Cargando…
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...
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 |
Ejemplares similares
-
Roles of metal ions in the selective inhibition of oncogenic variants of isocitrate dehydrogenase 1
por: Liu, Shuang, et al.
Publicado: (2021) -
Exploiting Electrode Nanoconfinement to Investigate
the Catalytic Properties of Isocitrate Dehydrogenase (IDH1) and a
Cancer-Associated Variant
por: Herold, Ryan A., et al.
Publicado: (2021) -
Natural and synthetic 2-oxoglutarate derivatives are substrates for oncogenic variants of human isocitrate dehydrogenase 1 and 2
por: Liu, Xiao, et al.
Publicado: (2023) -
Resistance to the isocitrate dehydrogenase 1 mutant inhibitor ivosidenib can be overcome by alternative dimer-interface binding inhibitors
por: Reinbold, Raphael, et al.
Publicado: (2022) -
Isocitrate dehydrogenase variants in cancer — Cellular consequences and therapeutic opportunities
por: Liu, Shuang, et al.
Publicado: (2020)