Article
Radioprotection of IDH1-Mutated Cancer Cells by the IDH1-Mutant Inhibitor AGI-5198.
Cancer research - 15 Nov 2015
Molenaar Remco J, Botman Dennis, Smits Myrthe A, Hira Vashendriya V, van Lith Sanne A, Stap Jan, Henneman Peter, Khurshed Mohammed, Lenting Krissie, Mul Adri N, Dimitrakopoulou Dionysia, van Drunen Cornelis M, Hoebe Ron A, Radivoyevitch Tomas, Wilmink Johanna W, Maciejewski Jaroslaw P, Vandertop W Peter, Leenders William P, Bleeker Fonnet E, van Noorden Cornelis J
Abstract excerpt
Isocitrate dehydrogenase 1 (IDH1) is mutated in various types of human cancer to IDH1(R132H), a structural alteration that leads to catalysis of α-ketoglutarate to the oncometabolite D-2-hydroxyglutarate. In this study, we present evidence that small-molecule inhibitors of IDH1(R132H) that are being developed for cancer therapy may pose risks with coadministration of radiotherapy. Cancer cells heterozygous for...
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