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Updated: May 17, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Histone deacetylase inhibitors: a patent review (2009 - 2011)
Vincenzo Carafa1, Marco Miceli, Lucia Altucci
1Seconda Università degli Studi di Napoli, Dipartimento di Patologia Generale, Italy.
Introduction:
Given the involvement of histone deacetylases (HDACs) in regulation of gene expression, they are believed to be 'master regulators' of many diseases. Thus, HDAC inhibitors (HDACis) are able to modulate transcriptional activity. These molecules can induce cell cycle arrest, differentiation and apoptosis of tumor cells in culture and in animal models and therefore are emerging as an exciting new class of potential anti-cancer agents for the treatment of solid and hematological malignancies.
Areas Covered:
The aim of this review is to provide an overview of current knowledge and molecular mechanisms of HDACis, and the most recent patents existing in the field of HDACis from 2009 until 2011.
Expert Opinion:
In recent years, an increasing number of structurally diverse HDACis have been identified. In addition, non-cancer diseases, including neurodegeneration, metabolic, inflammatory and autoimmune disorders, infectious and cardiovascular diseases have also been proposed for an HDACi treatment. The growing body of evidence of the potential benefits of disease treatment based on the use of HDACis has led to a large number of patent applications throughout the world.
Insights
Histone deacetylase inhibitors (HDACis) show promise as anti-cancer agents by modulating gene expression and inducing tumor cell death. Research is expanding to explore HDACis for treating various non-cancer diseases as well.
Area of Science:
- Molecular Biology
- Pharmacology
- Oncology
Background:
- Histone deacetylases (HDACs) are key regulators of gene expression implicated in numerous diseases.
- HDAC inhibitors (HDACis) modulate transcriptional activity, offering therapeutic potential.
- HDACis induce anti-tumor effects like cell cycle arrest, differentiation, and apoptosis.
Purpose of the Study:
- To review current knowledge and molecular mechanisms of HDAC inhibitors.
- To survey recent patents related to HDAC inhibitors from 2009-2011.
Main Methods:
- Literature review
- Patent analysis
Main Results:
- Identification of diverse HDAC inhibitor structures.
- Expansion of HDAC inhibitor applications beyond cancer.
Conclusions:
- HDAC inhibitors are emerging as potential treatments for solid and hematological malignancies.
- Non-cancer diseases like neurodegeneration, metabolic, inflammatory, autoimmune, infectious, and cardiovascular disorders are potential targets for HDACi therapy.
- A significant increase in global patent applications for HDAC inhibitors reflects their growing therapeutic importance.
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