Distal Covalent Targeting Suppresses Signaling of Oncogenic K-Ras(G13C) in Cancer Cells.

Abstract excerpt

Oncogenic mutations of Ras are among the most common genetic alterations in human cancer, with an estimated disease burden of >3 million new patients per year worldwide. Despite widespread appreciation of the importance of Ras in cancer, direct binding ligands, which block downstream signaling, were not reported until 2013 due to the lack of obvious drug binding pockets in the protein. The clinically approved...

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