Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aβ Reduction in Rodents

[Image: see text] By targeting the flap backbone of the BACE1 active site, we discovered 6-dimethylisoxazole-substituted biaryl aminothiazine 18 with 34-fold improved BACE1 inhibitory activity over the lead compound 1. The cocrystal structure of 18 bound to the active site indicated two hydrogen-bon...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Wu, Yong-Jin, Guernon, Jason, Yang, Fukang, Snyder, Lawrence, Shi, Jianliang, Mcclure, Andrea, Rajamani, Ramkumar, Park, Hyunsoo, Ng, Alicia, Lewis, Hal, Chang, ChiehYing, Camac, Dan, Toyn, Jeremy H., Ahlijanian, Michael K., Albright, Charles F., Macor, John E., Thompson, Lorin A.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2016
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4789663/
https://ncbi.nlm.nih.gov/pubmed/26985314
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00432
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