Vascular endothelial growth factor receptor-3 activity is modulated by its association with caveolin-1 on endothelial membrane

Biochemistry. 2007 Apr 3;46(13):3998-4005. doi: 10.1021/bi061400n. Epub 2007 Mar 10.

Abstract

Vascular endothelial growth factor receptor-3 (VEGFR-3) is constitutively expressed in lymphatic vessels and transiently in endothelial cells of blood vessels during angiogenesis. Here we report that VEGFR-3 localizes in the caveolae membrane of endothelial cells and co-immunoprecipitates with caveolin-1. Caveolin-1 silencing or its depletion from the cell membrane by cholesterol increases VEGFR-3 autophosphorylation, suggesting that caveolin acts as a negative regulator of VEGFR-3 activity. Receptor activation induces caveolin-1 phosphorylation on tyrosine residues including tyrosine 14. Cell treatment with Src or Abl inhibitors PP2 or STI571, prior to receptor stimulation, affects caveolin-1 phosphorylation without affecting receptor autophosphorylation, suggesting that both Src and Abl are involved in VEGFR-3-dependent caveolin-1 phosphorylation. Caveolin-1 phosphorylation in Src/Fyn/Yes knockout cells demonstrated that Abl phosphorylates caveolin-1 independently from Src family members. These results suggest a functional interaction between VEGFR-3 and caveolin-1 to modulate endothelial cell activation during angiogenesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzamides
  • Caveolae / chemistry
  • Caveolin 1 / metabolism*
  • Cell Membrane / physiology
  • Clone Cells
  • Endothelium, Vascular / cytology*
  • Humans
  • Imatinib Mesylate
  • Lymphoid Tissue / chemistry
  • Mice
  • Phosphorylation
  • Piperazines / pharmacology
  • Proto-Oncogene Proteins c-abl / physiology
  • Proto-Oncogene Proteins pp60(c-src) / physiology
  • Pyrimidines / pharmacology
  • Sus scrofa
  • Vascular Endothelial Growth Factor Receptor-3 / drug effects*
  • Vascular Endothelial Growth Factor Receptor-3 / metabolism*

Substances

  • AG 1879
  • Benzamides
  • Caveolin 1
  • Piperazines
  • Pyrimidines
  • Imatinib Mesylate
  • Vascular Endothelial Growth Factor Receptor-3
  • Proto-Oncogene Proteins c-abl
  • Proto-Oncogene Proteins pp60(c-src)