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Chemical phylogenetics of histone deacetylases.
|Publication Type||Journal Article|
|Authors||Bradner, JE, West N., Grachan ML, Greenberg EF, Haggarty SJ, Warnow T., and Mazitschek R.|
|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.|
|Year of Publication||2010|
|Journal||Nature chemical biology|
|Date Published (YYYY/MM/DD)||2010/03/01|