Histone deacetylases and cancer: causes and therapies
Abstract
Together, histone acetyltransferases and histone deacetylases (HDACs) determine the acetylation status of histones. This acetylation affects the regulation of gene expression, and inhibitors of HDACs have been found to cause growth arrest, differentiation and/or apoptosis of many tumours cells by altering the transcription of a small number of genes. HDAC inhibitors are proving to be an exciting therapeutic approach to cancer, but how do they exert this effect?
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SAHA is a broad-spectrum HDAC inhibitor.
“SAHA exemplifies broad-spectrum inhibition (Marks et al., 2001; Duvic et al., 2007)”
From Histone modifications and depression: epigenetic mechanisms, therapeutic targets, and translational outlook (2026) · cites this paper as Marks et al., 2001
Some genes annotated with regulation of cyclin-dependent kinase activity have been previously shown to be induced following HDACi treatment.
“Some of the genes annotated with this term have been previously shown to be induced following HDACi treatment (3, 4, 31, 36, 44-46).”
From Histone Deacetylase (HDAC) Inhibitor Kinetic Rate Constants Correlate with Cellular Histone Acetylation but Not Transcription and Cell Viability (2013) · cites this paper as [44]
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“SAHA exemplifies broad-spectrum inhibition (Marks et al., 2001; Duvic et al., 2007), whereas entinostat shows greater class I selectivity (Kiany et al., 2020).”
- Authors
- Marks, P. A., Rifkind, R. A., Richon, V. M., Breslow, R., Miller, T., & Kelly, W. K.
- Affiliations
- Memorial Sloan Kettering Cancer Center (US)
- Columbia University (US)
- Corresponding author
- Marks, Paul A.
- ORCID
- Kelly, William K.
- Venue
- Nature reviews. Cancer
- Published
- 2001-12
- Volume
- 1
- Issue
- 3
- Pages
- 194-202
- ISSN
- 1474-175X (ISSN-L)
- 1474-1768
- OpenAlex
- W2022285476
- Cited by
- 1,866
- References
- 86
- Citations by year
- 2026: 20 · 2025: 27 · 2024: 27 · 2023: 29 · 2022: 38 · 2021: 45 · 2020: 47 · 2019: 57 · 2018: 60 · 2017: 75 · 2016: 65 · 2015: 67 · 2014: 76 · 2013: 100 · 2012: 107
- FWCI
- 5.00
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Nature reviews. Cancer (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, histone deacetylase inhibitors, histone acetylation, histone acetyltransferase, gene expression regulation, tumor cell differentiation, apoptosis, cancer therapy
- MeSH terms
- Acetylation, Animals, Antineoplastic Agents, Cell Cycle, Chromatin, Clinical Trials as Topic, Drug Screening Assays, Antitumor, Enzyme Inhibitors, Female, Forecasting, Histone Deacetylases, Histones, Humans, Male, Models, Molecular, Neoplasm Proteins, Neoplasms, Neoplasms, Experimental, Nucleosomes, Protein Processing, Post-Translational, Saccharomyces cerevisiae, Species Specificity, Transcription Factors, Transcriptional Activation, Gene Expression Regulation, Neoplastic, Apoptosis, Gene Silencing, Saccharomyces cerevisiae Proteins, Histone Deacetylase Inhibitors
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