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Updated: Jul 10, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Histone deacetylase inhibitors for cancer therapy
Tae-You Kim1, Yung-Jue Bang, Keith D Robertson
1National Research Laboratory for Cancer Epigenetics, Cancer Research Institute, Department of Internal Medicine, Seoul National University College of Medicine, Seoul, Korea. kimty@snu.ac.kr
Abstract:
The epigenome of cancer cells is determined by DNA methylation and an array of post-translational modifications of the core histones. Epigenetic abnormalities are commonly found in human tumors and importantly, they can be reversed by pharmacologic inhibitors. Histone deacetylase inhibitors (HDACIs) represent one of the most promising epigenetic treatments for cancer. HDACIs have emerged as promising targets for cancer therapy because they reactivate the transcription of multiple genes that are silenced in human tumors and they show pleiotropic anti-tumor effects selectively in cancer cells. HDACIs are well-tolerated and several show promising anti-tumor activity. While gene transcription has been considered to be the major target of HDACIs, inhibition of acetylation of non-histone proteins is now emerging as a novel basis for their anti-tumor effects. In this review, we discuss new insights into the molecular mechanism of HDACIs, their current status of clinical development, and possible future uses in cancer therapy.
Insights
Histone deacetylase inhibitors (HDACIs) show promise in cancer therapy by reversing epigenetic abnormalities and reactivating silenced genes. New research reveals their anti-tumor effects also involve non-histone protein acetylation.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Background:
- Cancer epigenomes are characterized by DNA methylation and histone modifications.
- Epigenetic abnormalities are common in tumors and potentially reversible.
- Histone deacetylase inhibitors (HDACIs) are a promising class of epigenetic drugs for cancer treatment.
Purpose of the Study:
- To review new insights into the molecular mechanisms of HDACIs.
- To discuss the current clinical development status of HDACIs.
- To explore potential future applications of HDACIs in cancer therapy.
Main Methods:
- Review of current scientific literature on HDACIs and cancer.
- Analysis of molecular mechanisms, including gene transcription and non-histone protein acetylation.
- Summary of clinical trial data and therapeutic outcomes.
Main Results:
- HDACIs reactivate silenced genes and exhibit selective anti-tumor effects in cancer cells.
- HDACIs are generally well-tolerated with demonstrated anti-tumor activity.
- Inhibition of non-histone protein acetylation is an emerging mechanism for HDACIs' anti-tumor effects.
Conclusions:
- HDACIs represent a significant therapeutic strategy in oncology due to their epigenetic modulation.
- Understanding novel mechanisms, such as non-histone protein acetylation, will enhance HDACIs' clinical utility.
- Further clinical development and research into HDACIs hold promise for improved cancer treatment outcomes.
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