Discovery of cell active macrocyclic peptides with on-target inhibition of KRAS signaling
S. Lim, N. Boyer, N. Boo, C. Huang, G. Venkatachalam, Y.-C. A. Juang, M. Garrigou, K. Kaan, K. M. Peh, A. Sadruddin, P. Gopal, R. Duggal, T. Y. Yuen, S. Ng, S. Kannan, , A. W. Partridge
This paper identifies macrocyclic peptides that inhibit KRAS signaling by binding to its hydrophobic pocket, showing on-target activity and improved proteolytic stability.
bioRxiv · Sep 11, 2021Biochemistry