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Differentiating Inhibition Selectivity and Binding Affinity of Isocitrate Dehydrogenase 1 Variant Inhibitors

[Image: see text] Isocitrate dehydrogenase (IDH) 1/2 gain-of-function variants catalyze the production of the oncometabolite 2-hydroxyglutarate and are validated targets for leukemia treatment. We report binding and inhibition studies on 13 IDH1/2 variant inhibitors, including clinical candidates an...

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Detalles Bibliográficos
Autores principales: Liu, Shuang, Abboud, Martine, Mikhailov, Victor, Liu, Xiao, Reinbold, Raphael, Schofield, Christopher J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2023
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10108345/
https://www.ncbi.nlm.nih.gov/pubmed/36952395
http://dx.doi.org/10.1021/acs.jmedchem.3c00203