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Updated: Jun 9, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Recent advances in histone deacetylase targeted cancer therapy
Isamu Hoshino1, Hisahiro Matsubara
1Department of Frontier Surgery, Graduate School of Medicine, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8670, Japan.
Abstract:
Epigenetic regulators such as histone acetyltransferases (HATs) and histone deacetylases (HDACs) are known to play an important role in gene expression. Of these enzymes, HDACs have been shown to be commonly associated with many types of cancers and to affect cancer development. Consequently, HDACs have been considered as promising targets for cancer therapy. In addition, the inhibition of HDACs by histone deacetylase inhibitors (HDACIs) shifts the balance between the deacetylating activity of HDACs and the acetylating activity of HATs in the regulation of gene expression. Therefore, HDACIs are an exciting new addition in cancer therapies. Numerous HDACIs have been identified and some have recently been used in clinical trials for cancer treatment, although the mechanisms underlying the anticancer effects of HDACIs remain unclear. In this review, we examine the most recent developments in HDACIs and various aspects of HDAC-targeted cancer treatment.
Insights
Histone deacetylase inhibitors (HDACIs) offer a promising new avenue for cancer therapy by targeting histone deacetylases (HDACs). This review explores recent advancements in HDACIs and their role in cancer treatment.
Area of Science:
- Molecular Biology
- Cancer Research
- Epigenetics
Background:
- Histone acetyltransferases (HATs) and histone deacetylases (HDACs) are key epigenetic regulators of gene expression.
- HDACs are frequently implicated in cancer development and progression, making them attractive therapeutic targets.
- Histone deacetylase inhibitors (HDACIs) modulate gene expression by altering the balance between histone deacetylation and acetylation.
Purpose of the Study:
- To review recent developments in histone deacetylase inhibitors (HDACIs).
- To explore various aspects of histone deacetylase (HDAC)-targeted cancer treatment.
- To elucidate the mechanisms underlying the anticancer effects of HDACIs.
Main Methods:
- Literature review of recent studies on HDACIs and HDAC-targeted cancer therapy.
- Analysis of current clinical trials involving HDACIs.
- Examination of the molecular mechanisms of HDAC inhibition in cancer.
Main Results:
- Numerous HDACIs have been identified, with some progressing to clinical trials.
- HDACIs demonstrate potential in cancer treatment by modulating gene expression.
- The precise mechanisms of HDACIs' anticancer effects are still under investigation.
Conclusions:
- HDACIs represent a significant advancement in cancer therapy.
- Further research is needed to fully understand and optimize HDAC-targeted treatments.
- HDAC-targeted cancer therapy holds considerable promise for future clinical applications.
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