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Dynamic combinatorial mass spectrometry leads to inhibitors of a 2-oxoglutarate-dependent nucleic acid demethylase

…, DW Wegman, KN Dack, MA McDonough…

文献索引:Woon, Esther C. Y.; Demetriades, Marina; Bagg, Eleanor A. L.; Aik, Weishen; Krylova, Svetlana M.; Ma, Jerome H. Y.; Chan, Munchiang; Walport, Louise J.; Wegman, David W.; Dack, Kevin N.; McDonough, Michael A.; Krylov, Sergey N.; Schofield, Christopher J. Journal of Medicinal Chemistry, 2012 , vol. 55, # 5 p. 2173 - 2184

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被引用次数: 25

摘要

2-Oxoglutarate-dependent nucleic acid demethylases are of biological interest because of their roles in nucleic acid repair and modification. Although some of these enzymes are linked to physiology, their regulatory roles are unclear. Hence, there is a desire to develop selective inhibitors for them; we report studies on AlkB, which reveal it as being amenable to selective inhibition by small molecules. Dynamic combinatorial chemistry linked to mass ...