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Discovery of the First Histone Deacetylase 6/8 Dual Inhibitors

David E Olson, Florence F Wagner, Taner Kaya, Jennifer P Gale, Nadia Aidoud, Emeline L Davoine, Fanny Lazzaro, Michel Weïwer, Yan-Ling Zhang, Edward B Holson

J Med Chem. 2013 Jun 13;56(11):4816-20.

PMID: 23672185

Abstract:

We disclose the first small molecule histone deacetylase (HDAC) inhibitor (3, BRD73954) capable of potently and selectively inhibiting both HDAC6 and HDAC8 despite the fact that these isoforms belong to distinct phylogenetic classes within the HDAC family of enzymes. Our data demonstrate that meta substituents of phenyl hydroxamic acids are readily accommodated upon binding to HDAC6 and, furthermore, are necessary for the potent inhibition of HDAC8.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP1440209960 BRD73954 BRD73954 1440209-96-0 Price
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