAR:22-2-2002]Lee,H.J., Jung,K.M., Huang,Y.Z., Bennett,L.B., Lee,J.S., Mei,L. and Kim,T.W.
Presenilin-dependent gamma-secretase-like intramembrane cleavage of ErbB4
J Biol Chem (22-2-2002) 277, 6318-6323. PubMed Europe PubMed DOI
[YEAR:22-11-2002]Lee,S.F., Shah,S., Li,H., Yu,C., Han,W. and Yu,G.
Mammalian APH-1 interacts with presenilin and nicastrin and is required for intramembrane proteolysis of amyloid-beta precursor protein and Notch
J Biol Chem (22-11-2002) 277, 45013-45019. PubMed Europe PubMed DOI
[YEAR:24-5-2002]Leem,J.Y., Vijayan,S., Han,P., Cai,D., Machura,M., Lopes,K.O., Veselits,M.L., Xu,H. and Thinakaran,G.
Presenilin 1 is required for maturation and cell surface accumulation of nicastrin
J Biol Chem (24-5-2002) 277, 19236-19240. PubMed Europe PubMed DOI
[YEAR:5-2-2002]Lichtenthaler,S.F., Beher,D., Grimm,H.S., Wang,R., Shearman,M.S., Masters,C.L. and Beyreuther,K.
The intramembrane cleavage site of the amyloid precursor protein depends on the length of its transmembrane domain
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Berezovska,O., Jack,C., McLean,P., Aster,J.C., Hicks,C., Xia,W., Wolfe,M.S., Kimberly,W.T., Weinmaster,G., Selkoe,D.J. and Hyman,B.T.
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Presenilin 1 is linked with gamma-secretase activity in the detergent solubilized state
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Presenilin complexes with the C-terminal fragments of amyloid precursor protein at the sites of amyloid beta-protein generation
Proc Natl Acad Sci U S A (1-8-2000) 97, 9299-9304. PubMed Europe PubMed DOI PMC EPMC
Yu,G., Chen,F., Nishimura,M., Steiner,H., Tandon,A., Kawarai,T., Arawaka,S., Supala,A., Song,Y.Q., Rogaeva,E., Holmes,E., Zhang,D.M., Milman,P., Fraser,P., Haass,C. and St George-Hyslop,P.
Mutation of conserved aspartates affect maturation of presenilin 1 and presenilin 2 complexes
Acta Neurol Scand Suppl (2000) 176, 6-11. PubMed Europe PubMed
Zhang,Z., Nadeau,P., Song,W., Donoviel,D., Yuan,M., Bernstein,A. and Yankner,B.A.
Presenilins are required for gamma-secretase cleavage of beta-APP and transmembrane cleavage of Notch-1
Nat Cell Biol (2000) 2, 463-465. PubMed Europe PubMed DOI

