Modulation of gamma-secretase specificity using small molecule allosteric inhibitors

scientific article

Modulation of gamma-secretase specificity using small molecule allosteric inhibitors is …
instance of (P31):
scholarly articleQ13442814

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P819ADS bibcode2009PNAS..10620228S
P356DOI10.1073/PNAS.0910757106
P8608Fatcat IDrelease_5pra5goixbc4ljh22la7jtd3oq
P932PMC publication ID2787169
P698PubMed publication ID19906985
P5875ResearchGate publication ID38083502

P2093author name stringLi Yang
Hui Zheng
Hakim Djaballah
Rong Wang
Lei Zhu
Yue-Ming Li
Christopher C Shelton
Deming Chau
P2860cites workPresenilin 1 is linked with gamma-secretase activity in the detergent solubilized stateQ22254058
Gleevec inhibits β-amyloid production but not Notch cleavageQ24683037
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Alzheimer's disease: genes, proteins, and therapyQ28131806
Photoactivated gamma-secretase inhibitors directed to the active site covalently label presenilin 1Q28139001
Regulated intramembrane proteolysis: a control mechanism conserved from bacteria to humansQ28145545
Presenilin-dependent intramembrane proteolysis of CD44 leads to the liberation of its intracellular domain and the secretion of an Abeta-like peptideQ28201180
Diverse compounds mimic Alzheimer disease-causing mutations by augmenting Abeta42 productionQ28245521
Notch-1 signalling requires ligand-induced proteolytic release of intracellular domainQ28273268
Presenilin clinical mutations can affect gamma-secretase activity by different mechanismsQ28290934
Spatial segregation of gamma-secretase and substrates in distinct membrane domainsQ28591973
Notch/gamma-secretase inhibition turns proliferative cells in intestinal crypts and adenomas into goblet cellsQ29614268
Two transmembrane aspartates in presenilin-1 required for presenilin endoproteolysis and gamma-secretase activityQ29616491
Mean age-of-onset of familial alzheimer disease caused by presenilin mutations correlates with both increased Abeta42 and decreased Abeta40.Q33245678
Cryoelectron microscopy structure of purified gamma-secretase at 12 A resolutionQ33694348
Familial Alzheimer's disease-linked presenilin 1 variants elevate Abeta1-42/1-40 ratio in vitro and in vivoQ34063772
A common enzyme connects notch signaling and Alzheimer's diseaseQ34088470
{gamma}-Secretase Substrate Concentration Modulates the Abeta42/Abeta40 Ratio: IMPLICATIONS FOR ALZHEIMER DISEASE.Q34635580
Aph-1, Pen-2, and Nicastrin with Presenilin generate an active gamma-Secretase complexQ35105866
gamma-Secretase as a target for drug intervention in Alzheimer's disease.Q35927325
The profile of soluble amyloid beta protein in cultured cell media. Detection and quantification of amyloid beta protein and variants by immunoprecipitation-mass spectrometryQ36835366
Pen2 and presenilin-1 modulate the dynamic equilibrium of presenilin-1 and presenilin-2 gamma-secretase complexesQ37075276
Substrate-targeting gamma-secretase modulatorsQ37182828
Processing of Notch and amyloid precursor protein by gamma-secretase is spatially distinctQ37705090
Coumarin-based inhibitors of human NAD(P)H:quinone oxidoreductase-1. Identification, structure-activity, off-target effects and in vitro human pancreatic cancer toxicity.Q40052618
Stereo-controlled synthesis of novel photoreactive gamma-secretase inhibitorsQ40278030
Mutations in APP have independent effects on Abeta and CTFgamma generationQ40506128
The C-terminus of the beta protein is critical in amyloidogenesisQ40779575
L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid beta-protein precursor gamma-secretase activityQ40865987
Coumarin-based inhibitors of HIV integraseQ42551512
A subset of NSAIDs lower amyloidogenic Abeta42 independently of cyclooxygenase activityQ43793656
Linear non-competitive inhibition of solubilized human gamma-secretase by pepstatin A methylester, L685458, sulfonamides, and benzodiazepinesQ44033487
Stereoselective synthesis of photoreactive peptidomimetic gamma-secretase inhibitorsQ45095870
A new dicoumarin and anticoagulant activity from Viola yedoensis MakinoQ46078450
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's diseaseQ46243973
Abeta40 inhibits amyloid deposition in vivo.Q48305645
Deletion of presenilin 1 hydrophilic loop sequence leads to impaired gamma-secretase activity and exacerbated amyloid pathology.Q48592298
Transition-state analogue inhibitors of gamma-secretase bind directly to presenilin-1.Q53341822
P433issue48
P407language of work or nameEnglishQ1860
P921main subjectallosteric inhibitorQ70361704
P304page(s)20228-20233
P577publication date2009-11-11
P1433published inProceedings of the National Academy of Sciences of the United States of AmericaQ1146531
P1476titleModulation of gamma-secretase specificity using small molecule allosteric inhibitors
P478volume106

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