1222185-07-0Relevant articles and documents
Inhibition of histone demethylases by 4-Carboxy-2,2'-Bipyridyl compounds
Chang, Kai-Hsuan,King, Oliver N. F.,Tumber, Anthony,Woon, Esther C. Y.,Heightman, Tom D.,Mcdonough, Michael A.,Schofield, Christopher J.,Rose, Nathan R.
, p. 759 - 764 (2012/01/06)
Exploiting epigenetics: 2-Oxoglutarate (2OG)-dependent histone lysine demethylases, such as JMJD2E, are potential therapeutic targets in a range of diseases. Through structure-activity relationship studies and analyses, we identified a potent 4-carboxy-2,2'-bipyridyl compound, which inhibits JMJD2E with an IC50 value of 110nM, representing a 66-fold improvement over the lead compound. These bipyridyl derivatives bind in the 2-oxoglutarate binding site.