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J Med Chem. 2013 Jun 13;56(11):4816-20. doi: 10.1021/jm400390r. Epub 2013 May 29.

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

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1
Stanley Center for Psychiatric Research, Broad Institute of MIT and Harvard, 7 Cambridge Center, Cambridge, Massachusetts 02142, USA.

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.

PMID:
23672185
DOI:
10.1021/jm400390r
[Indexed for MEDLINE]
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