Figure 1.
Potential routes for covalent inhibition of G12C Ras. (Left) Shokat et al. recently revealed a small molecule that occupies an allosteric pocket and inhibits Ras signaling (PDB: 4LYH). (Right) We aimed to develop a covalent orthosteric ligand by mimicking the contact helix from Sos (PDB: 1NVW)