1999

Annaert,W. and De Strooper,B.
Presenilins: molecular switches between proteolysis and signal transduction
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Presenilins: structural aspects and posttranslational events
Mol Neurobiol (1999) 19, 255-265. PubMed Europe PubMed DOI
da Costa,C.A., Ancolio,K. and Checler,F.
C-Terminal maturation fragments of presenilin 1 and 2 control secretion of APP alpha and A beta by human cells and are degraded by proteasome
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De Jonghe,C., Cruts,M., Rogaeva,E.A., Tysoe,C., Singleton,A., Vanderstichele,H., Meschino,W., Dermaut,B., Vanderhoeven,I., Backhovens,H., Vanmechelen,E., Morris,C.M., Hardy,J., Rubinsztein,D.C., St George-Hyslop,P.H. and Van Broeckhoven,C.
Aberrant splicing in the presenilin-1 intron 4 mutation causes presenile Alzheimer's disease by increased Abeta42 secretion
Hum Mol Genet (1999) 8, 1529-1540. PubMed Europe PubMed DOI
[YEAR:8-4-1999]De Strooper,B., Annaert,W., Cupers,P., Saftig,P., Craessaerts,K., Mumm,J.S., Schroeter,E.H., Schrijvers,V., Wolfe,M.S., Ray,W.J., Goate,A. and Kopan,R.
A presenilin-1-dependent gamma-secretase-like protease mediates release of Notch intracellular domain
Nature (8-4-1999) 398, 518-522. PubMed Europe PubMed DOI
[YEAR:29-10-1999]Haass,C. and De Strooper,B.
The presenilins in Alzheimer's disease - proteolysis holds the key
Science (29-10-1999) 286, 916-919. PubMed Europe PubMed DOI
[YEAR:12-10-1999]Leimer,U., Lun,K., Romig,H., Walter,J., Grunberg,J., Brand,M. and Haass,C.
Zebrafish (Danio rerio) presenilin promotes aberrant amyloid beta-peptide production and requires a critical aspartate residue for its function in amyloidogenesis
Biochemistry (12-10-1999) 38, 13602-13609. PubMed Europe PubMed DOI
[YEAR:16-3-1999]Lichtenthaler,S.F., Wang,R., Grimm,H., Uljon,S.N., Masters,C.L. and Beyreuther,K.
Mechanism of the cleavage specificity of Alzheimer's disease gamma-secretase identified by phenylalanine-scanning mutagenesis of the transmembrane domain of the amyloid precursor protein
Proc Natl Acad Sci U S A (16-3-1999) 96, 3053-3058. PubMed Europe PubMed PMC EPMC
[YEAR:23-4-1999]Murphy,M.P., Hickman,L.J., Eckman,C.B., Uljon,S.N., Wang,R. and Golde,T.E.
gamma-Secretase, evidence for multiple proteolytic activities and influence of membrane positioning of substrate on generation of amyloid beta peptides of varying length
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Cell surface presenilin-1 participates in the gamma-secretase-like proteolysis of notch
J Biol Chem (17-12-1999) 274, 36801-36807. PubMed Europe PubMed DOI
[YEAR:14-5-1999]Saura,C.A., Tomita,T., Davenport,F., Harris,C.L., Iwatsubo,T. and Thinakaran,G.
Evidence that intramolecular associations between presenilin domains are obligatory for endoproteolytic processing
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[YEAR:8-6-1999]Song,W., Nadeau,P., Yuan,M., Yang,X., Shen,J. and Yankner,B.A.
Proteolytic release and nuclear translocation of Notch-1 are induced by presenilin-1 and impaired by pathogenic presenilin-1 mutations
Proc Natl Acad Sci U S A (8-6-1999) 96, 6959-6963. PubMed Europe PubMed DOI PMC EPMC
Steiner,H., Capell,A., Leimer,U. and Haass,C.
Genes and mechanisms involved in beta-amyloid generation and Alzheimer's disease
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Amyloidogenic function of the Alzheimer's disease-associated presenilin 1 in the absence of endoproteolysis
Biochemistry (2-11-1999) 38, 14600-14605. PubMed Europe PubMed DOI
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An in vivo assay for the identification of target proteases which cleave membrane-associated substrates
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[YEAR:8-4-1999]Wolfe,M.S., Xia,W., Ostaszewski,B.L., Diehl,T.S., Kimberly,W.T. and Selkoe,D.J.
Two transmembrane aspartates in presenilin-1 required for presenilin endoproteolysis and gamma-secretase activity
Nature (8-4-1999) 398, 513-517. PubMed Europe PubMed DOI I
[YEAR:31-8-1999]Wolfe,M.S., De Los Angeles,J., Miller,D.D., Xia,W. and Selkoe,D.J.
Are presenilins intramembrane-cleaving proteases? Implications for the molecular mechanism of Alzheimer's disease
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[YEAR:13-4-1999]Wolfe,M.S., Xia,W., Moore,C.L., Leatherwood,D.D., Ostaszewski,B., Rahmati,T., Donkor,I.O. and Selkoe,D.J.
Peptidomimetic probes and molecular modeling suggest that Alzheimer's gamma-secretase is an intramembrane-cleaving aspartyl protease
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1998

