Methods for assessing binding of a small-molecule radioligand to soluble enzyme isocitrate dehydrogenase 1 variants
Isocitrate dehydrogenase 1 (IDH1) is a cytosolic NADP+-dependent enzyme involved in cellular redox homeostasis and 2-oxoglutarate (2-OG) metabolism. Glioma-associated mutations in IDH1 confer a neomorphic enzymatic activity, resulting in the production and accumulation of the oncometabolite D-2-hydroxyglutarate (2-HG),...