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Updated: Mar 26, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Potential use of histone deacetylase inhibitors in cancer therapy
Karolina Gołąbek1, Joanna K Strzelczyk1, Andrzej Wiczkowski1
1Chair and Department of Medical and Molecular Biology, School of Medicine with the Division of Dentistry, Medical University of Silesia, Katowice, Poland.
Abstract:
Epigenetics is a branch of science that focuses on mechanisms related to control and modification of expression of genetic material without any changes to its sequences. Such mechanisms include post-translational modifications of histones. It is widely known that carcinogenesis is related to hypoacetylation of genes that influence apoptosis, the cell cycle, cell signaling, the immunologic response, angiogenesis and occurrence of metastasis. Currently conducted research focuses on several strategies related to epigenetic therapy. One such strategy is based on the use of histone deacetylase inhibitors. This paper presents mechanisms through which these compounds work and a summary of their characteristics. It also includes a review of clinical tests related to histone deacetylase inhibitors, as well as their relationship with other chemotherapeutic methods. A better understanding of the involved mechanisms will provide a rational basis to improve the therapeutic outcome of available antitumor agents.
Insights
Histone deacetylase inhibitors offer a promising epigenetic therapy strategy by targeting gene expression in cancer. Research explores their mechanisms, clinical trials, and combination with chemotherapy for improved antitumor outcomes.
Area of Science:
- Epigenetics
- Molecular Biology
- Cancer Research
Background:
- Epigenetics involves modifying gene expression without altering DNA sequence, including histone modifications.
- Carcinogenesis is linked to hypoacetylation of genes controlling critical cellular processes like apoptosis, cell cycle, and metastasis.
- Epigenetic therapy is an emerging strategy to counteract cancer-driving epigenetic changes.
Purpose of the Study:
- To review the mechanisms of action for histone deacetylase inhibitors (HDACi).
- To summarize the characteristics of HDACi.
- To present a review of clinical trials involving HDACi and their integration with chemotherapy.
Main Methods:
- Literature review of epigenetic mechanisms in cancer.
- Analysis of histone deacetylase inhibitor characteristics and functions.
- Review of clinical trial data for HDAC inhibitors in cancer treatment.
Main Results:
- Histone deacetylase inhibitors work by reversing gene silencing associated with hypoacetylation.
- HDAC inhibitors have demonstrated potential in modulating cancer-related pathways.
- Clinical trials are evaluating the efficacy and safety of HDAC inhibitors, alone and in combination therapies.
Conclusions:
- Understanding HDAC inhibitor mechanisms is crucial for enhancing their therapeutic efficacy.
- HDAC inhibitors represent a significant area of development in epigenetic cancer therapy.
- Further research and clinical evaluation are needed to optimize the use of HDAC inhibitors in combination with other anticancer agents.
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