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Updated: Feb 21, 2026
Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Targeting Histone Deacetylases in Malignant Melanoma: A Future Therapeutic Agent or Just Great Expectations?
Nikolaos Garmpis1, Christos Damaskos2,3, Anna Garmpi4
1Second Department of Propedeutic Surgery, Laiko General Hospital, Medical School, National and Kapodistrian University of Athens, Athens, Greece nikosg22@hotmail.com.
Background/Aim:
Malignant melanoma is the most aggressive type of skin cancer, with increasing frequency and mortality. Melanoma is characterized by rapid proliferation and metastases. Malignant transformation of normal melanocytes is associated with imbalance between oncogenes' action and tumor suppressor genes. Mutations or inactivation of these genes plays an important role in the pathogenesis of malignant melanoma. Many target-specific agents improved progression-free survival but unfortunately metastatic melanoma remains incurable, so new therapeutic strategies are needed. The balance of histones' acetylation affects cell cycle progression, differentiation and apoptosis. Histone deacetylases (HDAC) are associated with different types of cancer. Histone deacetylase inhibitors (HDACI) are enzymes that inhibit the action of HDAC, resulting in block of tumor cell proliferation. A small number of these enzymes has been studied regarding their anticancer effects in melanoma. The purpose of this article was to review the therapeutic effect of HDACI against malignant melanoma, enlightening the molecular mechanisms of their action.
Materials And Methods:
The MEDLINE database was used. The keywords/ phrases were; HDACI, melanoma, targeted therapies for melanoma. Our final conclusions were based on studies that didn't refer solely to melanoma due to their wider experimental data. Thirty-two articles were selected from the total number of the search's results. Only English articles published until March 2017 were used.
Results:
Molecules, such as valproid acid (VPA), LBH589, LAQ824 (dacinostat), vorinostat, tubacin, sirtinol and tx-527, suberoyl bis-hydroxamic acid (SBHA), depsipeptide and Trichostatin A (TSA) have shown promising antineoplastic effects against melanoma.
Conclusion:
HDACI represent a promising agent for targeted therapy. More trials are required.
Insights
Histone deacetylase inhibitors (HDACI) show promise in treating malignant melanoma by blocking tumor cell proliferation. Further clinical trials are needed to explore their full therapeutic potential against this aggressive skin cancer.
Area of Science:
- Oncology
- Molecular Biology
- Dermatology
Background:
- Malignant melanoma is an aggressive skin cancer with increasing incidence and mortality.
- Its pathogenesis involves genetic imbalances and uncontrolled cell proliferation.
- Current treatments for metastatic melanoma are limited, necessitating novel therapeutic strategies.
Purpose of the Study:
- To review the therapeutic effects of histone deacetylase inhibitors (HDACI) against malignant melanoma.
- To elucidate the molecular mechanisms underlying HDACI's action in melanoma treatment.
Main Methods:
- A systematic literature search was conducted using the MEDLINE database.
- Keywords included HDACI, melanoma, and targeted therapies for melanoma.
- Thirty-two English articles published up to March 2017 were selected.
Main Results:
- Several molecules, including valproic acid (VPA), LBH589, and vorinostat, demonstrated significant antineoplastic effects in melanoma models.
- These compounds inhibit histone deacetylases (HDAC), leading to the blockage of tumor cell proliferation.
Conclusions:
- Histone deacetylase inhibitors (HDACI) represent a promising class of agents for targeted melanoma therapy.
- Additional clinical trials are essential to validate their efficacy and safety in patients.
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