An Overview on Small Molecule Inhibitors of BRD4

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:

• Institute of Materia Medica, Zhejiang Academy of Medical Sciences, Hangzhou, China.,China

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.

Cite this article as:

Huang Wenhai, Zheng Xiaoliang, Yang Yewei, Wang Xiaoju and Shen Zhengrong, An Overview on Small Molecule Inhibitors of BRD4, Mini-Reviews in Medicinal Chemistry 2016; 16(17) . https://dx.doi.org/10.2174/1389557516666160611014130