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Description

An NRP-1-binding heptapeptide whose target was initially mistaken as VEGFR2/KDR/Flk-1 due to its binding activity to a CHO-KDR culture that was later shown to express primarily NRP-1 and little KDR. V1/A7R specifically competes against VEGF165 binding to recombinant NRP-1 in cell-free binding assays (IC50 = 60 µ,M), while exhibiting no activity against the interaction between NRP-1 and heparin or VEGF165 binding to KDR, VEGFR1/Flt-1, and heparin. V1/A7R is demonstrated to inhibit VEGF-dependent angiogenesis activity in HMVEC (IC50 = 0.3 µ,M) and HUVEC cultures in vitro, as well as in a rabbit corneal neovascularization model and in mice bearing MDA-MB-231-derived tumor in vivo.