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Updated: Nov 12, 2025

Evaluating the Effectiveness of Cancer Drug Sensitization In Vitro and In Vivo
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Achieving clinical success with BET inhibitors as anti-cancer agents

Tatiana Shorstova1, William D Foulkes2, Michael Witcher3

  • 1Departments of Oncology and Experimental Medicine, McGill University, Lady Davis Institute and Segal Cancer Centre, Jewish General Hospital, Montreal, QC, Canada.

British Journal of Cancer
|March 16, 2021
PubMed

Insights

Bromo- and extra-terminal domain (BET) inhibitors offer a new way to target cancer by switching off oncogenic pathways. Research advances BET inhibitor design, identifies biomarkers, and explores combination therapies for improved cancer treatment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Transcriptional upregulation of oncogenes drives tumor progression.
  • Targeting oncogenic pathways was historically challenging.
  • Bromo- and extra-terminal domain (BET) proteins are key activators of oncogenic networks in various cancers.

Purpose of the Study:

  • To discuss the biology of BET proteins.
  • To review advances in BET inhibitor (BETi) design.
  • To highlight potential biomarkers for BETi activity and explore combination therapy strategies.

Main Methods:

  • Review of existing literature on BET protein biology and BET inhibitors.
  • Analysis of BET protein function dependent on bromodomains (BD1 and BD2) for chromatin recruitment.
  • Discussion of biomarker identification and combination therapy logic.

Main Results:

  • BET proteins are crucial for activating oncogenic networks.
  • Potent BET inhibitors targeting bromodomains have been developed.
  • Potential biomarkers for predicting BETi activity exist.
  • Combination therapies with BETi may enhance efficacy.

Conclusions:

  • BET inhibitors represent a significant advancement in suppressing oncogenic networks.
  • Understanding BET protein mechanisms, defining predictive biomarkers, and identifying synergistic combinations are crucial for clinical success.
  • BET inhibitors offer a promising therapeutic strategy for various cancers.

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