Inhibition of histone deacetylases in melanoma—a perspective from bench to bedside

Hornig, Eva; Heppt, Markus V.; Graf, Saskia A.; Ruzicka, Thomas; Berking, Carola

doi:10.1111/exd.13089

Cited by 53Histone Deacetylase Inhibitors ResearchMelanoma and MAPK PathwaysEpigenetics and DNA Methylation

Inhibition of histone deacetylases in melanoma—a perspective from bench to bedside

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Hornig, Eva, Heppt, Markus V., Graf, Saskia A., Ruzicka, Thomas, Berking, Carola·2016·Experimental Dermatology

DOI 10.1111/exd.13089

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Abstract

Histone deacetylases (HDACs) are critically involved in epigenetic gene regulation through alterations of the chromatin status of DNA. Aberrant expression, dysregulation of their enzymatic activity or imbalances between HDACs and histone acetyltransferases are likely involved in the development and progression of cancer. Pharmacologic inhibition of HDACs shows potent antitumor activity in a panel of malignancies such as colon or gastric cancer and multiple myeloma. In this review, we summarize the current knowledge of HDACs in melanoma and evaluate the application of HDAC inhibition from an experimental and clinical perspective. The molecular functions of HDACs can be classified into histone and non‐histone effects with diverse implications in proliferation, cell cycle progression and apoptosis. HDAC inhibition results in G1 cell cycle arrest, induces apoptosis and increases the immunogenicity of melanoma cells. Some studies proposed that HDAC inhibition may overcome the resistance of melanoma cells to BRAF inhibition. Several inhibitors such as vorinostat, entinostat and valproic acid have recently been tested in phase I and early phase II trials, yet most agents show limited efficacy and tolerability as single agents. The most frequent adverse events of HDAC inhibition comprise haematological toxicity, fatigue, nausea and laboratory abnormalities. Existing evidence supports the hypothesis that HDAC inhibitors (HDACi) may sensitize melanoma cells to immunotherapy and targeted therapy and hence bear therapeutic potential concurrent with immune checkpoint blockade or BRAF and MEK inhibition.

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HDAC inhibitors have been considered for usage in combinatorial therapies for several cancers including melanoma.
“HDAC inhibitors have been considered for usage in combinatorial therapies for several cancers including melanoma47,65–67.”
From Epigenetic control of melanoma cell invasiveness by the stem cell factor SALL4 (2021) · cites this paper as [66]

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BindingDB Entry 50001427: Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models.
BindingDB (2020) · UC San Diego · doi:10.7270/q2280b3g
BindingDB Entry 50012424: Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
BindingDB (2022) · UC San Diego · doi:10.7270/q24m987x
BindingDB Entry 50021333: Design, synthesis, and biological evaluation of phenylcyclopropylamine-entinostat conjugates that selectively target cancer cells.
BindingDB (2025) · UC San Diego · doi:10.7270/q2t43zqk
BindingDB Entry 50007910: Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models.
BindingDB (2021) · UC San Diego · doi:10.7270/q2542rxh
BindingDB Entry 50021778: Histone deacetylase (HDAC) inhibitor specificity determinants are preserved in a class of dual HDAC/non-covalent proteasome inhibitors.
BindingDB (2025) · UC San Diego · doi:10.7270/q2qj7nzq
BindingDB Entry 50023418: Discovery of Novel Hydrazide-Based HDAC3 Inhibitors as Epigenetic Immunomodulators for Cancer Immunotherapy.
BindingDB (2026) · UC San Diego · doi:10.7270/q2tf038c

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Authors: Hornig, E., Heppt, M. V., Graf, S. A., Ruzicka, T., & Berking, C.
Affiliations: LMU Klinikum (DE)
Corresponding author: Berking, Carola
ORCID: Heppt, Markus V.
Ruzicka, Thomas
Berking, Carola
Venue: Experimental Dermatology
Publisher: Wiley
Published: 2016-10-28
Volume: 25
Issue: 11
Pages: 831-838
ISSN: 0906-6705 (ISSN-L)
1600-0625
DOI: 10.1111/exd.13089
OpenAlex: W2543055468
Cited by: 50
References: 69
Citations by year: 2026: 2 · 2025: 6 · 2024: 5 · 2023: 3 · 2022: 2 · 2021: 6 · 2020: 2 · 2019: 8 · 2018: 7 · 2017: 9
FWCI: 0.72
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: onlinelibrary.wiley.com/termsAndConditions#vor (vor)
Locations: Experimental Dermatology (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 › Melanoma and MAPK Pathways
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Epigenetics and DNA Methylation
Keywords: histone deacetylase, melanoma, histone deacetylase inhibitors, epigenetic regulation, chromatin, vorinostat, entinostat, valproic acid, G1 cell cycle arrest, apoptosis, immunogenicity, BRAF inhibitor resistance, immune checkpoint blockade, combination therapy, hematologic toxicity
MeSH terms: Animals, Clinical Trials as Topic, Histone Deacetylases, Humans, Melanoma, Histone Deacetylase Inhibitors

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Inhibition of histone deacetylases in melanoma—a perspective from bench to bedside

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