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2013•Journal of Medicinal ChemistryOpen access

Discovery of the First Histone Deacetylase 6/8 Dual Inhibitors

David E. Olson, Florence F. Wagner, Taner Kaya, Jennifer Gale, Nadia Aidoud, Emeline Davoine, Fanny Lazzaro, Michel Weïwer, Yanling Zhang, Edward B. Holson

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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.

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What this paper is about

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.

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Available 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.

Key concepts: HDAC8, HDAC6, Chemistry, Histone deacetylase, Hydroxamic acid, Histone deacetylase 2, Gene isoform, HDAC10

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