App Note

KRAS GTP competitors and KRAS/SOS1 inhibitors screening with new HTRF biochemical-based assays

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Screening for KRAS competitors and inhibitors with HTRF® technology

KRAS is a proto-oncogene known to be mutated in many cancer subtypes, inducing uncontrolled proliferation and cell metabolism changes. Like most small GTPases, KRAS will bind to GDP in its inactive form or to GTP in its active form. KRAS G12C is one of the most commonly found mutant forms in cancers, and leads to a permanently active state of KRAS. The upregulation of KRAS interaction with the exchange factor SOS1 leads to cancer phenotypes. Reducing KRAS activity would allow the biological processes involved in cancer growth to be controlled.                                                            

This application note provides a relevant demonstration of the reliability of the new HTRF KRAS binding kit portfolio to:

  • Identify KRAS/SOS1 inhibitors in primary compound screens
  • Classify inhibitors that target only the KRAS G12C mutant
  • Discriminate GTP competitors from inhibitors which may spefically target the KRAS/SOS1 complex
  • Study the mechanisms of biochemical interactions

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