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Selective Targeting of the KRAS G12C Mutant: Kicking KRAS When It's Down

G Aaron Hobbs1, Alfred Wittinghofer2, Channing J Der1

  • 1Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.

Cancer Cell
|March 16, 2016
PubMed

Insights

New research on KRAS G12C inhibitors suggests this mutant protein may not always be in its active state. These findings challenge the long-held assumption about its persistent GTP-bound form.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • KRAS mutations are common in cancer.
  • KRAS G12C is a specific mutation targeted by new drugs.
  • The active state of KRAS G12C has been assumed to be persistent.

Purpose of the Study:

  • To evaluate a novel small molecule inhibitor for KRAS G12C.
  • To investigate the conformational state of KRAS G12C in response to inhibition.

Main Methods:

  • Biochemical assays to assess KRAS G12C binding and inactivation.
  • Studies to determine the GTP-bound status of the mutant protein.

Main Results:

  • A small molecule inhibitor was found to bind and inactivate KRAS G12C.
  • Evidence suggests KRAS G12C may not be constitutively locked in its active GTP-bound form.

Conclusions:

  • The developed small molecule shows promise for targeting KRAS G12C.
  • Current understanding of KRAS G12C dynamics may need revision.

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