Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.

J Med Chem
Authors
Keywords
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.

Year of Publication
2013
Journal
J Med Chem
Volume
56
Issue
4
Pages
1772-6
Date Published
2013 Feb 28
ISSN
1520-4804
URL
DOI
10.1021/jm301355j
PubMed ID
23368884
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