Abstract
IPS-05002, a novel antagonist of integrin a5β1, was screened from a phytochemical compound library using ProteoChip-based integrin a5β1-fibronectin interaction assay method. The novel compound inhibited VEGF-stimulated human umbilical vein endothelial cell (HUVEC) proliferation, adhesion, and migration in a dose-dependent manner. It also suppressed tubular network formation. Differential expression profiling of cell cycle proteins in VEGF-induced HUVECs in the presence of IPS-05002 showed up-regulation of IKB-β, XRCC4, and down-regulation of Cdc6 compared with HUVECs induced by VEGF alone. In conclusion, these data suggest that IPS-05002 will be a potent inhibitor for VEGF-mediated angiogenesis.
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