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Current Drug Targets

Author(s): Yingying Shi, Jingwen Liu, Yuanyuan Zhao, Jiaoxian Cao, Yiming Li* and Fujiang Guo*

DOI: 10.2174/1574885514666190618113519

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Bromodomain-Containing Protein 4: A Druggable Target

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Abstract

Bromodomain-containing protein 4 (BRD4) belongs to the bromodomain and extraterminal family. BRD4 inhibitors can regulate acetylated lysine and form protein complexes that initiate transcriptional programs as an epigenetic regulator of the histone code. BRD4 was initially considered to be one of the most promising targets for combating malignant tumors. However, many recent studies have shown that BRD4 plays a crucial role in various kinds of diseases, including cancer, coronary heart disease, neurological disorder, and obesity. Currently, several BRD4 inhibitors are undergoing clinical trials. A search for new BRD4 inhibitors appears to be of great utility for developing novel drugs. In this mini-review, we highlight the inhibitors of BRD4 from natural products and synthesized sources, as well as their applications in cancer, glucolipid metabolism, inflammation, neuronal stimulation activation, human immunodeficiency virus and renal fibrosis.

Keywords: Bromodomain-containing protein 4, small molecule inhibitors, pharmacology, tumor, coronary heart disease, natural products, synthetic compounds.

Graphical Abstract

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