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Updated: Jun 3, 2025

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Histone Deacetylase (HDAC) Inhibitors as a Novel Therapeutic Option Against Fibrotic and Inflammatory Diseases
Maria A Theodoropoulou1,2, Christiana Mantzourani1,2, George Kokotos1,2
1Department of Chemistry, National and Kapodistrian University of Athens, 15771 Athens, Greece.
Abstract:
Histone deacetylases (HDACs) are enzymes that play an essential role in the onset and progression of cancer. As a consequence, a variety of HDAC inhibitors (HDACis) have been developed as potent anticancer agents, several of which have been approved by the FDA for cancer treatment. However, recent accumulated research results have suggested that HDACs are also involved in several other pathophysiological conditions, such as fibrotic, inflammatory, neurodegenerative, and autoimmune diseases. Very recently, the HDAC inhibitor givinostat has been approved by the FDA for an indication beyond cancer: the treatment of Duchenne muscular dystrophy. In recent years, more and more HDACis have been developed as tools to understand the role that HDACs play in various disorders and as a novel therapeutic approach to fight various diseases other than cancer. In the present perspective article, we discuss the development and study of HDACis as anti-fibrotic and anti-inflammatory agents, covering the period from 2020-2024. We envision that the discovery of selective inhibitors targeting specific HDAC isozymes will allow the elucidation of the role of HDACs in various pathological processes and will lead to the development of promising treatments for such diseases.
Insights
Histone deacetylase inhibitors (HDACis) show promise beyond cancer treatment. Research from 2020-2024 highlights their potential as anti-fibrotic and anti-inflammatory agents for various diseases.
Area of Science:
- Biochemistry
- Pharmacology
- Molecular Biology
Background:
- Histone deacetylases (HDACs) are crucial in cancer development.
- HDAC inhibitors (HDACis) are FDA-approved cancer treatments.
- Emerging research links HDACs to fibrotic, inflammatory, neurodegenerative, and autoimmune diseases.
Purpose of the Study:
- To review the development and application of HDAC inhibitors as anti-fibrotic and anti-inflammatory agents.
- To cover research published between 2020 and 2024.
- To explore the therapeutic potential of HDAC inhibitors beyond oncology.
Main Methods:
- Literature review of scientific articles published from 2020-2024.
- Analysis of research on HDAC inhibitors' roles in fibrotic and inflammatory conditions.
- Synthesis of findings on HDAC isozyme-specific inhibition.
Main Results:
- HDAC inhibitors are being investigated for non-cancerous diseases, including Duchenne muscular dystrophy.
- Givinostat, an HDAC inhibitor, received FDA approval for Duchenne muscular dystrophy.
- HDACis demonstrate potential as anti-fibrotic and anti-inflammatory therapeutics.
Conclusions:
- HDAC inhibitors offer a promising therapeutic avenue for fibrotic, inflammatory, and other diseases.
- Targeting specific HDAC isozymes may elucidate disease mechanisms and lead to novel treatments.
- Continued research into HDAC inhibitors is vital for expanding their clinical applications beyond cancer.
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