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Updated: Mar 23, 2026
Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
HDAC expression and clinical prognosis in human malignancies
1Institut für Pathologie, Charité Universitätsmedizin, Berlin, Germany. weichert@charite.de
Abstract:
Histone deacetylases are known to play a central role in the regulation of several cellular properties intimately interlinked with the development and progression of cancer. Consequently, a multitude of histone deacetylase (HDAC) inhibitors have been developed and are currently tested as anticancer agents in a variety of solid and hematologic malignancies. However, only recently research began to focus on the actual expression patterns of specific HDAC isoforms in neoplasias. The majority of studies investigating this issue reported an enhanced expression of class I HDAC isoforms in solid human tumours, both on mRNA and protein level, when compared to the respective tissue of origin. In most studies, class I HDAC expression was high in locally advanced, dedifferentiated, strongly proliferating tumours. In some but not all entities elevated class I HDAC expression was associated with compromised patient prognosis, however, an association of elevated class I HDAC expression with improved prognosis has also be reported for selected tumour entities. In contrast to class I isoforms, expression of class II HDACs has been found reduced in tumours and high expression of these isoforms in some entities predicted better patient outcome. Since all of these data point to a potential biological role of differences in HDAC expression in human tumours, future translational studies will focus on the question, whether HDAC expression patterns are predictive for response to treatment with histone deacetylase inhibitors.
Insights
Histone deacetylase (HDAC) expression varies in cancers, with Class I HDACs often upregulated and Class II HDACs downregulated. This differential expression may impact patient prognosis and predict response to HDAC inhibitors in cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Epigenetics
Background:
- Histone deacetylases (HDACs) regulate cellular functions critical to cancer development and progression.
- HDAC inhibitors are actively investigated as anticancer agents for various malignancies.
- Research is increasingly focusing on the expression patterns of specific HDAC isoforms in tumors.
Purpose of the Study:
- To review and synthesize current findings on the expression patterns of HDAC isoforms in human tumors.
- To explore the correlation between HDAC isoform expression and clinicopathological features, including patient prognosis.
- To evaluate the potential of HDAC expression patterns as predictive biomarkers for response to HDAC inhibitor therapy.
Main Methods:
- Systematic review of studies investigating HDAC isoform expression (mRNA and protein levels) in various human neoplasms.
- Comparative analysis of HDAC expression in tumor tissues versus normal tissues of origin.
- Correlation analysis of HDAC expression with tumor grade, proliferation, stage, and patient survival data.
Main Results:
- Enhanced expression of Class I HDAC isoforms (mRNA and protein) is frequently observed in solid human tumors compared to normal tissues.
- Elevated Class I HDAC expression is often associated with advanced, dedifferentiated, and highly proliferative tumors.
- While sometimes linked to poorer prognosis, elevated Class I HDAC expression has also predicted better outcomes in specific cancer types.
- Conversely, Class II HDAC expression is often reduced in tumors, with high expression correlating with better patient outcomes in certain entities.
Conclusions:
- Differential expression of HDAC isoforms (Class I vs. Class II) is a common feature in human cancers.
- HDAC expression patterns show potential as prognostic indicators and may predict patient response to HDAC inhibitor therapies.
- Further translational studies are warranted to validate HDAC expression as a predictive biomarker for HDAC inhibitor treatment efficacy.
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