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PROTACs for BRDs proteins in cancer therapy: a review

Chao Wang1, Yujing Zhang2,3, Shanbo Yang1

  • 1The Affiliated Hospital of Qingdao University, Qingdao Cancer Institute, Qingdao University, Qingdao, PR China.

Journal of Enzyme Inhibition and Medicinal Chemistry
|June 15, 2022
PubMed

Insights

Bromodomain and extra-terminal domain (BET) proteins are key epigenetic readers. Proteolysis-Targeting Chimaeras (PROTACs) offer a novel therapeutic strategy to degrade BET proteins for cancer treatment, overcoming limitations of traditional drugs.

Area of Science:

  • Biochemistry
  • Epigenetics
  • Medicinal Chemistry

Background:

  • Bromodomain and extra-terminal domain (BET) proteins are crucial epigenetic readers and transcription coactivators.
  • Dysregulation of BET proteins is implicated in various diseases, notably cancer.
  • Conventional therapeutic approaches targeting BET proteins face limitations in efficacy and specificity.

Purpose of the Study:

  • To provide a comprehensive overview of Proteolysis-Targeting Chimaeras (PROTACs) for BET protein regulation in cancer.
  • To highlight the potential and challenges of utilizing PROTACs as a therapeutic strategy against BET proteins.

Main Methods:

  • Review of existing literature on BET protein inhibitors and PROTAC technology.
  • Analysis of the development and application of small-molecule PROTACs targeting BET proteins.
  • Discussion of the advantages and limitations of PROTACs compared to traditional inhibitors.

Main Results:

  • Development of potent and efficacious small-molecule PROTACs targeting BET proteins has been reported.
  • PROTACs offer a promising approach to selectively degrade disease-associated BET proteins.
  • PROTACs demonstrate potential for enhanced therapeutic efficacy in cancer treatment.

Conclusions:

  • PROTACs represent an advanced therapeutic modality for targeting BET proteins in cancer.
  • Further research and development are needed to overcome challenges and fully realize the therapeutic potential of BET-targeting PROTACs.
  • PROTAC technology holds significant promise for novel cancer therapies by enabling targeted protein degradation.
Keywords:
BRDs proteinsPROTACsdegradationinhibitorpromising treatment

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