NMR in integrated biophysical drug discovery for RAS: past, present, and future.

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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• Cyclic Nucleotide Phosphodiesterases, Type 6
• Drug Discovery
• Guanine Nucleotide Exchange Factors
• Membrane Proteins
• Nuclear Magnetic Resonance, Biomolecular