Progress on covalent inhibition of KRASG12C

Kenneth D. Westover, Pasi A. Jänne, Nathanael S. Gray

Research output: Contribution to journalArticlepeer-review

18 Scopus citations


Recent reports of small-molecule approaches to directly inhibit oncogenic KRAS G12C have invigorated the RAS research community by raising the possibility of drugging a protein that was long considered “undruggable.” A new iteration of covalent compounds targeting the allosteric switch II pocket of KRASG12C showed improved potency and selectivity and enabled studies demonstrating that KRASG12C rapidly cycles its nucleotide substrate. This report illustrates the value of chemical probes in dissecting RAS biology and raises additional hope for development of viable pharmacologic strategies for directly targeting KRASG12C.

Original languageEnglish (US)
Pages (from-to)233-234
Number of pages2
JournalCancer discovery
Issue number3
StatePublished - Mar 2016

ASJC Scopus subject areas

  • Oncology


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