Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

[Image: see text] The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT members, are epigenetic “readers” and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive therapeutic targets for can...

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Foilsithe in:J Med Chem
Main Authors: Zhou, Bing, Hu, Jiantao, Xu, Fuming, Chen, Zhuo, Bai, Longchuan, Fernandez-Salas, Ester, Lin, Mei, Liu, Liu, Yang, Chao-Yie, Zhao, Yujun, McEachern, Donna, Przybranowski, Sally, Wen, Bo, Sun, Duxin, Wang, Shaomeng
Formáid: Artigo
Teanga:Inglês
Foilsithe: American Chemical Society 2017
Rochtain Ar Líne:https://ncbi.nlm.nih.gov/pmc/articles/PMC5788414/
https://ncbi.nlm.nih.gov/pubmed/28339196
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b01816
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