Article
Optimization of Covalent 6-Cyanoquinazoline KRASG12C Inhibitors for the Treatment of Solid Tumors.
Journal of medicinal chemistry - 23 Apr 2026
Waldo Jesse P, Krawczuk Paul J, Kelly Christopher B, Callas Christopher G, Cisar Justin S, Eccles Wendy, Guerrero Carlos A, Hack Michael D, Jones William M, Keohane Colleen E, Li Lian-Sheng, Meegalla Sanath, Padilla-Salinas Rosaura, Rosano Robert J, Shimkin Kirk W, Simonnet Yvan R F, Sitkoff Doree, Sookezian Anasheh, Winters Michael P, Bush Tammy L, Cheung Sheldon T, Del Rosario Amanda M, Hansen Rasmus, Janes Matthew R, Janjua Haleema, Kazmi Faraz, Kirkpatrick Robert, La David, Lenhart Ryan, Lorenzi Matthew V, Liu Yi, Mesens Natalie, Milligan Cynthia M, Murrey Heather, Peters Ulf, Ren Pingda, Richter Mark, Rizzolio Michele, Rao Swetha, Shaffer Paul, Stratton Christopher F, Szewczuk Lawrence M, Wen Jenny, Wong Victoria, Yanovich Carol, Laquerre Sylvie, Edwards James P, Leonard Kristi A
Abstract excerpt
The KRASG12C mutation is a critical therapeutic target in the management of solid tumors, owing to its role in oncogenic signaling. Recent advances in covalent inhibitors that target mutant KRAS cysteine-12 have demonstrated the potential to halt aberrant signaling associated with this historically "undruggable" target. Here, we report the identification of 6-cyanoquinazoline covalent irreversible KRASG12C...
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