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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, Alex G. Waterson, Chris A. Smethurst, Dirk Kessler, Jark Böttcher, Moriz Mayer, Gerhard Gmaschitz, Jason Phan, Andrew J. Little, Jason R. Abbott,

Journal of Medicinal Chemistry · 2022 · 81 citations · 21 references

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Abstract

inhibitors but also provides a starting point for the discovery of inhibitors against other oncogenic KRAS mutants.

References

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The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients

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