Articles with "variant inhibitors" as a keyword



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

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Published in 2023 at "Journal of Medicinal Chemistry"

DOI: 10.1021/acs.jmedchem.3c00203

Abstract: 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 and… read more here.

Keywords: inhibition selectivity; binding affinity; inhibition; idh1 ... See more keywords