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

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 IC(50). Our work suggests that targeting...

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Detalles Bibliográficos
Autores principales: Zhao, Jing, Xiao, Yuanyuan, Liu, Xinyue, Kim, Soohyun, Wu, Xianzhong, Barros, Marilia, Zhuang, Ran, Hou, Xuben, Zhang, Yingkai, Robakis, Nikolaos K., Li, Yue-Ming, Dordick, Jonathan S., Ubarretxena-Belandia, Iban, Wang, Chunyu
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8219260/
https://www.ncbi.nlm.nih.gov/pubmed/32016207
http://dx.doi.org/10.1039/c9cc09170j