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Nat Chem Biol 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
JournalNat Chem Biol
Volume6
Issue3
Pages238-243
Date Published2010 Mar
ISSN1552-4469
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

Alternate JournalNat. Chem. Biol.
PubMed ID20139990
PubMed Central IDPMC2822059
Grant ListN01 / HL / NHLBI NIH HHS / United States
P01 CA078048-08 / CA / NCI NIH HHS / United States
K08 CA128972-02 / CA / NCI NIH HHS / United States
N01-C0-012400 / CO / NCI NIH HHS / United States
T32 CA079443-08 / CA / NCI NIH HHS / United States
T32 CA079443 / CA / NCI NIH HHS / United States
K08 CA128972-02S1 / CA / NCI NIH HHS / United States
K08 CA128972-01A1 / CA / NCI NIH HHS / United States
P01 CA078048-09 / CA / NCI NIH HHS / United States
P01 CA078048-10 / CA / NCI NIH HHS / United States
R01 DA028301-01 / DA / NIDA NIH HHS / United States
K08 CA128972 / CA / NCI NIH HHS / United States
N01-C0-012400 / / PHS HHS / United States
N01CO12400 / CA / NCI NIH HHS / United States
P01 CA078048 / CA / NCI NIH HHS / United States
R01 DA028301 / DA / NIDA NIH HHS / United States