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Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases.


ABSTRACT: Histone deacetylase (HDAC) inhibitors, including various benzamides and hydroxamates, are currently in clinical development for a broad range of human diseases, including cancer and neurodegenerative diseases. We recently reported the identification of a family of benzamide-type HDAC inhibitors that are relatively non-toxic compared with the hydroxamates. Members of this class of compounds have shown efficacy in cell-based and mouse models for the neurodegenerative diseases Friedreich ataxia and Huntington disease. Considerable differences in IC(50) values for the various HDAC enzymes have been reported for many of the HDAC inhibitors, leading to confusion as to the HDAC isotype specificities of these compounds. Here we show that a benzamide HDAC inhibitor, a pimelic diphenylamide (106), i

SUBMITTER: Chou CJ 

PROVIDER: S-EPMC2602898 | biostudies-literature | 2008 Dec

REPOSITORIES: biostudies-literature