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Linking of 2-Oxoglutarate and Substrate Binding Sites Enables Potent and Highly Selective Inhibition of JmjC Histone Demethylases


  • This work was supported by the Biotechnology and Biological Sciences Research Council, the Wellcome Trust, the European Research Council, the German Academic Exchange Service (DAAD) (L.H.), the European Union, and the Structural Genomics Consortium (registered charity no. 1097737).


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Select an isoform: Linking of cosubstrate and substrate binding sites enables highly selective inhibiton of isoforms of human histone lysine demethylases. The results should provide a basis for the development of potent and selective JmjC inhibitors, possibly suitable for clinical use.

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