Wisconsin Alumni Research Foundation

New Strategies to Drug Challenging Targets by Exploiting Covalent Targeting, Beyond Rule of 5 Bitopic Ligands and Binary Pharmacology


The GTP-ase K-Ras represents the most frequently altered oncogene in cancer patients. Directly targeting K-Ras is difficult due to its picomolar affinity for GTP/GDP and the absence of easily identifiable allosteric sites. Kevan M. Shokat, a professor of cellular and molecular pharmacology at UCSF, a professor of chemistry at UC Berkeley and an investigator with…

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