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

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

Florence F Wagner, 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

J Med Chem. 2013 Feb 28;56(4):1772-6.

PMID: 23368884

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1423058858	BRD9757		1423058-85-8	Price

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