化学
BRD4
X射线晶体学
溴尿嘧啶
X射线
结晶学
立体化学
生物化学
结合位点
组合化学
DNA
组蛋白
衍射
量子力学
光学
物理
作者
Zhiqing Liu,Yi Li,Haiying Chen,Hsien‐Tsung Lai,Pingyuan Wang,Szu‐Yuan Wu,Eric A. Wold,Paul G. Leonard,Sarah Joseph,Haitao Hu,Cheng‐Ming Chiang,Allan R. Brasier,Bing Tian,Jia Zhou
标识
DOI:10.1021/acs.jmedchem.1c01851
摘要
Bromodomain-containing protein 4 (BRD4) is an emerging epigenetic drug target for intractable inflammatory disorders. The lack of highly selective inhibitors among BRD4 family members has stalled the collective understanding of this critical system and the progress toward clinical development of effective therapeutics. Here we report the discovery of a potent BRD4 bromodomain 1 (BD1)-selective inhibitor ZL0590 (
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