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Updated: Feb 3, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Histone deacetylase inhibitors as a new anticancer option: How far can we go with expectations? delivery systems
Anna Garmpi1, Nikolaos Garmpis, Christos Damaskos
1Internal Medicine Department, "Laiko" General Hospital, Medical School, National and Kapodistrian University of Athens, Athens, Greece.
Abstract:
Histone modification that occurs through the process of acetylation plays a key role in the epigenetic regulation of gene expression. The balance between histone deacetylases (HDACs) and histone acetyltransferases controls this process. Histone deacetylase inhibitors (HDACIs) can induce cancer cell cycle arrest, differentiation and cell death, reduce angiogenesis and modulate immune response. Therefore, HDAIs represent a group of enzymes that can be used for the development of pharmaceutical agents against a variety of malignant diseases. The mechanisms of their anticancer effect depend on many factors. HDACIs vorinostat, romidepsin and belinostat have been approved for some T-cell lymphomas and panobinostat for multiple myeloma. Other HDACIs are tested in clinical trials for the treatment of hematological and solid malignancies. The results of such studies are promising but further larger studies are needed.
Insights
Histone deacetylase inhibitors (HDACIs) show promise in cancer treatment by inducing cell death and modulating immune responses. Approved HDACIs treat certain lymphomas and myeloma, with others in clinical trials for various malignancies.
Area of Science:
- Epigenetics
- Molecular Biology
- Cancer Research
Background:
- Histone acetylation is crucial for epigenetic gene regulation.
- Histone deacetylases (HDACs) and histone acetyltransferases maintain this balance.
- Histone deacetylase inhibitors (HDACIs) disrupt this balance, impacting cancer cell behavior.
Purpose of the Study:
- To explore the anticancer mechanisms of HDACIs.
- To review the therapeutic potential of HDACIs in various malignancies.
- To summarize the current clinical applications and ongoing trials of HDACIs.
Main Methods:
- Review of scientific literature on HDACIs and their anticancer effects.
- Analysis of approved HDACIs and their indications.
- Summary of ongoing clinical trials involving HDACIs for hematological and solid tumors.
Main Results:
- HDACIs induce cancer cell cycle arrest, differentiation, and apoptosis.
- HDACIs can inhibit angiogenesis and modulate the immune system.
- Vorinostat, romidepsin, belinostat, and panobinostat are approved for specific hematological cancers.
- Numerous HDACIs are under investigation in clinical trials for diverse cancers.
Conclusions:
- HDACIs represent a promising class of drugs for cancer therapy.
- While current results are encouraging, larger clinical studies are necessary to fully establish their efficacy and safety across various malignancies.
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