Fig. 4: Mutant-selectivity of the KRAS(G12D) inhibitor TH-Z827.
From: KRAS(G12D) can be targeted by potent inhibitors via formation of salt bridge
a Binding affinities between TH-Z827 and GDP- or GMPPNP-bound KRAS (WT, G12C, or G12D). b SOS-catalyzed KRAS(G12C) or KRAS(G12D) nucleotide exchange assays in the presence of TH-Z827. c Principle of the split-luciferase reporter assay that detects the KRAS–CRAF interaction in lysates from HEK 293T cells, with or without TH-Z827. Two other compounds (the G12C inhibitor MRTX and the pan-RAS inhibitor BI-2852) were included as controls.
