Coupling of mutated Met variants to DNA repair via Abl and Rad51

Cancer Res. 2008 Jul 15;68(14):5769-77. doi: 10.1158/0008-5472.CAN-08-1269.

Abstract

Abnormal activation of DNA repair pathways by deregulated signaling of receptor tyrosine kinase systems is a compelling likelihood with significant implications in both cancer biology and treatment. Here, we show that due to a potential substrate switch, mutated variants of the receptor for hepatocyte growth factor Met, but not the wild-type form of the receptor, directly couple to the Abl tyrosine kinase and the Rad51 recombinase, two key signaling elements of homologous recombination-based DNA repair. Treatment of cells that express the mutated receptor variants with the Met inhibitor SU11274 leads, in a mutant-dependent manner, to a reduction of tyrosine phosphorylated levels of Abl and Rad51, impairs radiation-induced nuclear translocation of Rad51, and acts as a radiosensitizer together with the p53 inhibitor pifithrin-alpha by increasing cellular double-strand DNA break levels following exposure to ionizing radiation. Finally, we propose that in order to overcome a mutation-dependent resistance to SU11274, this aberrant molecular axis may alternatively be targeted with the Abl inhibitor, nilotinib.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Active Transport, Cell Nucleus
  • Animals
  • Benzothiazoles / metabolism
  • DNA Damage
  • DNA Repair*
  • Genes, abl*
  • Genetic Variation*
  • Indoles / pharmacology
  • Mice
  • Mutation*
  • NIH 3T3 Cells
  • Phosphorylation
  • Piperazines / pharmacology
  • Rad51 Recombinase / genetics*
  • Rad51 Recombinase / physiology
  • Radiation-Sensitizing Agents / pharmacology
  • Sulfonamides / pharmacology
  • Toluene / analogs & derivatives
  • Toluene / metabolism
  • Tyrosine / chemistry

Substances

  • ((3Z)-N-(3-chlorophenyl)-3-((3,5-dimethyl-4-((4-methylpiperazin-1-yl)carbonyl)-1H-pyrrol-2-yl)methylene)-N-methyl-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide)
  • Benzothiazoles
  • Indoles
  • Piperazines
  • Radiation-Sensitizing Agents
  • Sulfonamides
  • Toluene
  • Tyrosine
  • pifithrin
  • Rad51 Recombinase