Histone demethylases catalyze the removal of methyl groups from lysine side chains in histone proteins and are important enzymes for regulating gene expression. They play key roles in various aspects of development, and several have been identified as potential targets for the treatment of esophageal, breast, prostate and colon cancers.

Nathan Rose and colleagues, University of Oxford, UK, report the most potent histone demethylase inhibitors identified to date, using a combination of in vitro screening, mass spectrometry, and crystallographic approaches.

This work forms a basis for the design of even more potent and selective inhibitors of histone demethylases, for use in defining their roles in developmental and pathogenic pathways, and could lead to therapeutically useful inhibitors of these enzymes.

• Inhibition of Histone Demethylases by 4-Carboxy-2,2′-Bipyridyl Compounds
  K.-H. Chang, O. N. F. King, A. Tumber, E. C. Y. Woon, T. D. Heightman, M. A. McDonough, C. J. Schofield, N. R. Rose,
  ChemMedChem 2011, 6(05).
  DOI: 10.1002/cmdc.201100026