Article
Biochemical, cellular, and biophysical characterization of a potent inhibitor of mutant isocitrate dehydrogenase IDH1.
The Journal of biological chemistry - 16 May 2014
Davis Mindy I, Gross Stefan, Shen Min, Straley Kimberly S, Pragani Rajan, Lea Wendy A, Popovici-Muller Janeta, DeLaBarre Byron, Artin Erin, Thorne Natasha, Auld Douglas S, Li Zhuyin, Dang Lenny, Boxer Matthew B, Simeonov Anton
Abstract excerpt
Two mutant forms (R132H and R132C) of isocitrate dehydrogenase 1 (IDH1) have been associated with a number of cancers including glioblastoma and acute myeloid leukemia. These mutations confer a neomorphic activity of 2-hydroxyglutarate (2-HG) production, and 2-HG has previously been implicated as...
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