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Updated: Apr 24, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Histone deacetylase inhibitors in oral squamous cell carcinoma treatment
Jason Tasoulas1, Constantinos Giaginis, Efstratios Patsouris
1National and Kapodistrian University of Athens, Medical School, First Department of Pathology , Athens , Greece.
Abstract:
Introduction: The involvement of the histone deacetylases (HDACs) family in tumor development and progression is well demonstrated. HDAC inhibitors (HDACis) constitute a novel, heterogeneous family of highly selective anticancer agents that inhibit HDACs and present significant antitumor activity in several human malignancies, including oral squamous cell carcinoma (OSCC). Areas covered: This review summarizes the current research on the anticancer activity of HDACis against OSCC. The review also presents the molecular mechanisms of HDACis action and the existing studies evaluating their utilization in combined therapies of OSCC. Expert opinion: The currently available data support evidence that HDACis may provide new therapeutic options against OSCC, decreasing treatment side effects and allowing a more conservative therapeutic approach. Future research should be focused on in vivo and clinical evaluation of their utilization as combined therapies or monotherapies. Before HDACis can be brought into clinical practice as treatment options for OSCC, further evaluation is needed to determine their optimal dosage, the appropriate duration of treatment and whether they should be used in combination or as stand-alone therapeutics.
Insights
Histone deacetylase inhibitors (HDACis) show promise as anticancer agents for oral squamous cell carcinoma (OSCC). Further research is needed to optimize their use as monotherapies or in combination treatments.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Histone deacetylases (HDACs) play a crucial role in cancer development and progression.
- HDAC inhibitors (HDACis) are a class of anticancer agents targeting HDACs.
- HDACis have demonstrated significant antitumor activity in various human cancers, including OSCC.
Purpose of the Study:
- To review current research on the anticancer activity of HDACis against OSCC.
- To summarize the molecular mechanisms underlying HDACis action in OSCC.
- To evaluate existing studies on the combined use of HDACis in OSCC therapy.
Main Methods:
- Literature review of preclinical and clinical studies on HDACis in OSCC.
- Analysis of molecular mechanisms of HDACis.
- Synthesis of data on combination therapies involving HDACis for OSCC.
Main Results:
- HDACis exhibit notable antitumor effects in OSCC models.
- HDACis function through various molecular pathways impacting cancer cells.
- Studies suggest potential benefits of combining HDACis with other therapeutic modalities for OSCC.
Conclusions:
- HDACis represent promising therapeutic options for OSCC, potentially reducing side effects and allowing conservative treatment.
- Further in vivo and clinical studies are essential to determine optimal dosage, treatment duration, and combination strategies for HDACis in OSCC.
- Clinical implementation of HDACis for OSCC requires comprehensive evaluation of their efficacy and safety as monotherapies or in combination regimens.
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