Fig. 1: Identification of a non-covalent inhibitor that inactivates common cancer-causing KRAS mutants.
From: Pan-KRAS inhibitor disables oncogenic signalling and tumour growth
a, Chemical structures of the indicated compounds. b, Isogenic BaF3 cells expressing the indicated KRAS mutants were treated for 5 days in the absence of IL3 (oncogene dependent growth) to determine the effect on proliferation (mean ± s.e.m., n = 5, unless otherwise indicated, n denotes biological replicates). c, Cocrystal structures of drug-bound WT, G12C, G12D, G12V and G13D mutant KRAS. d,e, The effect of KRASi treatment on nucleotide exchange stimulated either by SOS1 (d) or EDTA (e). The reaction of KRAS G12C with the covalent inhibitor sotorasib is shown for comparison. A representative of two independent repeats is shown in d and e.
