2. Academic Validation
  3. Flk-1 as a target for tumor growth inhibition

Flk-1 as a target for tumor growth inhibition

  • Cancer Res. 1996 Aug 1;56(15):3540-5.
L M Strawn 1,  G McMahon,  H App,  R Schreck,  W R Kuchler,  M P Longhi,  T H Hui,  C Tang,  A Levitzki,  A Gazit,  I Chen,  G Keri,  L Orfi,  W Risau,  I Flamme,  A Ullrich,  K P Hirth,  L K Shawver
Affiliations

Affiliation

  • 1 SUGEN, Inc., Redwood City, California 94063, USA.
PMID: 8758924
Abstract

A number of growth factor Receptor Tyrosine Kinases have been implicated in angiogenesis, including epidermal growth factor receptor, Fibroblast Growth Factor receptor, platelet-derived growth factor receptor, VEGFR2/KDR/Flk-1/VEGFR2/KDR/Flk-1, Flt-1, TIE-1, and Tek/TIE-2. VEGFR2/KDR/Flk-1/VEGFR2/KDR/Flk-1, a receptor for vascular endothelial growth factor (VEGF), is expressed exclusively in endothelial cells. Using dominant-negative methods, VEGFR2/KDR/Flk-1 was shown to play a role in angiogenesis and the growth of a variety of tumor types. Because of this, a drug discovery effort was established to identify VEGFR2/KDR/Flk-1 kinase inhibitors. For initial screening, an ELISA in, a 96-well format was used to measure VEGF-induced VEGFR2/KDR/Flk-1 tyrosine phosphorylation in whole cells. Compounds that inhibited ligand-induced receptor autophosphorylation were confirmed by antiphosphotyrosine immunoblotting. Inhibition of VEGF-stimulated DNA synthesis in human endothelial cells was also assessed. Inhibitors were further evaluated for their effects on vessel formation using the chorioallantoic membrane assay. Using these methods, antiangiogenesis compounds that inhibit VEGFR2/KDR/Flk-1 tyrosine kinase activity, endothelial cell mitogenesis, and blood vessel formation in the chorioallantoic membrane assay have been found.

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