2. Academic Validation
  3. Chemical phylogenetics of histone deacetylases

Chemical phylogenetics of histone deacetylases

  • Nat Chem Biol. 2010 Mar;6(3):238-243. doi: 10.1038/nchembio.313.
James E Bradner 1,  Nathan West,  Melissa L Grachan,  Edward F Greenberg,  Stephen J Haggarty,  Tandy Warnow,  Ralph Mazitschek
Affiliations

Affiliation

  • 1 [1] Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts, USA. [2] Chemical Biology Program, Broad Institute of Harvard and Massachusetts Institute of Technology, Cambridge, Massachusetts, USA. [3] Department of Medicine, Harvard Medical School, Boston, Massachusetts, USA.
PMID: 20139990 DOI: 10.1038/nchembio.313
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-115585
    HDAC4抑制剂
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