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Updated: Sep 13, 2025
Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Targeting histone deacetylase 1: Inhibition and activation as promising therapeutic strategies for diverse disorders
Giuliana Costanzo1, Rocco Buccheri1, Giuseppe Cosentino1
1Department of Drug and Health Sciences, University of Catania, Catania, Italy.
Abstract:
Epigenetic regulation plays a crucial role in several pathological conditions. Dysregulation of histone deacetylase (HDAC) enzymes has been implicated in the onset and progression of numerous diseases, including cancer, inflammatory disorders, and neurodegenerative conditions. Most known HDAC inhibitors (HDACi) are classified as "pan-inhibitors", targeting multiple HDAC isoforms indiscriminately. However, the growing demand for isoform-selective ligands has emphasized the need for more targeted therapeutic strategies. Among HDAC isoforms, HDAC1 has emerged as a particularly promising target for pharmacological intervention. This review provides a comprehensive overview of current HDAC1-selective ligands, including inhibitors and activators, highlighting their potential as useful therapeutic tools. The most promising class I of HDACi currently in clinical trials is discussed.
Insights
Histone deacetylase 1 (HDAC1) selective ligands offer targeted therapies for diseases like cancer. This review covers HDAC1 inhibitors and activators, focusing on promising Class I HDAC inhibitors in clinical trials.
Area of Science:
- Biochemistry
- Pharmacology
- Epigenetics
Background:
- Epigenetic regulation is vital in disease pathology.
- Histone deacetylase (HDAC) dysregulation is linked to cancer, inflammation, and neurodegeneration.
- Current HDAC inhibitors (HDACi) are often pan-inhibitors, lacking specificity.
Purpose of the Study:
- To provide a comprehensive overview of HDAC1-selective ligands.
- To highlight potential therapeutic applications of HDAC1 modulators.
- To discuss promising Class I HDAC inhibitors in clinical trials.
Main Methods:
- Literature review of HDAC1-selective inhibitors and activators.
- Analysis of current therapeutic strategies targeting HDAC1.
- Examination of Class I HDAC inhibitors in clinical development.
Main Results:
- HDAC1 is a promising target for selective pharmacological intervention.
- Various HDAC1-selective ligands, including inhibitors and activators, have been developed.
- Specific Class I HDAC inhibitors show significant therapeutic potential in clinical trials.
Conclusions:
- HDAC1-selective ligands represent a significant advancement in targeted therapy.
- Further research into HDAC1 modulators could lead to novel treatments for various diseases.
- Clinical progression of Class I HDAC inhibitors warrants continued investigation.
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