Isoform-selective histone deacetylase inhibitors.

ABSTRACT: 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.

SUBMITTER: Bieliauskas AV 

PROVIDER: S-EPMC2593472 | biostudies-other | 2008 Jul

REPOSITORIES: biostudies-other