Resistance to the isocitrate dehydrogenase 1 mutant inhibitor ivosidenib can be overcome by alternative dimer-interface binding inhibitors

Ivosidenib, an inhibitor of isocitrate dehydrogenase 1 (IDH1) R132C and R132H variants, is approved for the treatment of acute myeloid leukaemia (AML). Resistance to ivosidenib due to a second site mutation of IDH1 R132C, leading to IDH1 R132C/S280F, has emerged. We describe biochemical, crystallogr...

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Bibliographic Details
Main Authors: Reinbold, R, Hvinden, IC, Rabe, P, Herold, RA, Finch, A, Wood, J, Morgan, M, Staudt, M, Clifton, IJ, Armstrong, FA, McCullagh, JSO, Redmond, J, Bardella, C, Abboud, MI, Schofield, CJ
Format: Journal article
Language:English
Published: Springer Nature 2022