Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Editor-in-Chief: Natalia Ortúzar
Impact Factor: 3.046
ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 74/254 (Pharmacology & Pharmacy)
Online ISSN: 1860-7187
April 19, 2011
VIP: Inhibition of Histone Demethylases by 4-Carboxy-2,2'-Bipyridyl Compounds
Kai-Hsuan Chang, Oliver N. F. King, Anthony Tumber, Esther C. Y. Woon, Tom D. Heightman, Michael A. McDonough, Christopher J. Schofield, and Nathan R. Rose*
Histone demethylases, which catalyze the removal of methyl groups from lysine side chains in histone proteins, are important enzymes in the regulation of 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. This Communication by Rose and colleagues at the University of Oxford (UK) reports 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.
Received January 27, 2011; published online March 15, 2011, DOI: 10.1002/cmdc.201100026.