Scientific Publications

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

Publication TypeJournal Article
AuthorsOlson, DE, Wagner FF, Kaya T., Gale JP, Aidoud N., Davoine EL, Lazzaro F., Weïwer M., Zhang YL, and Holson EB
AbstractWe 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.
Year of Publication2013
JournalJournal of medicinal chemistry
Volume56
Issue11
Pages4816-20
Date Published (YYYY/MM/DD)2013/06/13
ISSN Number0022-2623
DOI10.1021/jm400390r
PubMedhttp://www.ncbi.nlm.nih.gov/pubmed/23672185?dopt=Abstract