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Potent and Selective Inhibition of Histone Deacetylase 6 (HDAC6) Does Not Require a Surface-Binding Motif.

Publication TypeJournal Article
AuthorsWagner, FF, Olson DE, Gale JP, Kaya T., Weïwer M., Aidoud N., Thomas M., Davoine EL, Lemercier BC, Zhang YL, and Holson EB
AbstractHydroxamic acids were designed, synthesized, and evaluated for their ability to selectively inhibit human histone deacetylase 6 (HDAC6). Several inhibitors, including compound 14 (BRD9757), exhibited excellent potency and selectivity despite the absence of a surface-binding motif. The binding of these highly efficient ligands for HDAC6 is rationalized via structure-activity relationships. These results demonstrate that high selectivity and potent inhibition of HDAC6 can be achieved through careful choice of linker element only.
Year of Publication2013
JournalJournal of medicinal chemistry
Date Published (YYYY/MM/DD)2013/02/18
ISSN Number0022-2623
DOI10.1021/jm301355j
PubMedhttp://www.ncbi.nlm.nih.gov/pubmed/23368884?dopt=Abstract