After approvals for one of cancer's 'undruggable' targets, research into new KRAS therapies booms: #AACR24
For cancer researchers, the potential was as obvious as the problem.
Mutations to the KRAS gene drive nearly a third of all cancers. A laundry list of code alterations — mutations called G12C, G12D, G12V, G12A, G13C, Q61H, and so on — resulting in protein building block changes could all be targets to stop aggressive cancers if only the right molecule could be found.
And that was the challenge. Long known as one of biopharma’s “undruggable” targets, the protein’s smooth and unusual shape meant it lacked the grooves that typically act as binding sites for drugs. That was until a landmark 2013 paper from Kevan Shokat’s lab at the University of California San Francisco described a new, hidden pocket and small molecules that used it to inhibit the KRAS G12C-mutated protein.
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