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Selective class IIa HDAC inhibitors: myth or reality

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Abstract

The prospect of intervening, through the use of a specific molecule, with a cellular alteration responsible for a disease, is a fundamental ambition of biomedical science. Epigenetic-based therapies appear as a remarkable opportunity to impact on several disorders, including cancer. Many efforts have been made to develop small molecules acting as inhibitors of histone deacetylases (HDACs). These enzymes are key targets to reset altered genetic programs and thus to restore normal cellular activities, including drug responsiveness. Several classes of HDAC inhibitors (HDACis) have been generated, characterized and, in certain cases, approved for the use in clinic. A new frontier is the generation of subtype-specific inhibitors, to increase selectivity and to manage general toxicity. Here we will discuss about a set of molecules, which can interfere with the activity of a specific subclass of HDACs: the class IIa.

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Acknowledgments

Research activities were supported by FIRB (Progetto RBAP11S8C3_002), PRIN (Progetto 2010W4J4RM_002) and AIRC to CB.

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  1. Dipartimento di Scienze Mediche e Biologiche, Università degli Studi di Udine, P.le Kolbe, 4, 33100, Udine, Italy

    Eros Di Giorgio, Enrico Gagliostro & Claudio Brancolini

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  1. Eros Di Giorgio
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  2. Enrico Gagliostro
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  3. Claudio Brancolini
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Correspondence to Claudio Brancolini.

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Di Giorgio, E., Gagliostro, E. & Brancolini, C. Selective class IIa HDAC inhibitors: myth or reality. Cell. Mol. Life Sci. 72, 73–86 (2015). https://doi.org/10.1007/s00018-014-1727-8

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  • DOI: https://doi.org/10.1007/s00018-014-1727-8

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