Article
Resistance to the isocitrate dehydrogenase 1 mutant inhibitor ivosidenib can be overcome by alternative dimer-interface binding inhibitors.
Nature communications - 15 Aug 2022
Reinbold Raphael, Hvinden Ingvild C, Rabe Patrick, Herold Ryan A, Finch Alina, Wood James, Morgan Melissa, Staudt Maximillian, Clifton Ian J, Armstrong Fraser A, McCullagh James S O, Redmond Jo, Bardella Chiara, Abboud Martine I, Schofield Christopher J
Abstract excerpt
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, crystallographic, and cellular studies on the IDH1 R132C/S280F and R132H/S280F variants that inform on the mechanism of...
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