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Recently, clinically effective covalent inhibitors of KRAS G12C have been developed, establishing two principles that form a foundation for future efforts.
Johnson et al. 2022a Cancer Discov 12: 913-23
First, KRAS is druggable. Second, each mutant form of KRAS is likely to have properties that make it uniquely druggable.
Johnson et al. 2022a Cancer Discov 12: 913-23
KRAS G12C inhibitors are currently changing the treatment paradigm for patients with NSCLC (KRAS G12C m.) and CRC.
Hofmann et al. 2022 Cancer Discov 12: 924-37
Mutant-selective KRAS G12C inhibitors target approx. 13.6% of all KRAS-driven cancers.
Hofmann et al. 2022 Cancer Discov 12: 924-37
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