Related Experiment Video
Updated: Dec 14, 2025
Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
The application of histone deacetylases inhibitors in glioblastoma
Rui Chen1, Mengxian Zhang2, Yangmei Zhou1
1Department of Oncology, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030, China.
Abstract:
The epigenetic abnormality is generally accepted as the key to cancer initiation. Epigenetics that ensure the somatic inheritance of differentiated state is defined as a crucial factor influencing malignant phenotype without altering genotype. Histone modification is one such alteration playing an essential role in tumor formation, progression, and resistance to treatment. Notably, changes in histone acetylation have been strongly linked to gene expression, cell cycle, and carcinogenesis. The balance of two types of enzyme, histone acetyltransferases (HATs) and histone deacetylases (HDACs), determines the stage of histone acetylation and then the architecture of chromatin. Changes in chromatin structure result in transcriptional dysregulation of genes that are involved in cell-cycle progression, differentiation, apoptosis, and so on. Recently, HDAC inhibitors (HDACis) are identified as novel agents to keep this balance, leading to numerous researches on it for more effective strategies against cancers, including glioblastoma (GBM). This review elaborated influences on gene expression and tumorigenesis by acetylation and the antitumor mechanism of HDACis. Besdes, we outlined the preclinical and clinical advancement of HDACis in GBM as monotherapies and combination therapies.
Insights
Epigenetic changes, specifically histone acetylation, are key in cancer. Histone deacetylase inhibitors (HDACis) show promise for treating cancers like glioblastoma by restoring gene expression balance.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Background:
- Epigenetic alterations, crucial for cancer initiation, influence malignant phenotypes without changing genotype.
- Histone modifications, particularly acetylation, play a vital role in tumor development, progression, and treatment resistance.
- The balance between histone acetyltransferases (HATs) and histone deacetylases (HDACs) regulates chromatin structure and gene expression.
Purpose of the Study:
- To review the influence of histone acetylation on gene expression and tumorigenesis.
- To explore the antitumor mechanisms of histone deacetylase inhibitors (HDACis).
- To outline the clinical and preclinical progress of HDACis in glioblastoma (GBM) treatment.
Main Methods:
- Literature review on epigenetics, histone acetylation, and HDAC inhibitors.
- Analysis of preclinical and clinical data for HDACis in cancer therapy.
- Focus on glioblastoma as a model for HDAC inhibitor research.
Main Results:
- Aberrant histone acetylation disrupts gene expression, affecting cell cycle, differentiation, and apoptosis.
- HDAC inhibitors re-establish normal histone acetylation patterns, impacting cancer cell behavior.
- HDACis demonstrate potential as monotherapies and in combination treatments for GBM.
Conclusions:
- Histone acetylation is a critical epigenetic mechanism in cancer.
- HDAC inhibitors represent a promising therapeutic strategy for epigenetic-driven cancers like GBM.
- Further research into HDAC inhibitors is essential for advancing cancer treatment.
