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Updated: Apr 14, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Emerging approaches for histone deacetylase inhibitor drug discovery
Clemens Zwergel1, Sergio Valente, Claus Jacob
1Sapienza University of Rome, Department of Drug Chemistry and Technologies , Piazzale Aldo Moro 5, 00185 Rome , Italy +00390649913392 ; sergio.valente@uniroma1.it ; antonello.mai@uniroma1.it.
Introduction:
Histone deacetylases (HDACs) are key players in the mediation of gene expression for both cancerous and noncancerous malignancies. Overexpression of these enzymes has been demonstrated in numerous types of cancer with some enzyme isoforms also involved in neurological, inflammatory and viral pathologies. Hence, the development of HDAC inhibitors (HDACis) represents a promising approach for their treatment. Numerous chemical entities have been studied in the recent years and some of them have reached clinical trials.
Areas Covered:
This review summarizes the recent efforts in the drug development of HDACis and their potential application as therapeutic agents in cancerous, neurological, inflammatory and viral diseases.
Expert Opinion:
The development of novel potent and selective HDACis is ongoing. However, increased scientific effort is needed to aid the fight of specific types of cancerous or noncancerous disease with more selective agents required to avoid side effects during therapy. An interesting therapeutic approach is the use of HDACis in combination with other epigenetic target modulators to combine their therapeutic potential for a synergistic effect.
Insights
Histone deacetylase inhibitors (HDACis) show promise for treating cancers and other diseases by regulating gene expression. Further research is needed for selective agents and combination therapies to improve treatment outcomes.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Histone deacetylases (HDACs) are crucial regulators of gene expression implicated in various cancers and non-cancerous diseases.
- Overexpressed HDACs are linked to malignancies, neurological disorders, inflammation, and viral infections.
- HDAC inhibitors (HDACis) are a developing therapeutic strategy, with several compounds in clinical trials.
Purpose of the Study:
- To review recent advancements in HDAC inhibitor drug development.
- To explore the therapeutic potential of HDAC inhibitors in treating cancerous, neurological, inflammatory, and viral diseases.
Main Methods:
- Literature review of recent studies on HDAC inhibitor drug development.
- Analysis of potential therapeutic applications across various disease types.
Main Results:
- Ongoing development of novel, potent, and selective HDAC inhibitors.
- HDAC inhibitors show therapeutic promise for a range of conditions.
Conclusions:
- Continued research is essential for developing more selective HDAC inhibitors to minimize side effects.
- Combination therapies involving HDAC inhibitors and other epigenetic modulators may offer synergistic therapeutic benefits.
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