Substrate interaction inhibits γ-secretase production of amyloid-β peptides.

ABSTRACT: Combining NMR, mass spectrometry, AlphaLISA and cell assays, we discovered a compound C1 that binds C-terminal juxtamembrane lysines at the transmembrane domain of the amyloid precursor protein (APPTM) and inhibits γ-secretase production of amyloid-β with μM IC50. Our work suggests that targeting APPTM is a novel and viable strategy in AD drug discovery.

SUBMITTER: Zhao J 

PROVIDER: S-EPMC8219260 | biostudies-literature | 2020 Feb

REPOSITORIES: biostudies-literature