Chemical phylogenetics of histone deacetylases.
Nat Chem Biol
Authors | |
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
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Journal | Nat Chem Biol
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Volume | 6
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Issue | 3
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Pages | 238-243
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Date Published | 2010 Mar
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ISSN | 1552-4469
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URL | |
DOI | 10.1038/nchembio.313
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PubMed ID | 20139990
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PubMed Central ID | PMC2822059
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Links | |
Grant list | N01 / 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
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