Title:An Overview on Small Molecule Inhibitors of BRD4
Volume: 16
Issue: 17
Author(s): Wenhai Huang, Xiaoliang Zheng, Yewei Yang, Xiaoju Wang and Zhengrong Shen
Affiliation:
Keywords:
BRD4 inhibitor, bromodomain, JQ1, target therapy.
Abstract: BRD4, an epigenetic regulator that recognizes and binds the acetylated
lysine residues in histone, has been reported as a potential therapeutic target for
cancers. Since the first BRD4 inhibitor JQ1 developed in 2010, numerous BRD4
inhibitors have been discovered in past five years. In this review, we have
systematically summarized a series of BRD4 binding compounds, which are divided
into five categories based on the similarity of their chemical structures and
respectively referred as JQ1 derivatives, tetrahydroquinoline derivatives, 3,5-
dimethylisoxazole derivatives, 2-thiazolidinone derivatives and others. The binding
affinities for each class of compounds are also discussed.