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The emerging role of BET inhibitors in breast cancer

Angeliki Andrikopoulou1, Michalis Liontos1, Konstantinos Koutsoukos1

  • 1Oncology Unit, Department of Clinical Therapeutics, Alexandra Hospital, National and Kapodistrian University of Athens School of Medicine, Athens, Greece.

Breast (Edinburgh, Scotland)
|August 23, 2020
PubMed

Insights

Bromodomain and extraterminal domain (BET) inhibitors show promise for breast cancer by targeting gene expression. Clinical trials are ongoing, with early results suggesting efficacy when combined with other cancer therapies.

Area of Science:

  • Epigenetics
  • Molecular Biology
  • Oncology

Background:

  • Breast cancer exhibits heterogeneity driven by aberrant gene expression and epigenetic alterations.
  • Bromodomain and extraterminal domain (BET) proteins are epigenetic regulators implicated in carcinogenesis.
  • Overexpression of BET proteins is observed in breast tumors, indicating clinical relevance.

Purpose of the Study:

  • To review preclinical and clinical evidence of BET inhibitors in breast cancer treatment.
  • To summarize the mechanism of action and therapeutic potential of BET inhibitors.
  • To discuss current clinical trial status and emerging toxicities.

Main Methods:

  • Review of preclinical studies on BET inhibitors in breast cancer cell lines and xenograft models.
  • Analysis of data from Phase I/II clinical trials investigating BET inhibitors in solid tumors and breast cancer.
  • Evaluation of in vitro studies assessing the sensitization of breast tumors to various therapies by BET inhibition.

Main Results:

  • BET inhibitors disrupt BET protein binding to chromatin, suppressing oncogene transcription.
  • Promising results observed in breast cancer cells and xenograft models.
  • Phase I/II trials are evaluating safety and efficacy, with reported toxicities like thrombocytopenia.
  • Preliminary data indicate enhanced response rates when BET inhibitors are combined with existing anticancer agents.
  • In vitro studies show BET inhibition sensitizes breast tumors to chemotherapy, hormone therapy, and PI3K inhibitors.

Conclusions:

  • BET inhibitors represent a promising therapeutic strategy for breast cancer.
  • Combination therapies involving BET inhibitors demonstrate enhanced efficacy.
  • Further clinical investigation is warranted to optimize safety and effectiveness.
Keywords:
BET inhibitorsBreast cancerBromodomainsDrug discoveryEpigenetic agentsTriple negative

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