An Overview on Small Molecule Inhibitors of BRD4

被引：23

作者：

Huang, Wenhai ^{[1
]}

Zheng, Xiaoliang ^{[2
]}

Yang, Yewei ^{[1
]}

Wang, Xiaoju ^{[2
]}

Shen, Zhengrong ^{[1
]}

机构：

[1] Zhejiang Acad Med Sci, Inst Mat Med, Hangzhou, Zhejiang, Peoples R China

[2] Zhejiang Acad Med Sci, Ctr Mol Med, Hangzhou, Zhejiang, Peoples R China

来源：

MINI-REVIEWS IN MEDICINAL CHEMISTRY | 2016年 / 16卷 / 17期

基金：

中国国家自然科学基金;

关键词：

BRD4; inhibitor; bromodomain; JQ1; target therapy; BROMODOMAIN INHIBITORS; P-TEFB; THERAPEUTIC TARGET; PROTEIN; DISCOVERY; BINDING; STIMULATION; ACETYLATION; RECRUITMENT; HOMOLOG;

D O I：

10.2174/1389557516666160611014130

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：1403 / 1414

页数：12

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