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

Liu et al investigate the effects of divalent metal ions on catalysis and inhibition of the enzyme isocitrate dehydrogenase (IDH) and its cancer-linked variant R132H. They further identify the substrates for IDH as complexes with Mg2+ and show that allosteric inhibitors work by weakening Mg2+ bindin...

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Autores principales: Shuang Liu, Martine I. Abboud, Tobias John, Victor Mikhailov, Ingvild Hvinden, John Walsby-Tickle, Xiao Liu, Ilaria Pettinati, Tom Cadoux-Hudson, James S. O. McCullagh, Christopher J. Schofield
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2021
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Acceso en línea:https://doaj.org/article/87f044b46ee747dba26b0e27f7cc54e6
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Sumario:Liu et al investigate the effects of divalent metal ions on catalysis and inhibition of the enzyme isocitrate dehydrogenase (IDH) and its cancer-linked variant R132H. They further identify the substrates for IDH as complexes with Mg2+ and show that allosteric inhibitors work by weakening Mg2+ binding of R132H, providing mechanistic insights into the basis for selective R132H IDH1 inhibition.