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Updated: Feb 22, 2026
Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Targeting triple negative breast cancer with histone deacetylase inhibitors
Palma Fedele1, Laura Orlando1, Saverio Cinieri1
1a Medical Oncology & Breast Unit , "Antonio Perrino" Hospital , Brindisi , Italy.
Introduction:
Triple negative breast cancer (TNBC) is a heterogeneous disease characterized by poor outcomes, higher rates of relapse, lack of biomarkers for rational use of targeted treatments and insensitivity to current available treatments. Histone deacetylase inhibitors (HDACis) perform multiple cytotoxic actions and are emerging as promising multifunctional agents in TNBC. Areas covered: This review focuses on the challenges so far addressed in the targeted treatment of TNBC and explores the various mechanisms by which HDACis control cancer cell growth, tumor progression and metastases. Pivotal preclinical trials on HDACis like panobinostat, vorinostat, and entinostat show that these epigenetic agents exert an anti-proliferative effect on TNBC cells and control tumor growth by multiple mechanisms of action, including apoptosis and regulation of the epithelial to mesenchimal transition (EMT). Combination studies have reported the synergism of HDACis with other anticancer agents. Expert opinion: In recent years, treatment of TNBC has recorded a high number of failures in the development of targeted agents. HDACis alone or in combination strategies show promising activity in TNBC and could have implications for the future targeted treatment of TNBC patients. Future research should identify which agent synergizes better with HDACis and which patient will benefit more from these epigenetic agents.
Insights
Triple negative breast cancer (TNBC) treatments face challenges. Histone deacetylase inhibitors (HDACis) show promise as multifunctional agents, controlling cancer growth and progression through various mechanisms, alone or in combination therapies.
Area of Science:
- Oncology
- Epigenetics
- Cancer Therapeutics
Background:
- Triple negative breast cancer (TNBC) presents significant challenges due to its heterogeneity, poor prognosis, and lack of targeted treatment biomarkers.
- Current treatments for TNBC are often ineffective, highlighting the need for novel therapeutic strategies.
Purpose of the Study:
- To review the challenges in targeted TNBC treatment.
- To explore the mechanisms of histone deacetylase inhibitors (HDACis) in controlling TNBC progression.
- To evaluate the potential of HDACis as multifunctional agents in TNBC therapy.
Main Methods:
- Review of preclinical trials investigating HDACis such as panobinostat, vorinostat, and entinostat.
- Analysis of studies on HDACis' mechanisms of action, including apoptosis and epithelial-to-mesenchymal transition (EMT) regulation.
- Examination of combination studies involving HDACis and other anticancer agents.
Main Results:
- Preclinical data indicate that HDACis exert anti-proliferative effects on TNBC cells.
- HDACis demonstrate multifaceted mechanisms to control tumor growth, metastasis, and cancer cell proliferation.
- Combination therapies involving HDACis show synergistic effects with other anticancer agents.
Conclusions:
- Histone deacetylase inhibitors (HDACis) represent promising multifunctional agents for TNBC treatment.
- HDACis, used alone or in combination, exhibit promising activity and potential for future TNBC targeted therapies.
- Further research is needed to identify optimal synergistic partners and patient populations for HDACis in TNBC treatment.
