Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752

Proc Natl Acad Sci U S A. 2006 Feb 14;103(7):2316-21. doi: 10.1073/pnas.0508776103. Epub 2006 Feb 6.

Abstract

The success of molecular targeted therapy in cancer may depend on the selection of appropriate tumor types whose survival depends on the drug target, so-called "oncogene addiction." Preclinical approaches to defining drug-responsive subsets are needed if initial clinical trials are to be directed at the most susceptible patient population. Here, we show that gastric cancer cells with high-level stable chromosomal amplification of the growth factor receptor MET are extraordinarily susceptible to the selective inhibitor PHA-665752. Although MET activation has primarily been linked with tumor cell migration and invasiveness, the amplified wild-type MET in these cells is constitutively activated, and its continued signaling is required for cell survival. Treatment with PHA-665752 triggers massive apoptosis in 5 of 5 gastric cancer cell lines with MET amplification but in 0 of 12 without increased gene copy numbers (P = 0.00016). MET amplification may thus identify a subset of epithelial cancers that are uniquely sensitive to disruption of this pathway and define a patient group that is appropriate for clinical trials of targeted therapy using MET inhibitors.

Publication types

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

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Apoptosis
  • Biomarkers, Tumor / genetics
  • Cell Line, Tumor
  • Cell Movement
  • Drug Resistance, Neoplasm / genetics*
  • Gene Amplification*
  • Genetic Testing
  • Humans
  • Indoles / pharmacology*
  • Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Proto-Oncogene Proteins / genetics*
  • Proto-Oncogene Proteins c-met
  • Receptors, Growth Factor / genetics*
  • Stomach Neoplasms / enzymology
  • Stomach Neoplasms / genetics*
  • Sulfones / pharmacology*

Substances

  • 5-((2,6-dichlorobenzyl)sulfonyl)-3-((3,5-dimethyl-4-((2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl)carbonyl)-1H-pyrrol-2-yl)methylene)-1,3-dihydro-2H-indol-2-one
  • Antineoplastic Agents
  • Biomarkers, Tumor
  • Indoles
  • Proto-Oncogene Proteins
  • Receptors, Growth Factor
  • Sulfones
  • MET protein, human
  • Protein-Tyrosine Kinases
  • Proto-Oncogene Proteins c-met