Role of BET Inhibitors in Triple Negative Breast Cancers

Durga Khandekar1, Venkataswarup Tiriveedhi1,2

  • 1Department of Biological Sciences, Tennessee State University, 3500 John A Merritt Blvd, Nashville, TN 37209, USA.

Cancers
|March 29, 2020
PubMed

Insights

Bromodomain and extraterminal domain (BET) inhibitors show promise in cancer therapy, but monotherapy results are inconclusive. Combinatorial strategies are being explored to enhance efficacy, particularly in triple-negative breast cancer.

Area of Science:

  • Molecular biology
  • Oncology
  • Pharmacology

Background:

  • Bromodomain and extraterminal domain (BET) proteins regulate gene expression, influencing cell proliferation and cancer development.
  • Preclinical data support BET inhibitors in various cancer models, leading to numerous ongoing clinical trials.

Purpose of the Study:

  • To review the molecular mechanisms of BET inhibitors in cancer.
  • To summarize preliminary clinical outcomes of BET inhibitors.
  • To focus on their application in triple-negative breast cancer.

Main Methods:

  • Literature review of preclinical and clinical studies on BET inhibitors.
  • Analysis of gene expression regulation by BET proteins.
  • Evaluation of clinical trial data for BET inhibitor efficacy.

Main Results:

  • BET inhibitors modulate transcriptional machinery involved in carcinogenesis.
  • Current clinical trials show limited efficacy for BET inhibitors as monotherapy.
  • The combinatorial potential of BET inhibitors with other cancer treatments requires further investigation.

Conclusions:

  • BET inhibitors are key regulators of gene expression with potential in cancer therapy.
  • Monotherapy with BET inhibitors has not yet proven effective in clinical settings.
  • Further research is needed to optimize combinatorial approaches involving BET inhibitors, especially for triple-negative breast cancer.

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