Recent Developments in Targeting Bromodomain and Extra Terminal Domain Proteins for Cancer Therapeutics.

Bromodomain and extra-terminal domain (BET) proteins are a well-studied family of proteins associated with a variety of diseases including malignancy and chronic inflammation. Currently, numerous pan BET inhibitors have exhibited potent efficacy in several in vivo preclinical models and entered clinical trials, but have largely stalled due to their adverse events. Therefore, the development of new selective inhibitors and PROTACs (Proteolysis Targeting Chimeras) targeting BET is urgently needed. In the present review, we summarize the BET protein structure, the recent development of BET inhibitors, focusing mainly on BRD4-selective inhibitors and PROTAC degraders.

• Publication year

  2022

• Venue

  Current Medicinal Chemistry

• Publication date

  2022-02-11

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.2174/0929867329666220211091806PMID 35152859
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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