Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains

…, T Shen, K Morohashi, J Joshua, L Zeng…

Index: Zhang, Guangtao; Plotnikov, Alexander N.; Rusinova, Elena; Shen, Tong; Morohashi, Keita; Joshua, Jennifer; Zeng, Lei; Mujtaba, Shiraz; Ohlmeyer, Michael; Zhou, Ming-Ming Journal of Medicinal Chemistry, 2013 , vol. 56, # 22 p. 9251 - 9264

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Citation Number: 34

Abstract

BRD4, characterized by two acetyl-lysine binding bromodomains and an extra-terminal (ET) domain, is a key chromatin organizer that directs gene activation in chromatin through transcription factor recruitment, enhancer assembly, and pause release of the RNA polymerase II complex for transcription elongation. BRD4 has been recently validated as a new epigenetic drug target for cancer and inflammation. Our current knowledge of the ...