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Updated: Feb 20, 2026

Utilization of the Soft Agar Colony Formation Assay to Identify Inhibitors of Tumorigenicity in Breast Cancer Cells
Published on: May 20, 2015
BET inhibitors as novel therapeutic agents in breast cancer
Alberto Ocaña1, Cristina Nieto-Jiménez1, Atanasio Pandiella2
1Unidad de Investigación Traslacional, Hospital Universitario de Albacete, Universidad de Castilla La Mancha, Albacete, Spain.
Abstract:
Tumoral cells not only depend on oncogenic abnormalities to maintain its malignant phenotype but on non-oncogenic vulnerabilities. Targeting epigenomics can modify specific cellular functions required for malignant transformation. The Bromodomain (BRD) family mediates their effect by recruiting proteins of the transcription machinery, recognizing acetylated-lysine residues in nucleosomal histones. Bromodomain and extra-terminal (BET) inhibitors have shown to produce growth inhibition in several tumors through the inhibition of the expression of several transcription factors. In this review we will discuss the current knowledge regarding BET inhibitors in breast cancer. Recent data demonstrates their antiproliferative effect in several cancer subtypes, including the triple negative subtype, or when combined with cell signaling inhibitors. We will also describe options for therapeutic combinations or potential mechanisms of resistance, with special emphasis on their future clinical development.
Insights
Bromodomain and extra-terminal (BET) inhibitors show promise in treating breast cancer by halting tumor cell growth. This review explores their effectiveness, especially in triple-negative breast cancer, and future clinical applications.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Background:
- Malignant cells exploit oncogenic and non-oncogenic vulnerabilities.
- Epigenomic targeting can modulate cellular functions crucial for cancer development.
- Bromodomain and extra-terminal (BET) inhibitors target transcription machinery by recognizing acetylated histones.
Purpose of the Study:
- To review the current knowledge on BET inhibitors in breast cancer treatment.
- To discuss the antiproliferative effects of BET inhibitors across various breast cancer subtypes.
- To explore therapeutic combinations, resistance mechanisms, and future clinical development of BET inhibitors.
Main Methods:
- Literature review of preclinical and clinical studies on BET inhibitors in breast cancer.
- Analysis of data on the efficacy of BET inhibitors in different breast cancer subtypes, including triple-negative breast cancer.
- Examination of studies investigating combinations of BET inhibitors with other therapies and mechanisms of resistance.
Main Results:
- BET inhibitors demonstrate antiproliferative effects in several breast cancer subtypes.
- Efficacy is noted in triple-negative breast cancer and in combination with cell signaling inhibitors.
- Potential therapeutic combinations and mechanisms of resistance have been identified.
Conclusions:
- BET inhibitors represent a promising therapeutic strategy for breast cancer.
- Further research into combinations and resistance mechanisms is crucial for clinical development.
- Future clinical trials are warranted to establish the role of BET inhibitors in breast cancer treatment.
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