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Article

Roles of metal ions in the selective inhibition of oncogenic variants of isocitrate dehydrogenase 1.

Communications biology - 1 Nov 2021

Liu Shuang, Abboud Martine I, John Tobias, Mikhailov Victor, Hvinden Ingvild, Walsby-Tickle John, Liu Xiao, Pettinati Ilaria, Cadoux-Hudson Tom, McCullagh James S O, Schofield Christopher J

Abstract excerpt

Cancer linked isocitrate dehydrogenase (IDH) 1 variants, notably R132H IDH1, manifest a 'gain-of-function' to reduce 2-oxoglutarate to 2-hydroxyglutarate. High-throughput screens have enabled clinically useful R132H IDH1 inhibitors, mostly allosteric binders at the dimer interface. We report investigations on roles of divalent metal ions in IDH substrate and inhibitor binding that rationalise this observation....

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PMID: 34725432
DOI: 10.1038/s42003-021-02743-5
PMCID: PMC8560763

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