Article
Inhibition of Cancer-Associated Mutant Isocitrate Dehydrogenases by 2-Thiohydantoin Compounds.
Journal of medicinal chemistry - 10 Sept 2015
Wu Fangrui, Jiang Hong, Zheng Baisong, Kogiso Mari, Yao Yuan, Zhou Chao, Li Xiao-Nan, Song Yongcheng
Abstract excerpt
Somatic mutations of isocitrate dehydrogenase 1 (IDH1) at R132 are frequently found in certain cancers such as glioma. With losing the activity of wild-type IDH1, the R132H and R132C mutant proteins can reduce α-ketoglutaric acid (α-KG) to d-2-hydroxyglutaric acid (D2HG). The resulting high conce...
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