Dual-target Inhibitors Based on BRD4: Novel Therapeutic Approaches for Cancer

(E-pub Ahead of Print)

Author(s): Sitao Zhang, Yanzhao Chen, Chengsen Tian, Yujing He, Zeru Tian, Yichao Wan, Tingting Liu*

Journal Name: Current Medicinal Chemistry

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Bromodomain and Extraterminal domain (BET) proteins are a family of important proteins to build transcriptionpromoting complexes by reading acetylated chromatin status and accumulating on transcriptionally active regulatory elements. BRD4 as an important member of BET family proteins can assist the expression of various well-known oncogenes, indicating that inhibiting BRD4 is an effective strategy for cancer treatment. In view of the fact that BRD4 inhibitor and inhibitors of some enzymatic/non-enzymatic proteins share many common targets and do similar effects on cellular processes, combined inhibition of BRD4 and these proteins is regarded as a rational strategy to improve treatment efficacy. In this review, we summarize the molecular interplay between BRD4 and other proteins. Moreover, we summarize the corresponding dual targeting inhibitors, for example HDAC/BRD4 dual inhibitors, PLK1/BRD4 dual inhibitors, PI3K/BRD4 dual inhibitors and so on, in cancer therapy and we make an insight into the structure-activity relationships of these dual-target agents.

Keywords: BRD4, drug design, anti-cancer, dual-target, enzymatic/non-enzymatic protein, combined.

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(E-pub Ahead of Print)
DOI: 10.2174/0929867327666200610174453
Price: $95

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