Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS <sup>G12C</sup> Inhibitor
Joachim Bröker(Boehringer Ingelheim (Austria)), Alex G. Waterson(Vanderbilt University), Chris A. Smethurst(Boehringer Ingelheim (Austria)), Dirk Kessler(Boehringer Ingelheim (Austria)), Jark Böttcher(Boehringer Ingelheim (Austria)), Moriz Mayer(Boehringer Ingelheim (Austria)), Gerhard Gmaschitz(Boehringer Ingelheim (Austria)), Jason Phan(Vanderbilt University), Andrew J. Little(Vanderbilt University), Jason R. Abbott(Vanderbilt University), Qi Sun(Vanderbilt University), Michael Gmachl(Boehringer Ingelheim (Austria)), Dorothea Rudolph(Boehringer Ingelheim (Austria)), Heribert Arnhof(Boehringer Ingelheim (Austria)), Klaus Rumpel(Boehringer Ingelheim (Austria)), Fabio Savarese(Boehringer Ingelheim (Austria)), Thomas Gerstberger(Boehringer Ingelheim (Austria)), Nikolai Mischerikow(Boehringer Ingelheim (Austria)), Matthias Treu(Boehringer Ingelheim (Austria)), Lorenz Herdeis(Boehringer Ingelheim (Austria)), Tobias Wunberg(Boehringer Ingelheim (Austria)), Andreas Gollner(Boehringer Ingelheim (Austria)), Harald Weinstabl(Boehringer Ingelheim (Austria)), Andreas Mantoulidis(Boehringer Ingelheim (Austria)), Oliver Krämer(Boehringer Ingelheim (Austria)), Darryl B. McConnell(Boehringer Ingelheim (Austria)), Stephen W. Fesik(Vanderbilt University)
Cited by 80Open Access
Abstract
inhibitors but also provides a starting point for the discovery of inhibitors against other oncogenic KRAS mutants.
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