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A comprehensive review of BET-targeting PROTACs for cancer therapy

Xiao-Li Zhou1, Fang Zhao2, Yong-Tao Xu2

  • 1Sanquan college of Xinxiang Medical University, 453003 Xinxiang, Henan Province, PR China.

Bioorganic & Medicinal Chemistry
|October 6, 2022
PubMed

Insights

Proteolysis-targeting chimeras (PROTACs) offer advantages over traditional inhibition for drug discovery. This review summarizes recent advances in BET-targeting PROTACs for cancer therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Targeted protein degradation using proteolysis-targeting chimeras (PROTACs) is a promising drug discovery strategy.
  • Bromodomain and extra-terminal (BET) proteins are key regulators of oncogene expression and cancer progression.

Purpose of the Study:

  • To provide a comprehensive summary of recent advances in BET-targeting PROTACs.
  • To highlight novel strategies and E3 ligases utilized in BET-targeting PROTAC development.

Main Methods:

  • Review of recent scientific literature on BET-targeting PROTACs.
  • Analysis of novel PROTAC strategies including light-activated, macrocyclic, and antibody-coupling approaches.

Main Results:

  • Significant progress has been made in developing BET-targeting PROTACs.
  • Emerging strategies include light-activation, macrocyclic designs, and conjugation with aptamers or antibodies.

Conclusions:

  • BET-targeting PROTACs represent a rapidly advancing field with significant therapeutic potential in cancer.
  • Novel E3 ligases and innovative strategies are expanding the utility of PROTACs for targeting BET proteins.
Keywords:
BETCancerDegradationPROTACs

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