Design of Bcl-2 and Bcl-xL Inhibitors with Subnanomolar Binding Affinities Based Upon a New Scaffold

Employing a structure-based strategy, we have designed a new class of potent small-molecule inhibitors of the anti-apoptotic proteins Bcl-2 and Bcl-xL. An initial lead compound with a new scaffold was designed based upon the crystal structure of Bcl-xL and FDA-approved drugs and was found to have an...

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Bibliografiske detaljer
Main Authors:	Zhou, Haibin, Chen, Jianfang, Meagher, Jennifer L., Yang, Chao-Yie, Aguilar, Angelo, Liu, Liu, Bai, Longchuan, Cong, Xin, Cai, Qian, Fang, Xueliang, Stuckey, Jeanne A., Wang, Shaomeng
Format:	Artigo
Sprog:	Inglês
Udgivet:	2012
Fag:	Article
Online adgang:	https://ncbi.nlm.nih.gov/pmc/articles/PMC3397176/ https://ncbi.nlm.nih.gov/pubmed/22448988 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm300178u
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Design of Bcl-2 and Bcl-xL Inhibitors with Subnanomolar Binding Affinities Based Upon a New Scaffold

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