| Literature DB >> 23368884 |
Florence F Wagner1, David E Olson, Jennifer P Gale, Taner Kaya, Michel Weïwer, Nadia Aidoud, Méryl Thomas, Emeline L Davoine, Bérénice C Lemercier, Yan-Ling Zhang, Edward B Holson.
Abstract
Hydroxamic 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.Entities:
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Year: 2013 PMID： 23368884 DOI： 10.1021/jm301355j
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446