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Updated: Sep 27, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Histone deacetylase in carcinogenesis and its inhibitors as anti-cancer agents
Dong Hoon Kim1, Minjung Kim, Ho Jeong Kwon
1Department of Bioscience and Biotechnology, Institute of Bioscience, Sejong University, Seoul 143-747, Korea.
Abstract:
The acetylation state of histone is reversibly regulated by histone acetyltransferase (HAT) and deacetylase (HDAC). An imbalance of this reaction leads to an aberrant behavior of the cells in morphology, cell cycle, differentiation, and carcinogenesis. Recently, these key enzymes in the gene expression were cloned. They revealed a broad use of this modification, not only in histone, but also other proteins that involved transcription, nuclear transport, and cytoskeleton. These results suggest that HAT/HDAC takes charge of multiple-functions in the cell, not just the gene expression. HDAC is especially known to play an important role in carcinogenesis. The enzyme has been considered a target molecule for cancer therapy. The inhibition of HDAC activity by a specific inhibitor induces growth arrest, differentiation, and apoptosis of transformed or several cancer cells. Some of these inhibitors are in a clinical trial at phase I or phase II. The discovery and development of specific HDAC inhibitors are helpful for cancer therapy, and decipher the molecular mode of action for HDAC.
Insights
Histone acetyltransferase (HAT) and deacetylase (HDAC) regulate cell functions. HDAC inhibition shows promise for cancer therapy by inducing apoptosis and growth arrest in cancer cells.
Area of Science:
- Biochemistry
- Molecular Biology
- Epigenetics
Background:
- Histone acetylation, regulated by HAT and HDAC, is crucial for cellular processes.
- Dysregulation of HAT/HDAC activity is linked to abnormal cell behavior, including carcinogenesis.
- HAT and HDAC enzymes modify proteins beyond histones, impacting transcription, nuclear transport, and cytoskeleton.
Purpose of the Study:
- To highlight the multifaceted roles of HAT/HDAC enzymes in cellular functions.
- To emphasize the significance of HDAC in carcinogenesis.
- To discuss the therapeutic potential of HDAC inhibitors in cancer treatment.
Main Methods:
- Review of existing literature on HAT and HDAC enzymes.
- Analysis of the role of histone acetylation in gene expression and other cellular processes.
- Examination of preclinical and clinical data on HDAC inhibitors for cancer therapy.
Main Results:
- HAT and HDAC enzymes regulate gene expression and other cellular functions.
- HDAC plays a critical role in the development of cancer.
- HDAC inhibitors induce growth arrest, differentiation, and apoptosis in cancer cells.
- Several HDAC inhibitors are currently undergoing clinical trials.
Conclusions:
- HDAC enzymes are vital targets for cancer therapy.
- Development of specific HDAC inhibitors offers a promising avenue for cancer treatment.
- Further research into HDAC function and inhibition is essential for advancing cancer therapy.
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