Article
Crystal structures of pan-IDH inhibitor AG-881 in complex with mutant human IDH1 and IDH2.
Biochemical and biophysical research communications - 18 Sept 2018
Ma Rui, Yun Cai-Hong
Abstract excerpt
Some mutations of isocitrate dehydrogenase 1 and 2 observed in multiple kinds of malignant tumors can lead to a neomorphic enzyme activity that converts alpha-ketoglutarate (α-KG) to 2-hydroxyglutarate (2-HG). As an oncometabolite, 2-HG can cause epigenetic changes and impair cell differentiation. Inhibiting the activity of isocitrate dehydrogenase mutants (mIDH) is considered to be an effective therapy for the...
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