Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-mediated Activation

K-Ras 2, Ki-Ras, c-K-ras, c-Ki-ras, GTPase KRas, N-terminally processed

GMTEYKLVVVGAVGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFL
CVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKSDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQGVDDAFYTL
VREIRKHKEK

28% PEG8000, 0.1 M sodium acetate, 5% DMSO, pH 4.5, VAPOR DIFFUSION, SITTING DROP, temperature 291K

THE CRYSTALLIZED SEQUENCE CORRESPONDS TO UNP P01116-2 OF ISOFORM 2B OF GTPASE KRAS

HYDROGENS HAVE BEEN ADDED IN THE RIDING POSITIONS

small GTPase, Signaling transduction, Raf, Ral, Sos, PI3K, cytosol, binder, HYDROLASE, Inhibitor of Sos-mediated activation

MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLC
VFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQGVDDAFYTLV
REIRKHKEK