Small-molecule inhibitors of histone deacetylase for the treatment of cancer and non-cancer diseases: a patent review (2011 – 2013)

Abstract

Introduction: Histone deacetylases (HDACs) play an important role in mediating the expression of genes involved in cancer and non-cancer diseases. Overexpression of these enzymes has been shown in several types of cancer and some enzyme isoforms were described as responsible for neurological and inflammatory pathologies, hence the use of HDAC inhibitors represents a strategy for their treatment. Different chemical entities have been developed in the recent years and some of them entered clinical trials.

Areas covered: This review accounts for small-molecule inhibitors of HDAC reported in the patent literature covering the 2011 – 2013 period, and their potential use as therapeutics for cancer, neurological and inflammatory diseases.

Expert opinion: The development of isoform-selective HDAC inhibitors to avoid side effects in cancer therapy, to fight specific types of cancer, or for their potential use in non-cancer diseases is ongoing but still needs many scientific efforts. Moreover, the strategy of using these agents in combination with other epigenetic target modulators is a recent interesting therapeutic approach that could give promising results.

Keywords::

• cancer
• epigenetics
• histone deacetylase
• inflammation
• inhibitors
• small molecule

Notes

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