Anticancer activities of histone deacetylase inhibitors
Abstract
Histone deacetylases (HDACs) are enzymes involved in the remodelling of chromatin, and have a key role in the epigenetic regulation of gene expression. In addition, the activity of non-histone proteins can be regulated through HDAC-mediated hypo-acetylation. In recent years, inhibition of HDACs has emerged as a potential strategy to reverse aberrant epigenetic changes associated with cancer, and several classes of HDAC inhibitors have been found to have potent and specific anticancer activities in preclinical studies. However, such studies have also indicated that the effects of HDAC inhibitors could be considerably broader and more complicated than originally understood. Here we summarize recent advances in the understanding of the molecular events that underlie the anticancer effects of HDAC inhibitors, and discuss how such information could be used in optimizing the development and application of these agents in the clinic, either as monotherapies or in combination with other anticancer drugs.
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Among activated genes that subside with pulsed HDACi administration are genes known to be powerful effectors of cell cycle arrest in multiple cell types and may promote apoptosis.
“Among activated genes that subside with pulsed HDACi administration are genes known to be powerful effectors of cell cycle arrest in multiple cell types and may promote apoptosis (11, 50).”
From Histone Deacetylase (HDAC) Inhibitor Kinetic Rate Constants Correlate with Cellular Histone Acetylation but Not Transcription and Cell Viability (2013) · cites this paper as [50]
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- Authors
- Bolden, J. E., Peart, M. J., & Johnstone, R. W.
- Affiliations
- Peter MacCallum Cancer Centre (AU)
- Columbia University (US)
- The University of Melbourne (AU)
- Corresponding author
- Johnstone, Ricky W.
- ORCID
- Johnstone, Ricky W.
- Venue
- Nature Reviews Drug Discovery
- Published
- 2006-09
- Volume
- 5
- Issue
- 9
- Pages
- 769-784
- ISSN
- 1474-1776 (ISSN-L)
- 1474-1784
- OpenAlex
- W1967018540
- Cited by
- 2,919
- References
- 13
- Citations by year
- 2026: 40 · 2025: 86 · 2024: 56 · 2023: 96 · 2022: 99 · 2021: 106 · 2020: 121 · 2019: 110 · 2018: 145 · 2017: 153 · 2016: 178 · 2015: 209 · 2014: 176 · 2013: 229 · 2012: 204
- FWCI
- 12.68
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Nature Reviews Drug Discovery (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Histone Deacetylase Inhibitors Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Epigenetics and DNA Methylation
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Genomics and Chromatin Dynamics
- Keywords
- histone deacetylase inhibitors, anticancer activity, chromatin remodeling, epigenetic regulation, gene expression, combination therapy, clinical development
- MeSH terms
- Antineoplastic Agents, Cell Cycle, Enzyme Inhibitors, Histone Deacetylases, Humans, Neoplasms, Apoptosis, Histone Deacetylase Inhibitors
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