Linking of 2-Oxoglutarate and Substrate Binding Sites Enables Potent and Highly Selective Inhibition of JmjC Histone Demethylases (pages 1631–1634)
Dr. Esther C. Y. Woon, Dr. Anthony Tumber, Dr. Akane Kawamura, Dr. Lars Hillringhaus, Dr. Wei Ge, Dr. Nathan R. Rose, Jerome H. Y. Ma, Mun Chiang Chan, Louise J. Walport, Ka Hing Che, Dr. Stanley S. Ng, Dr. Brian D. Marsden, Prof. Udo Oppermann, Dr. Michael A. McDonough and Prof. Christopher J. Schofield
Article first published online: 12 JAN 2012 | DOI: 10.1002/anie.201107833
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.