Targeting wild-type KRAS-amplified gastroesophageal cancer through combined MEK and SHP2 inhibition

Nat Med. 2018 Jul;24(7):968-977. doi: 10.1038/s41591-018-0022-x. Epub 2018 May 28.

Abstract

The role of KRAS, when activated through canonical mutations, has been well established in cancer1. Here we explore a secondary means of KRAS activation in cancer: focal high-level amplification of the KRAS gene in the absence of coding mutations. These amplifications occur most commonly in esophageal, gastric and ovarian adenocarcinomas2-4. KRAS-amplified gastric cancer models show marked overexpression of the KRAS protein and are insensitive to MAPK blockade owing to their capacity to adaptively respond by rapidly increasing KRAS-GTP levels. Here we demonstrate that inhibition of the guanine-exchange factors SOS1 and SOS2 or the protein tyrosine phosphatase SHP2 can attenuate this adaptive process and that targeting these factors, both genetically and pharmacologically, can enhance the sensitivity of KRAS-amplified models to MEK inhibition in both in vitro and in vivo settings. These data demonstrate the relevance of copy-number amplification as a mechanism of KRAS activation, and uncover the therapeutic potential for targeting of these tumors through combined SHP2 and MEK inhibition.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Disease Models, Animal
  • Esophageal Neoplasms / genetics*
  • Esophageal Neoplasms / pathology
  • Gene Amplification*
  • Humans
  • Mice
  • Mitogen-Activated Protein Kinase Kinases / antagonists & inhibitors*
  • Mitogen-Activated Protein Kinase Kinases / metabolism
  • Piperidines / pharmacology
  • Protein Kinase Inhibitors / pharmacology
  • Protein Tyrosine Phosphatase, Non-Receptor Type 11 / antagonists & inhibitors*
  • Protein Tyrosine Phosphatase, Non-Receptor Type 11 / metabolism
  • Proto-Oncogene Proteins p21(ras) / genetics*
  • Pyridones / pharmacology
  • Pyrimidines / pharmacology
  • Pyrimidinones / pharmacology
  • Stomach Neoplasms / genetics*
  • Stomach Neoplasms / pathology

Substances

  • KRAS protein, human
  • Piperidines
  • Protein Kinase Inhibitors
  • Pyridones
  • Pyrimidines
  • Pyrimidinones
  • SHP099
  • trametinib
  • Mitogen-Activated Protein Kinase Kinases
  • Protein Tyrosine Phosphatase, Non-Receptor Type 11
  • Proto-Oncogene Proteins p21(ras)