[YEAR:22-1-1998]De Strooper,B., Saftig,P., Craessaerts,K., Vanderstichele,H., Guhde,G., Annaert,W., von Figura,K. and Van Leuven,F.
Deficiency of presenilin-1 inhibits the normal cleavage of amyloid precursor protein
Nature (22-1-1998) 391, 387-390. PubMed Europe PubMed DOI
Selkoe,D.J.
The cell biology of beta-amyloid precursor protein and presenilin in Alzheimer's disease
Trends Cell Biol (1998) 8, 447-453. PubMed Europe PubMed DOI
Thinakaran,G., Regard,J.B., Bouton,C.M., Harris,C.L., Price,D.L., Borchelt,D.R. and Sisodia,S.S.
Stable association of presenilin derivatives and absence of presenilin interactions with APP
Neurobiol Dis (1998) 4, 438-453. PubMed Europe PubMed DOI
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BetaAPP gamma-secretase and SREBP site 2 protease are two different enzymes
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Proteolytic fragments of the Alzheimer's disease associated presenilins-1 and -2 are phosphorylated in vivo by distinct cellular mechanisms
Biochemistry (28-4-1998) 37, 5961-5967. PubMed Europe PubMed DOI
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A substrate-based difluoro ketone selectively inhibits Alzheimer's gamma-secretase activity
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Presenilin 1 regulates the processing of beta-amyloid precursor protein C-terminal fragments and the generation of amyloid beta-protein in endoplasmic reticulum and Golgi
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The presenilin 1 protein is a component of a high molecular weight intracellular complex that contains beta-catenin
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1997

Podlisny,M.B., Citron,M., Amarante,P., Sherrington,R., Xia,W., Zhang,J., Diehl,T., Levesque,G., Fraser,P., Haass,C., Koo,E.H., Seubert,P., St George-Hyslop,P., Teplow,D.B. and Selkoe,D.J.
Presenilin proteins undergo heterogeneous endoproteolysis between Thr291 and Ala299 and occur as stable N- and C-terminal fragments in normal and Alzheimer brain tissue
Neurobiol Dis (1997) 3, 325-337. PubMed Europe PubMed DOI
[YEAR:22-7-1997]Xia,W., Zhang,J., Perez,R., Koo,E.H. and Selkoe,D.J.
Interaction between amyloid precursor protein and presenilins in mammalian cells: implications for the pathogenesis of Alzheimer disease
Proc Natl Acad Sci U S A (22-7-1997) 94, 8208-8213. PubMed Europe PubMed DOI PMC EPMC

1996

Citron,M., Diehl,T.S., Gordon,G., Biere,A.L., Seubert,P. and Selkoe,D.J.
Evidence that the 42- and 40-amino acid forms of amyloid beta protein are generated from the beta-amyloid precursor protein by different protease activities
Proc Natl Acad Sci U S A (1996) 93, 13170-13175. PubMed Europe PubMed DOI PMC EPMC
Doan,A., Thinakaran,G., Borchelt,D.R., Slunt,H.H., Ratovitsky,T., Podlisny,M., Selkoe,D.J., Seeger,M., Gandy,S.E., Price,D.L. and Sisodia,S.S.
Protein topology of presenilin 1
Neuron (1996) 17, 1023-1030. PubMed Europe PubMed DOI
Scheuner,D., Eckman,C., Jensen,M., Song,X., Citron,M., Suzuki,N., Bird,T.D., Hardy,J., Hutton,M., Kukull,W., Larson,E., Levy-Lahad,E., Viitanen,M., Peskind,E., Poorkaj,P., Schellenberg,G., Tanzi,R., Wasco,W., Lannfelt,L., Selkoe,D. and Younkin,S.
Secreted amyloid beta-protein similar to that in the senile plaques of Alzheimer's disease is increased in vivo by the presenilin 1 and 2 and APP mutations linked to familial Alzheimer's disease
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Beta-amyloid precursor protein. Location of transmembrane domain and specificity of gamma-secretase cleavage
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1995

Campion,D., Flaman,J.M., Brice,A., Hannequin,D., Dubois,B., Martin,C., Moreau,V., Charbonnier,F., Didierjean,O. and Tardieu,S.
Mutations of the presenilin I gene in families with early-onset Alzheimer's disease
Hum Mol Genet (1995) 4, 2373-2377. PubMed Europe PubMed