You are here

Nature chemical biology DOI:10.1038/nchembio.313

Chemical phylogenetics of histone deacetylases.

Publication TypeJournal Article
Year of Publication2010
AuthorsBradner, JE, West, N, Grachan, ML, Greenberg, EF, Haggarty, SJ, Warnow, T, Mazitschek, R
JournalNature chemical biology
Volume6
Issue3
Pages238-243
Date Published2010/03/01
ISSN1552-4450
Abstract

The broad study of histone deacetylases in chemistry, biology and medicine relies on tool compounds to derive mechanistic insights. A phylogenetic analysis of class I and II histone deacetylases (HDACs) as targets of a comprehensive, structurally diverse panel of inhibitors revealed unexpected isoform selectivity even among compounds widely perceived as nonselective. The synthesis and study of a focused library of cinnamic hydroxamates allowed the identification of, to our knowledge, the first nonselective HDAC inhibitor. These data will guide a more informed use of HDAC inhibitors as chemical probes and therapeutic agents.

URLhttp://dx.doi.org/10.1038/nchembio.313
DOI10.1038/nchembio.313
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/20139990?dopt=Abstract