Tumor cells frequently reprogram cellular metabolism from oxidative phosphorylation to
glycolysis. Isocitrate dehydrogenase 2 (IDH2) has been intensively studied due to its involvement in
the metabolic activity of cancer cells. Mutations in IDH2 promote neomorphic activity through the
generation of oncometabolite 2-hydroxyglutarate (2-HG). The overproduced 2-HG can competitively
inhibit α-KG-dependent dioxygenases to trigger cell differentiation disorders, a major cause of
blood tumors. This review outlines recent progress in the identification of IDH2 inhibitors in blood
cancer to provide a reference for ongoing and future clinical studies.
Keywords: Isocitrate dehydrogenase 2, IDH2, mutant, inhibitors, structure-activity relationship, blood cancer.
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