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J Med Chem. 2013 Feb 28;56(4):1772-6. doi: 10.1021/jm301355j. Epub 2013 Feb 18.

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

Author information

1
Stanley Center for Psychiatric Research, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.

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.

PMID:
23368884
DOI:
10.1021/jm301355j
[Indexed for MEDLINE]

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