Related Experiment Video
Updated: Mar 26, 2026
Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
HDAC and HDAC Inhibitor: From Cancer to Cardiovascular Diseases
1Department of Pharmacology, Chonnam National University Medical School, Gwangju, Korea.
Insights
Histone deacetylases (HDACs) regulate gene expression and protein acetylation. HDAC inhibitors show promise as anti-cancer drugs and may benefit neurodegenerative, inflammatory, and cardiovascular diseases.
Area of Science:
- Epigenetics
- Molecular Biology
- Pharmacology
Background:
- Histone deacetylases (HDACs) are key epigenetic regulators controlling gene expression and protein acetylation.
- Aberrant HDAC activity is implicated in various pathophysiologic states, including cancer and cardiovascular diseases.
- HDAC inhibitors represent a novel therapeutic strategy with approved agents for hematologic cancers.
Purpose of the Study:
- To review the role of HDACs in cancer development and the efficacy of HDAC inhibitors in oncology.
- To explore the functional relevance of HDACs in cardiovascular diseases.
- To discuss the potential therapeutic applications of HDAC inhibitors in cardiovascular disease.
Main Methods:
- Literature review of HDACs' roles in cancer.
- Analysis of HDAC inhibitors' clinical outcomes in hematologic malignancies.
- Review of studies investigating HDACs in cardiovascular pathophysiology.
- Examination of preclinical and clinical data on HDAC inhibitors for cardiovascular diseases.
Main Results:
- HDAC inhibitors are approved for hematologic cancers with manageable side effects.
- Expanding clinical trials investigate HDAC inhibitors for other cancers and nonmalignant conditions.
- HDAC inhibition demonstrates beneficial effects in neurodegenerative, inflammatory, and cardiovascular diseases.
Conclusions:
- HDACs are crucial epigenetic regulators with significant roles in cancer.
- HDAC inhibitors offer a promising therapeutic avenue for various cancers and nonmalignant diseases, including cardiovascular conditions.
- Further research is warranted to fully elucidate the therapeutic potential of HDAC inhibitors in cardiovascular disease.
Abstract:
Histone deacetylases (HDACs) are epigenetic regulators that regulate the histone tail, chromatin conformation, protein-DNA interaction, and even transcription. HDACs are also post-transcriptional modifiers that regulate the protein acetylation implicated in several pathophysiologic states. HDAC inhibitors have been highlighted as a novel category of anti-cancer drugs. To date, four HDAC inhibitors, Vorinostat, Romidepsin, Panobinostat, and Belinostat, have been approved by the United States Food and Drug Administration. Principally, these HDAC inhibitors are used for hematologic cancers in clinic with less severe side effects. Clinical trials are continuously expanding to address other types of cancer and also nonmalignant diseases. HDAC inhibition also results in beneficial outcomes in various types of neurodegenerative diseases, inflammation disorders, and cardiovascular diseases. In this review, we will briefly discuss 1) the roles of HDACs in the acquisition of a cancer's phenotype and the general outcome of the HDAC inhibitors in cancer, 2) the functional relevance of HDACs in cardiovascular diseases and the possible therapeutic implications of HDAC inhibitors in cardiovascular disease.
Related Concept Videos
02:34Inhibition of Cdk Activity
02:34Inhibition of CDK Activity
01:26Heart Failure Drugs: Inhibitors of Renin-Angiotensin System
01:25Antihypertensive Drugs: Direct Renin Inhibitors
01:30Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...