2. Academic Validation
  3. PROTACs for BRDs proteins in cancer therapy: a review

PROTACs for BRDs proteins in cancer therapy: a review

  • J Enzyme Inhib Med Chem. 2022 Dec;37(1):1694-1703. doi: 10.1080/14756366.2022.2081164.
Chao Wang 1,  Yujing Zhang 2 3,  Shanbo Yang 1,  Wujun Chen 1,  Dongming Xing 1 4
Affiliations

Affiliations

  • 1 The Affiliated Hospital of Qingdao University, Qingdao Cancer Institute, Qingdao University, Qingdao, PR China.
  • 2 The Affiliated Cardiovascular Hospital of Qingdao University, Qingdao University, Qingdao, PR China.
  • 3 School of Pharmacy, Qingdao University, Qingdao, PR China.
  • 4 School of Life Sciences, Tsinghua University, Beijing, PR China.
PMID: 35702740 DOI: 10.1080/14756366.2022.2081164
Abstract

BRDs proteins that recognise chromatin acetylation regulate gene expression, are epigenetic readers and master transcription coactivators. BRDs proteins are now emerging as targets for new therapeutic development. Blocking the function of any of BRDs proteins can be a control agent for diseases, such as Cancer. Traditional drugs like Enzyme inhibitors and protein-protein inhibitors have many limitations. The therapeutic efficacy of them remains to be proven. Recently, Proteolysis-Targeting Chimaeras (PROTACs) have become an advanced tool in therapeutic intervention as they remove disease-causing proteins. Extremely potent and efficacious small-molecule PROTACs of the BRDs proteins, based on available, potent, and selective BRDs inhibitors, have been reported. This review presents a comprehensive overview of the development of PROTACs for BRDs proteins regulation in Cancer, and the chances and challenges associated with this area are also highlighted.

Keywords

BRDs proteins; PROTACs; degradation; inhibitor; promising treatment.

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