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

Jing Zhao, Yuanyuan Xiao, Xinyue Liu, Soohyun Kim, Xianzhong Wu, Marilia Barros, Ran Zhuang, Xuben Hou, Yingkai Zhang, Nikolaos K. Robakis, Yue Ming Li, Jonathan S. Dordick, Iban Ubarretxena-Belandia, Chunyu Wang

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

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.

Original languageEnglish
Pages (from-to)2578-2581
Number of pages4
JournalChemical Communications
Volume56
Issue number17
DOIs
StatePublished - 28 Feb 2020

Fingerprint

Dive into the research topics of 'Substrate interaction inhibits γ-secretase production of amyloid-β peptides'. Together they form a unique fingerprint.

Cite this