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

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

文献索引：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

全文：HTML全文

被引用次数: 34

摘要

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 ...