A Selective and Oral Small Molecule Inhibitor of Vascular Epithelial Growth Factor Receptor (VEGFR)-2 and VEGFR-1 Inhibits Neovascularization and Vascular Permeability

  title={A Selective and Oral Small Molecule Inhibitor of Vascular Epithelial Growth Factor Receptor (VEGFR)-2 and VEGFR-1 Inhibits Neovascularization and Vascular Permeability},
  author={N. Patel and Li Sun and Deborah J Moshinsky and H. Chen and K. Leahy and Phuong Le and K. Moss and X. Wang and A. Rice and D. Tam and A. Laird and Xiaoming Yu and Q. Zhang and C. Tang and G. Mcmahon and A. Howlett},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={838 - 845}
  • N. Patel, Li Sun, +13 authors A. Howlett
  • Published 2003
  • Biology, Medicine
  • Journal of Pharmacology and Experimental Therapeutics
Vascular endothelial growth factor (VEGF) is a key driver of the neovascularization and vascular permeability that leads to the loss of visual acuity in diabetic retinopathy and neovascular age-related macular degeneration. Our aim was to identify an orally active, selective small molecule kinase inhibitor of vascular endothelial growth factor receptor (VEGFR)-2 with activity against both VEGF-induced angiogenesis and vascular permeability. We used a biochemical assay to identify 3-[5-methyl-2… Expand
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