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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Detalles Bibliográficos
Autores principales: 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.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2022
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9378673/
https://www.ncbi.nlm.nih.gov/pubmed/35970853
http://dx.doi.org/10.1038/s41467-022-32436-4

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