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Bromodomain and extraterminal domain protein bromodomain inhibitor based cancer therapeutics

Tithi Ghosh Halder1, Raffaella Soldi, Sunil Sharma

  • 1Applied Cancer Research and Drug Discovery, Translational Genomics Research Institute (TGen), Phoenix, Arizona, USA.

Current Opinion in Oncology
|July 19, 2021
PubMed
Abstract

Insights

Bromodomain and extraterminal domain (BET) inhibitors show anticancer potential but are not effective as monotherapy. Combination therapies and next-generation inhibitors offer promising avenues for personalized cancer treatment.

Area of Science:

  • Molecular Biology
  • Genetics
  • Pharmacology

Background:

  • Bromodomain and extraterminal domain (BET) proteins regulate gene transcription by recognizing acetyl-lysine.
  • BET inhibitors target these super-regulators, suppressing cancer-promoting genes.

Purpose of the Study:

  • To review the molecular basis of BET inhibitors.
  • To summarize preliminary clinical outcomes of BET inhibitors in cancer treatment.

Main Methods:

  • Literature review of studies on BET inhibitors.
  • Analysis of clinical trial data for BET inhibitors.

Main Results:

  • Early clinical trials confirm antitumor potential of BET inhibitors in hematologic and solid tumors.
  • BET inhibitors are not effective as monotherapy and can cause toxicities like thrombocytopenia.
  • Preclinical data suggest efficacy in combination therapies.

Conclusions:

  • BET inhibitors show promise in combination therapy for cancer.
  • Further research is needed to identify predictive biomarkers for personalized medicine.
  • Next-generation BET inhibitors may offer improved therapeutic outcomes.

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