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Updated: Jun 29, 2026
Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Histone deacetylase inhibitors in cancer therapy
Min-Jung Lee1, Yeong Sang Kim, Shivaani Kummar
1Medical Oncology Branch, Center for Cancer Research, NCI, NIH, Bethesda, Maryland 20892, USA.
Purpose Of Review:
The purpose of this review is to provide an overview of recent advances in the development of histone deacetylase inhibitors (HDACi) for the treatment of cancer.
Recent Findings:
Recently, there has been a dramatic expansion of HDACi clinical investigation. There are now 11 HDACi in clinical trial, including inhibitors with a broad spectrum of HDAC isoform inhibitory activity as well as drugs with isoform selectivity. Over 70 combination therapy trials are in progress. Major areas of progress covered include the entry of new HDAC inhibitors into clinical development, recent progress in understanding of molecular mechanisms of HDACi anticancer activity, and a preclinical and clinical update on HDACi in combination.
Summary:
In the period under review there have been advances in understanding of HDACi mechanisms of action, identification of rational combinations that address increased efficacy and overcoming resistance, and greatly expanded clinical development of pan-HDAC-inhibitory and isoform-selective inhibitors in monotherapy and combination therapy protocols.
Insights
Recent advances in histone deacetylase inhibitors (HDACi) for cancer treatment are highlighted. Expanded clinical trials and combination therapies show promise for HDAC inhibitors in oncology.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Histone deacetylase inhibitors (HDACi) represent a promising class of anticancer agents.
- Understanding the molecular mechanisms of HDACi is crucial for optimizing cancer therapy.
Purpose of the Study:
- To review recent advancements in the development and clinical application of HDAC inhibitors for cancer treatment.
- To provide an overview of novel HDAC inhibitors and their combination therapies.
Main Methods:
- Literature review of recent preclinical and clinical studies on HDAC inhibitors.
- Analysis of ongoing clinical trials and combination therapy research.
Main Results:
- Eleven HDAC inhibitors are currently in clinical trials, with varying isoform selectivity.
- Over 70 combination therapy trials are underway, exploring synergistic effects.
- Progress has been made in understanding HDACi's anticancer mechanisms and identifying rational combinations.
Conclusions:
- Significant progress has been achieved in HDAC inhibitor development and clinical investigation.
- Enhanced understanding of HDACi mechanisms aids in developing effective combination strategies.
- Expanded clinical development of both broad-spectrum and isoform-selective HDAC inhibitors is evident.
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