Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation
Copyright policy )Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation
IDHology Among the most exciting drug targets to emerge from cancer genome sequencing projects are two related metabolic enzymes, isocitrate dehydrogenases 1 and 2 (IDH1, IDH2). Mutations in the IDH1 and IDH2 genes are common in certain types of human cancer. Whether inhibition of mutant IDH activity might offer therapeutic benefits is unclear (see the Perspective by Kim and DeBerardinis ). F. Wang et al. (p. 622 , published online 4 April) isolated a small molecule that selectively inhibits mutant IDH2, describe the structural details of its binding to the mutant enzyme, and show that this compound suppresses the growth of patient-derived leukemia cells harboring the IDH2 mutation. Rohle et al. (p. 626 , published online 4 April) show that a small molecule inhibitor of IDH1 selectively slows the growth of patient-derived brain tumor cells with the IDH1 mutation.
- Inserm France
- Agios Pharmaceuticals (United States) United States
- Institut Gustave Roussy France
- French Institute of Health and Medical Research France
- Agios Pharmaceuticals United States
Gene Expression Regulation, Leukemic, Phenylurea Compounds, Antineoplastic Agents, Crystallography, X-Ray, Isocitrate Dehydrogenase, Hematopoiesis, Glutarates, Leukemia, Myeloid, Acute, Catalytic Domain, Cell Line, Tumor, Humans, Point Mutation, Erythropoiesis, Mutant Proteins, Leukemia, Erythroblastic, Acute, Molecular Targeted Therapy, Enzyme Inhibitors, Allosteric Site, Cells, Cultured, Cell Proliferation
Gene Expression Regulation, Leukemic, Phenylurea Compounds, Antineoplastic Agents, Crystallography, X-Ray, Isocitrate Dehydrogenase, Hematopoiesis, Glutarates, Leukemia, Myeloid, Acute, Catalytic Domain, Cell Line, Tumor, Humans, Point Mutation, Erythropoiesis, Mutant Proteins, Leukemia, Erythroblastic, Acute, Molecular Targeted Therapy, Enzyme Inhibitors, Allosteric Site, Cells, Cultured, Cell Proliferation
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