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Anal Chem. 2013 Dec 17;85(24):11987-92. doi: 10.1021/ac402947a. Epub 2013 Nov 22.

A highly facile and specific assay for cancer-causing isocitrate dehydrogenase mutant using 13C4-labeled α-ketoglutarate and heteronuclear NMR.

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  • 1College of Pharmacy, Natural Product Research Institute, Seoul National University , Sillim-dong, Gwanak-gu, Seoul 151-742, Korea.

Abstract

Isocitrate dehydrogenase mutations with neomorphic activity of converting α-ketoglutarate to 2-hydroxyglutarate have been found in many types of cancers. We report an NMR-based assay specific for the mutant using (13)C4-labeled α-ketoglutarate. It can be done in a complex mixture without extraction, give time-dependent absolute quantitation, and be applied to enzyme inhibition studies. Its merits over conventional assays should facilitate inhibitor developments for a new class of target-oriented anticancer agents.

PMID:
24266712
DOI:
10.1021/ac402947a
[PubMed - indexed for MEDLINE]
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