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Updated: Jun 16, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Novel histone deacetylase inhibitors in clinical trials as anti-cancer agents
Jiahuai Tan1, Shundong Cang, Yuehua Ma
1Department of Medicine, The Mount Vernon Hospital, Mount Vernon, NY 10550, USA.
Abstract:
Histone deacetylases (HDACs) can regulate expression of tumor suppressor genes and activities of transcriptional factors involved in both cancer initiation and progression through alteration of either DNA or the structural components of chromatin. Recently, the role of gene repression through modulation such as acetylation in cancer patients has been clinically validated with several inhibitors of HDACs. One of the HDAC inhibitors, vorinostat, has been approved by FDA for treating cutaneous T-cell lymphoma (CTCL) for patients with progressive, persistent, or recurrent disease on or following two systemic therapies. Other inhibitors, for example, FK228, PXD101, PCI-24781, ITF2357, MGCD0103, MS-275, valproic acid and LBH589 have also demonstrated therapeutic potential as monotherapy or combination with other anti-tumor drugs in CTCL and other malignancies. At least 80 clinical trials are underway, testing more than eleven different HDAC inhibitory agents including both hematological and solid malignancies. This review focuses on recent development in clinical trials testing HDAC inhibitors as anti-tumor agents.
Insights
Histone deacetylase (HDAC) inhibitors show promise in cancer treatment by regulating gene expression. Clinical trials are exploring their efficacy in various hematological and solid malignancies.
Area of Science:
- Molecular Biology
- Oncology
- Pharmacology
Background:
- Histone deacetylases (HDACs) regulate gene expression and chromatin structure, impacting cancer initiation and progression.
- Gene repression via acetylation modulation is a validated therapeutic strategy in cancer.
- Vorinostat, an HDAC inhibitor, is FDA-approved for cutaneous T-cell lymphoma (CTCL).
Purpose of the Study:
- To review recent developments in clinical trials of HDAC inhibitors as anti-tumor agents.
- To highlight the therapeutic potential of various HDAC inhibitors in different malignancies.
Main Methods:
- Review of current clinical trials involving HDAC inhibitors.
- Analysis of therapeutic potential of HDAC inhibitors as monotherapy or in combination treatments.
Main Results:
- Multiple HDAC inhibitors (e.g., FK228, PXD101, MS-275) demonstrate therapeutic potential.
- Over 80 clinical trials are investigating HDAC inhibitors for hematological and solid tumors.
Conclusions:
- HDAC inhibitors represent a promising class of anti-cancer agents.
- Ongoing clinical trials are crucial for evaluating the efficacy of HDAC inhibitors in diverse cancer types.
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