1222184-99-7Relevant academic research and scientific papers
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.
HISTONE LYSINE DEMETHYLASE INHIBITORS
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Page/Page column 82, (2010/04/30)
The invention provides a compound which is an iV-oxalylglycine derivative of formula (I): a hydroxamic acid derivative of formula (II): or a heteroaryl derivative of fomula (III): wherein n; Z1; Z2; Y1; Y2; A; p; X1; X2; m; R4; B; R5; R6; R7; R8; R9; X3; R10; R11 and R12 are as defined herein, or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of the human 2-oxoglutarate-dependant JMJD2 subfamily of histone demethylases, in particular JMJD2E. Such inhibitors are useful in changing the epigenetic state of cells resulting in the inhibition / activation of chromatin remodelling, multiple gene activation / deactivation, and in treating cancer and other conditions characterised by undesirable cellular proliferation, and psychiatric disorders including depression.
