Article
Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor.
Nature medicine - 1 Oct 2022
Hallin Jill, Bowcut Vickie, Calinisan Andrew, Briere David M, Hargis Lauren, Engstrom Lars D, Laguer Jade, Medwid James, Vanderpool Darin, Lifset Ella, Trinh David, Hoffman Natalie, Wang Xiaolun, David Lawson J, Gunn Robin J, Smith Christopher R, Thomas Nicole C, Martinson Matthew, Bergstrom Alex, Sullivan Francis, Bouhana Karyn, Winski Shannon, He Leo, Fernandez-Banet Julio, Pavlicek Adam, Haling Jacob R, Rahbaek Lisa, Marx Matthew A, Olson Peter, Christensen James G
Abstract excerpt
Recent progress in targeting KRASG12C has provided both insight and inspiration for targeting alternative KRAS mutants. In this study, we evaluated the mechanism of action and anti-tumor efficacy of MRTX1133, a potent, selective and non-covalent KRASG12D inhibitor. MRTX1133 demonstrated a high-affinity interaction with GDP-loaded KRASG12D with KD and IC50 values of ~0.2 pM and <2 nM, respectively, and ~700-fold...
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