2. Academic Validation
  3. Dual-target inhibitors of bromodomain-containing protein 4 (BRD4) in cancer therapy: Current situation and future directions

Dual-target inhibitors of bromodomain-containing protein 4 (BRD4) in cancer therapy: Current situation and future directions

  • Drug Discov Today. 2022 Jan;27(1):246-256. doi: 10.1016/j.drudis.2021.08.007.
Wenke Jin 1,  Huidan Tan 1,  Junhao Wu 1,  Gu He 2,  Bo Liu 3
Affiliations

Affiliations

  • 1 State Key Laboratory of Biotherapy and Cancer Center and Department of Otolaryngology, Head and Neck Surgery, West China Hospital, Sichuan University, Chengdu 610041, China.
  • 2 State Key Laboratory of Biotherapy and Cancer Center and Department of Otolaryngology, Head and Neck Surgery, West China Hospital, Sichuan University, Chengdu 610041, China. Electronic address: [email protected].
  • 3 State Key Laboratory of Biotherapy and Cancer Center and Department of Otolaryngology, Head and Neck Surgery, West China Hospital, Sichuan University, Chengdu 610041, China. Electronic address: [email protected].
PMID: 34438075 DOI: 10.1016/j.drudis.2021.08.007
Abstract

Bromodomain-containing protein 4 (BRD4) is emerging as a therapeutic target that acts synergistically with other targets of small-molecule drugs in Cancer. Therefore, the discovery of potential new dual-target inhibitors of BRD4 may be a promising strategy for Cancer therapy. In this review, we highlight a series of strategies to design therapeutic dual-target inhibitors of BRD4 that focus on the synergistic functions of this protein. Drug combinations that exploit synthetic lethality, protein-protein interactions, functional complementarity, and blocking of resistance mechanisms could ultimately overcome the barriers inherent to the development of BRD4 inhibitors as future Cancer drugs.

Keywords

Bromodomain-containing protein 4 (BRD4); Cancer therapy; Designing strategy; Dual-target inhibitor; Small-molecule drug.

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