Novel γ-secretase enzyme modulators directly target presenilin protein.
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Cellular mechanisms of γ-secretase substrate selection, processing and toxicityToward the structure of presenilin/γ-secretase and presenilin homologsAftins increase amyloid-β42, lower amyloid-β38, and do not alter amyloid-β40 extracellular production in vitro: toward a chemical model of Alzheimer's disease?Identification and Preclinical Pharmacology of the γ-Secretase Modulator BMS-869780.Allosteric regulation of γ-secretase activity by a phenylimidazole-type γ-secretase modulator.Presenilin is the molecular target of acidic γ-secretase modulators in living cells.Characterization of intermediate steps in amyloid beta (Aβ) production under near-native conditions.A peptide binding to the β-site of APP improves spatial memory and attenuates Aβ burden in Alzheimer's disease transgenic miceA subset of membrane-altering agents and γ-secretase modulators provoke nonsubstrate cleavage by rhomboid proteasesIndependent relationship between amyloid precursor protein (APP) dimerization and γ-secretase processivity.Increasing Membrane Cholesterol Level Increases the Amyloidogenic Peptide by Enhancing the Expression of Phospholipase C.Amyloid-PET predicts inhibition of de novo plaque formation upon chronic γ-secretase modulator treatmentCholestenoic acid, an endogenous cholesterol metabolite, is a potent γ-secretase modulator.γ-Secretase Modulators and APH1 Isoforms Modulate γ-Secretase Cleavage but Not Position of ε-Cleavage of the Amyloid Precursor Protein (APP).First and second generation γ-secretase modulators (GSMs) modulate amyloid-β (Aβ) peptide production through different mechanismsSecond generation γ-secretase modulators exhibit different modulation of Notch β and Aβ production.APLP1 as a cerebrospinal fluid biomarker for γ-secretase modulator treatmentγ-Secretase modulator (GSM) photoaffinity probes reveal distinct allosteric binding sites on presenilin.Efficacy of SPI-1865, a novel gamma-secretase modulator, in multiple rodent models.Robust Translation of γ-Secretase Modulator Pharmacology across Preclinical Species and Human Subjects.Steroids as γ-secretase modulators.Soluble γ-secretase modulators selectively inhibit the production of the 42-amino acid amyloid β peptide variant and augment the production of multiple carboxy-truncated amyloid β species.Development and mechanism of γ-secretase modulators for Alzheimer's disease.Complex relationships between substrate sequence and sensitivity to alterations in γ-secretase processivity induced by γ-secretase modulatorsIntramembrane proteases as drug targets.Dynamic Nature of presenilin1/γ-Secretase: Implication for Alzheimer's Disease Pathogenesis.Development of Sulfonamide Photoaffinity Inhibitors for Probing Cellular γ-Secretase.Target of γ-secretase modulators, presenilin marks the spot.Natural Product and Natural Product-Derived Gamma Secretase Modulators from Actaea Racemosa Extracts.γ-Secretase Modulators: Can We Combine Potency with Safety?Modulation of gamma-secretase for the treatment of Alzheimer's disease.Substrate determinants in the C99 juxtamembrane domains differentially affect γ-secretase cleavage specificity and modulator pharmacology.Structural and Chemical Biology of Presenilin Complexes.Binding of Bexarotene to the Amyloid Precursor Protein Transmembrane Domain in Liposomes Alters its α-Helical Conformation but Inhibits γ-Secretase Non-Selectively.
P2860
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P2860
Novel γ-secretase enzyme modulators directly target presenilin protein.
description
2011 nî lūn-bûn
@nan
2011年の論文
@ja
2011年論文
@yue
2011年論文
@zh-hant
2011年論文
@zh-hk
2011年論文
@zh-mo
2011年論文
@zh-tw
2011年论文
@wuu
2011年论文
@zh
2011年论文
@zh-cn
name
Novel γ-secretase enzyme modulators directly target presenilin protein.
@en
type
label
Novel γ-secretase enzyme modulators directly target presenilin protein.
@en
prefLabel
Novel γ-secretase enzyme modulators directly target presenilin protein.
@en
P2093
P2860
P356
P1476
Novel γ-secretase enzyme modulators directly target presenilin protein.
@en
P2093
Akio Fukumori
Amelie Ebke
Harald Steiner
Karlheinz Baumann
Keiro Shirotani
Thomas Luebbers
P2860
P304
37181-37186
P356
10.1074/JBC.C111.276972
P407
P577
2011-09-06T00:00:00Z