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Issue 7, 2008
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Isoform-selective histone deacetylaseinhibitors

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Histone deacetylase (HDAC) proteins are transcription regulators linked to cancer. As a result, multiple small molecule HDAC inhibitors are in various phases of clinical trials as anti-cancer drugs. The majority of HDAC inhibitors non-selectively influence the activities of eleven human HDAC isoforms, which are divided into distinct classes. This tutorial review focuses on the recent progress toward the identification of class-selective and isoform-selective HDAC inhibitors. The emerging trends suggest that subtle differences in the active sites of the HDAC isoforms can be exploited to dictate selectivity.

Graphical abstract: Isoform-selective histone deacetylase inhibitors

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Article information

05 Mar 2008
First published
08 May 2008

Chem. Soc. Rev., 2008,37, 1402-1413
Article type
Tutorial Review

Isoform-selective histone deacetylase inhibitors

A. V. Bieliauskas and M. K. H. Pflum, Chem. Soc. Rev., 2008, 37, 1402
DOI: 10.1039/B703830P

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