Discovery, SAR, and X-ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library

[Image: see text] As a potential target for obesity, human BCATm was screened against more than 14 billion DNA encoded compounds of distinct scaffolds followed by off-DNA synthesis and activity confirmation. As a consequence, several series of BCATm inhibitors were discovered. One representative com...

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Bibliographic Details
Published in:ACS Med Chem Lett
Main Authors: Deng, Hongfeng, Zhou, Jingye, Sundersingh, Flora S., Summerfield, Jennifer, Somers, Don, Messer, Jeffrey A., Satz, Alexander L., Ancellin, Nicolas, Arico-Muendel, Christopher C., (Sargent) Bedard, Katie L., Beljean, Arthur, Belyanskaya, Svetlana L., Bingham, Ryan, Smith, Sarah E., Boursier, Eric, Carter, Paul, Centrella, Paolo A., Clark, Matthew A., Chung, Chun-wa, Davie, Christopher P., Delorey, Jennifer L., Ding, Yun, Franklin, G. Joseph, Grady, LaShadric C., Herry, Kenny, Hobbs, Clare, Kollmann, Christopher S., Morgan, Barry A., (Pothier) Kaushansky, Laura J., Zhou, Quan
Format: Artigo
Language:Inglês
Published: American Chemical Society 2015
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC4538436/
https://ncbi.nlm.nih.gov/pubmed/26288694
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00179
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