Linking of 2-oxoglutarate and substrate binding sites enables potent and highly selective inhibition of JmjC histone demethylases

Angew Chem Int Ed Engl. 2012 Feb 13;51(7):1631-4. doi: 10.1002/anie.201107833. Epub 2012 Jan 12.
No abstract available

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding Sites / drug effects
  • Cross-Linking Reagents / chemical synthesis
  • Cross-Linking Reagents / chemistry
  • Cross-Linking Reagents / pharmacology*
  • Humans
  • Jumonji Domain-Containing Histone Demethylases / antagonists & inhibitors*
  • Jumonji Domain-Containing Histone Demethylases / chemistry
  • Ketoglutaric Acids / chemistry
  • Ketoglutaric Acids / pharmacology*
  • Models, Molecular
  • Molecular Structure
  • Structure-Activity Relationship
  • Substrate Specificity

Substances

  • Cross-Linking Reagents
  • Ketoglutaric Acids
  • Jumonji Domain-Containing Histone Demethylases