Roles of metal ions in the selective inhibition of oncogenic variants of isocitrate dehydrogenase 1

Autor: Shuang Liu, Martine I. Abboud, Tobias John, Victor Mikhailov, Ingvild Hvinden, John Walsby-Tickle, Xiao Liu, Ilaria Pettinati, Tom Cadoux-Hudson, James S. O. McCullagh, Christopher J. Schofield
Jazyk: angličtina
Rok vydání: 2021
Předmět:
Zdroj: Communications Biology, Vol 4, Iss 1, Pp 1-16 (2021)
Druh dokumentu: article
ISSN: 2399-3642
DOI: 10.1038/s42003-021-02743-5
Popis: 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.
Databáze: Directory of Open Access Journals