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

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 investi...

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Hlavní autoři: Liu, S, Abboud, MI, John, T, Mikhailov, V, Hvinden, I, Walsby-Tickle, J, Schofield, CJ, Liu, X, Pettinati, I, Cadoux-Hudson, T, McCullagh, JSO
Médium: Journal article
Jazyk:English
Vydáno: Springer Nature 2021