Article
NMR in integrated biophysical drug discovery for RAS: past, present, and future.
Journal of biomolecular NMR - 1 Nov 2020
Marshall Christopher B, KleinJan Fenneke, Gebregiworgis Teklab, Lee Ki-Young, Fang Zhenhao, Eves Ben J, Liu Ningdi F, Gasmi-Seabrook Geneviève M C, Enomoto Masahiro, Ikura Mitsuhiko
Abstract excerpt
Mutations in RAS oncogenes occur in ~ 30% of human cancers, with KRAS being the most frequently altered isoform. RAS proteins comprise a conserved GTPase domain and a C-terminal lipid-modified tail that is unique to each isoform. The GTPase domain is a 'switch' that regulates multiple signaling cascades that drive cell growth and proliferation when activated by binding GTP, and the signal is terminated by GTP...
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