Scientific Publications

Chemical phylogenetics of histone deacetylases.

Publication TypeJournal Article
AuthorsBradner, JE, West N., Grachan ML, Greenberg EF, Haggarty SJ, Warnow T., and Mazitschek R.
AbstractThe 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.
Year of Publication2010
JournalNature chemical biology
Date Published (YYYY/MM/DD)2010/03/01
ISSN Number1552-4450