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Updated: Mar 24, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Histone deacetylase inhibitors as immunomodulators in cancer therapeutics
Li Shen1, Ashley Orillion1,2, Roberto Pili1,2
1Genitourinary Program, Roswell Park Cancer Institute, Buffalo, NY, 14263, USA.
Abstract:
HDAC inhibitors (HDACIs) are anticancer agents being developed in preclinical and clinical settings due to their capacity to modulate gene expression involved in cell growth, differentiation and apoptosis, through modification of both chromatin histone and nonhistone proteins. Most HDACIs in clinical development have cytotoxic or cytostatic properties and their direct inhibitory effects on tumor cells are well documented. Numerous studies have revealed that HDACIs have potent immunomodulatory activity in tumor-bearing animals and cancer patients, providing guidance to apply these agents in cancer immunotherapies. Here, we summarize recent reports addressing the effects of HDACIs on tumor cell immunogenicity, and on different components of the host immune system. In addition, we discuss the complexity of the immunomodulatory activity of these agents, which depends on the class specificity of the HDACIs, different experimental settings and the target immune cell populations.
Insights
Histone deacetylase inhibitors (HDACIs) are anticancer drugs that can boost the immune system. Their complex effects on cancer immunotherapy depend on the specific drug class and immune cells targeted.
Area of Science:
- Oncology
- Immunology
- Epigenetics
Background:
- Histone deacetylase inhibitors (HDACIs) are anticancer agents targeting gene expression via chromatin modification.
- HDACIs exhibit cytotoxic and cytostatic effects on tumor cells, with established clinical development.
- Emerging evidence highlights potent immunomodulatory activities of HDACIs in preclinical and clinical cancer studies.
Purpose of the Study:
- To summarize recent findings on HDACIs' effects on tumor cell immunogenicity.
- To review the impact of HDACIs on various components of the host immune system.
- To discuss the complex and context-dependent immunomodulatory activities of HDACIs.
Main Methods:
- Literature review of preclinical and clinical studies on HDACIs.
- Analysis of data on HDACIs' effects on tumor cells and immune cells.
- Synthesis of information regarding class-specific and setting-dependent HDACIs' activities.
Main Results:
- HDACIs modulate tumor cell immunogenicity and interact with multiple immune system components.
- The immunomodulatory effects of HDACIs are intricate and vary based on HDACIs class specificity.
- Experimental settings and targeted immune cell populations significantly influence HDACIs' immunomodulatory outcomes.
Conclusions:
- HDACIs possess significant immunomodulatory potential for cancer immunotherapy.
- Understanding the nuances of HDACIs' immune effects is crucial for optimizing their therapeutic application.
- Further research is warranted to elucidate the complex interplay between HDACIs, tumor cells, and the immune system.
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