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Beschreibung

A macrocyclic 17-amino acid peptide derived from residues 79 - 93 of vascular endothelial growth factor that mediate its binding to VEGFR-2. It blocks the binding of VEGF165 to its receptors (IC50 = 700 nM for VEGFR1, 1.3 µ,M for VEGFR2) and exhibits anti-angiogenic activity as well as other VEGFR-mediated cellular functions, such as proliferation (IC50 = 5.8 µ,M), migration (IC50 = 8.2 µ,M), and activation of MAP kinases. Its anti-angiogenic activity has been successfully demonstrated in vivo using chick embryos and nude mice tumor models of human intracranial and syngeneic glioma., A macrocyclic, 17-amino acid peptide derived from residues 79-93 of vascular endothelial growth factor (VEGF) that mediates the binding of VEGF to its receptor, VEGFR-2. Blocks the binding of VEGF165 to its receptors (IC50 = 70 nM for VEGFR-1, 1.3 µ,M for VEGFR-2) and exhibits anti-angiogenic properties. Also reported to block other VEGF-mediated cellular functions such as proliferation (IC50 = 5.8 µ,M), migration (IC50 = 8.2 µ,M), and activation of MAP kinases. Also reported to exhibit anti-angiogenic properties in vivo using chick embryo and nude mouse tumor models of human intracranial and syngeneic glioma.