Histone deacetylase inhibition in the treatment of heart disease
Related Experiment Video
Updated: Jul 8, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Jeff M Berry1, Dian J Cao, Beverly A Rothermel
1University of Texas Southwestern Medical Center, Donald W Reynolds Cardiovascular Clinical Research Center, Dallas, Texas, USA.
Abstract:
Recent work has demonstrated the importance of chromatin remodeling, especially histone acetylation, in the control of gene expression in the heart. Studies in preclinical models suggest that inhibition of histone deacetylase (HDAC) activity - using compounds that show promise in ongoing oncology trials - blunts pathologic growth of cardiac myocytes. Indeed, small-molecule inhibitors of HDACs are members of an evolving class of pharmacologic agents in development for the treatment of several diseases. If proved effective in the treatment of heart disease, HDAC inhibitors could have a significant impact on public health, as cardiovascular disease remains the leading cause of death in the US. This paper reviews understanding of the mechanisms of action of HDAC inhibitors in the heart and summarizes emerging data regarding their effects on disease-related cardiac remodeling and function.
Insights
Histone deacetylase (HDAC) inhibitors show promise in treating heart disease by blocking pathologic cardiac myocyte growth. This review explores their mechanisms and effects on cardiac remodeling and function.
Area of Science:
- Cardiovascular Biology
- Molecular Cardiology
- Epigenetics
Background:
- Chromatin remodeling, particularly histone acetylation, regulates gene expression in the heart.
- Histone deacetylase (HDAC) inhibitors are emerging pharmacologic agents with potential in various diseases.
- Preclinical studies indicate HDAC inhibition may prevent adverse cardiac remodeling.
Purpose of the Study:
- To review the mechanisms of action of HDAC inhibitors in cardiac tissue.
- To summarize current data on the effects of HDAC inhibitors on cardiac remodeling and function in disease contexts.
Main Methods:
- Review of preclinical studies and ongoing clinical trials.
- Analysis of molecular mechanisms underlying HDAC inhibition in cardiomyocytes.
- Synthesis of data on functional outcomes in models of cardiac disease.
Main Results:
- HDAC inhibition can blunt pathological cardiac myocyte growth.
- Emerging data suggest potential therapeutic benefits in cardiovascular disease.
- Compounds targeting HDACs are under investigation for multiple conditions.
Conclusions:
- HDAC inhibitors represent a promising therapeutic strategy for heart disease.
- Understanding their mechanisms is crucial for clinical application.
- Further research is warranted to establish efficacy and safety in cardiovascular patients.
Related Concept Videos
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System
Atherosclerosis III: Management
Heart Failure Drugs: Inotropic Agents
Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
Heart Failure Drugs: β-Blockers
Heart Failure V: Medical Management

