HDAC inhibitors in cancer biology: emerging mechanisms and clinical applications

Khan, Omar; La Thangue, Nicholas B

doi:10.1038/icb.2011.100

Cited by 477Histone Deacetylase Inhibitors ResearchEpigenetics and DNA MethylationGenomics and Chromatin Dynamics

HDAC inhibitors in cancer biology: emerging mechanisms and clinical applications

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Khan, Omar, La Thangue, Nicholas B·2012·Immunology & Cell Biology

DOI 10.1038/icb.2011.100

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Abstract

Reversible acetylation mediated by histone deacetylases (HDACs) influences a broad repertoire of physiological processes, many of which are aberrantly controlled in tumor cells. As HDAC inhibition prompts tumor cells to enter apoptosis, small‐molecule HDAC inhibitors have been developed as a new class of mechanism‐based anti‐cancer agent, many of which have entered clinical trials. Although the clinical picture is evolving and the precise utility of HDAC inhibitors remains to be determined, it is noteworthy that certain tumor types undergo a favorable response, in particular hematological malignancies. Vorinostat and romidepsin have been approved for treating cutaneous T‐cell lymphoma in patients with progressive, persistent or recurrent disease. Here, we discuss developments in our understanding of molecular events that underlie the anti‐cancer effects of HDAC inhibitors and relate this information to the emerging clinical picture for the application of these inhibitors in the treatment of cancer.

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TSA and SAHA do not directly inhibit cGAS-STING signaling or p38/mTOR phosphorylation, but instead restore OXPHOS gene expression and reduce mitochondrial ROS, thereby suppressing CCF and SASP.
“TSA and SAHA, for example, do not directly inhibit cGAS–STING signaling or p38/mTOR phosphorylation, but instead restore OXPHOS gene expression and reduce mitochondrial ROS, thereby suppressing CCF and SASP (Vizioli et al., 2020; Khan and La Thangue, 2012; Venkataramani et al., 2010).”
From Histone modifications and depression: epigenetic mechanisms, therapeutic targets, and translational outlook (2026) · cites this paper as Khan and La Thangue, 2012
The Effects on DNA repair and damage section (page unavailable) says reactive oxygen species accumulate after HDAC inhibitor treatment, contrary to the claimed reduction in ROS. The Gene signatures section identifies trichostatin A and vorinostat (SAHA) as treatments studied, but does not connect them to restored OXPHOS expression or suppression of CCF and SASP. The ROS passage does not specifically measure mitochondrial ROS in the setting of the claim. (LLM, conf=0.76)
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Blocking HDAC enzymatic activity with small molecule HDAC inhibitors reduces malignancies in vitro and in vivo by blocking the cell cycle and inducing apoptosis.
“Importantly, blocking HDAC enzymatic activity with small molecule HDAC inhibitors has been shown to reduce malignancies in vitro and in vivo by blocking the cell cycle and inducing apoptosis (14).”
From Histone Deacetylase (HDAC) Inhibitor Kinetic Rate Constants Correlate with Cellular Histone Acetylation but Not Transcription and Cell Viability (2013) · cites this paper as [14]
The Abstract and ‘Effects on the cell cycle’ section say that small-molecule HDAC inhibitors suppress tumor-cell proliferation, cause cell-cycle arrest, and induce apoptosis. The review also reports clinical responses in some malignancies, but its Conclusions say the mechanism of anti-tumor activity remains unclear. It therefore does not establish that reduced malignancy in vivo occurs specifically by both mechanisms. (LLM, conf=0.84)
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[86]86. Stimson L, La Thangue NB. Biomarkers for predicting clinical responses to HDAC inhibitors. Cancer Lett 2009; 280: 177-183.

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“Importantly, blocking HDAC enzymatic activity with small molecule HDAC inhibitors has been shown to reduce malignancies in vitro and in vivo by blocking the cell cycle and inducing apoptosis (14).”
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Authors: Khan, O., & La Thangue, N. B.
Affiliations: University of Oxford (GB)
Laboratory of Cancer Biology, Department of Oncology Oxford UK
ORCID: Khan, Omar
Venue: Immunology & Cell Biology
Publisher: Wiley
Published: 2011-11-29
Volume: 90
Issue: 1
Pages: 85-94
ISSN: 0004-945X (ISSN-L)
0818-9641
1440-1711
DOI: 10.1038/icb.2011.100
OpenAlex: W2015047229
Semantic Scholar: 13ddbb976f948a015aef3264963e82450d8e7054
Cited by: 450
References: 132
Citations by year: 2026: 9 · 2025: 14 · 2024: 8 · 2023: 18 · 2022: 19 · 2021: 19 · 2020: 18 · 2019: 28 · 2018: 32 · 2017: 30 · 2016: 53 · 2015: 55 · 2014: 56 · 2013: 58 · 2012: 32
FWCI: 4.41
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: onlinelibrary.wiley.com/termsAndConditions#vor (vor)
Locations: Immunology and Cell Biology (publishedVersion)
PubMed (publishedVersion)
Funders: Cancer Research UK
Medical Research Council
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, histone acetylation, apoptosis, anticancer mechanism, hematologic malignancies, cutaneous T-cell lymphoma, vorinostat, romidepsin, small molecule inhibitors, clinical trials
MeSH terms: Vorinostat, Acetylation, Antineoplastic Agents, Histone Deacetylases, Humans, Hydroxamic Acids, Neoplasms, Lymphoma, T-Cell, Depsipeptides, Histone Deacetylase Inhibitors

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