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.
journal_name
Nat Chem Bioljournal_title
Nature chemical biologyauthors
Bradner JE,West N,Grachan ML,Greenberg EF,Haggarty SJ,Warnow T,Mazitschek Rdoi
10.1038/nchembio.313subject
Has Abstractpub_date
2010-03-01 00:00:00pages
238-243issue
3eissn
1552-4450issn
1552-4469pii
nchembio.313journal_volume
6pub_type
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