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Chem Soc Rev. 2008 Jul;37(7):1402-13. doi: 10.1039/b703830p. Epub 2008 May 8.

Isoform-selective histone deacetylase inhibitors.

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  • 1Department of Chemistry, Wayne State University, Detroit, MI 48202, USA.


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.

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