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Updated: Dec 25, 2025

Studying Triple Negative Breast Cancer Using Orthotopic Breast Cancer Model
Published on: March 20, 2020
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.
Abstract:
Bromodomain and extraterminal domain (BET) proteins have evolved as key multifunctional super-regulators that control gene expression. These proteins have been shown to upregulate transcriptional machinery leading to over expression of genes involved in cell proliferation and carcinogenesis. Based on favorable preclinical evidence of BET inhibitors in various cancer models; currently, 26 clinical trials are underway in various stages of study on various hematological and solid organ cancers. Unfortunately, preliminary evidence for these clinical studies does not support the application of BET inhibitors as monotherapy in cancer treatment. Furthermore, the combinatorial efficiency of BET inhibitors with other chemo-and immunotherapeutic agents remain elusive. In this review, we will provide a concise summary of the molecular basis and preliminary clinical outcomes of BET inhibitors in cancer therapy, with special focus on triple negative breast cancer.
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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