KRAS4B (KRAS) is arguably the most sought-after anti-cancer drug target that is found mutated in many forms of cancer, including in 98% of pancreatic and 45% of colorectal cancers. The FDA has recently approved a covalent inhibitor specific to the G12C variant of KRAS that is common in small cell lung cancer. However, no comparable progress has been made on other key KRAS mutants that together represent over 80% of KRAS-driven cancers. I will discuss our efforts to inhibit these mutants with small-molecule non-covalent allosteric inhibitors that have originally emerged from a computation-guided discovery workflow.

Targeting KRAS with small-molecule non-covalent inhibitors

ACS Spring 2022

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