Discovery of allosteric non-covalent KRAS inhibitors that bind with sub-micromolar affinity and disrupt effector binding
M. J. McCarthy, C. V. Pagba, P. Prakash, A. Naji, D. van der Hoeven, H. Liang, A. K. Gupta, Y. Zhou, K.-J. Cho, J. F. Hancock, A. A. Gorfe
This study identifies a pyrazolopyrimidine-based allosteric KRAS inhibitor with sub-micromolar affinity that disrupts effector binding and inhibits cancer cell growth.
bioRxiv · Oct 11, 2018Biochemistry