Strain-release alkylation of Asp12 enables mutant selective GTP-state targeting of K-Ras(G12D)
Q. Zheng, Z. Zhang, K. Z. Guiley, K. Shokat
This paper develops covalent inhibitors that target the K-Ras(G12D) mutation by crosslinking aspartate-12 in both GDP- and GTP-states, effectively suppressing cancer cell proliferation and tumor growth.
bioRxiv · Jul 1, 2023 · PreprintCancer Biology