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Identification of the Clinical Development Candidate <b>MRTX849</b>, a Covalent KRAS<sup>G12C</sup> Inhibitor for the Treatment of Cancer

Jay B. Fell, John P. Fischer, Brian R. Baer, James F. Blake, Karyn Bouhana, David M. Briere, Karin Brown, Laurence E. Burgess, Aaron C. Burns, Michael Burkard, Harrah Chiang, Mark J. Chicarelli, Adam W. Cook, John J. Gaudino, Jill Hallin, Lauren Hanson, Dylan P. Hartley, Erik J. Hicken, Gary P. Hingorani, Ronald J. Hinklin, Macedonio J. Mejia, Peter Olson, Jennifer Otten, Susan P. Rhodes, Martha E. Rodriguez, Pavel Y. Savechenkov, Darin Smith, Niranjan Sudhakar, Francis X. Sullivan, Tony P. Tang, Guy Vigers, Lance Wollenberg, James G. Christensen, Matthew A. Marx

2020Journal of Medicinal Chemistry597 citationsDOIOpen Access PDF

Abstract

is described.

Topics & Concepts

ChemistryCovalent bondCysteineKRASDrug discoveryDrug developmentPharmacologyPotencyDrugCombinatorial chemistryIn vitroBiochemistryEnzymeMedicineGeneMutationOrganic chemistryBiochemical and Molecular ResearchProtein Kinase Regulation and GTPase SignalingProtein Tyrosine Phosphatases
Identification of the Clinical Development Candidate <b>MRTX849</b>, a Covalent KRAS<sup>G12C</sup> Inhibitor for the Treatment of Cancer | Litcius