Roles of metal ions in the selective inhibition of oncogenic variants of isocitrate dehydrogenase 1
Liu et al investigate the effects of divalent metal ions on catalysis and inhibition of the enzyme isocitrate dehydrogenase (IDH) and its cancer-linked variant R132H. They further identify the substrates for IDH as complexes with Mg2+ and show that allosteric inhibitors work by weakening Mg2+ bindin...
Guardado en:
Autores principales: | , , , , , , , , , , |
---|---|
Formato: | article |
Lenguaje: | EN |
Publicado: |
Nature Portfolio
2021
|
Materias: | |
Acceso en línea: | https://doaj.org/article/87f044b46ee747dba26b0e27f7cc54e6 |
Etiquetas: |
Agregar Etiqueta
Sin Etiquetas, Sea el primero en etiquetar este registro!
|
Sumario: | Liu et al investigate the effects of divalent metal ions on catalysis and inhibition of the enzyme isocitrate dehydrogenase (IDH) and its cancer-linked variant R132H. They further identify the substrates for IDH as complexes with Mg2+ and show that allosteric inhibitors work by weakening Mg2+ binding of R132H, providing mechanistic insights into the basis for selective R132H IDH1 inhibition. |
---|