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Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation

4 Apr 2013

Abstract excerpt

A number of human cancers harbor somatic point mutations in the genes encoding isocitrate dehydrogenases 1 and 2 (IDH1 and IDH2). These mutations alter residues in the enzyme active sites and confer a gain-of-function in cancer cells, resulting in the accumulation and secretion of the oncometabolite (R)-2-hydroxyglutarate (2HG). We developed a small molecule, AGI-6780, that potently and selectively inhibits the...

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PMID: 23558173
DOI: 10.1126/science.1234769

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