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Journal of medicinal chemistry DOI:10.1021/jm400390r

Discovery of the first histone deacetylase 6/8 dual inhibitors.

Publication TypeJournal Article
Year of Publication2013
AuthorsOlson, DE, Wagner, FF, Kaya, T, Gale, JP, Aidoud, N, Davoine, EL, Lazzaro, F, Weïwer, M, Zhang, YL, Holson, EB
JournalJournal of medicinal chemistry
Volume56
Issue11
Pages4816-20
Date Published2013/06/13
ISSN0022-2623
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.

URLhttp://dx.doi.org/10.1021/jm400390r
DOI10.1021/jm400390r
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/23672185?dopt=Abstract