Integrin alpha V beta 3

Integrin alpha V beta 3, the vitronectin receptor, pairs CD51 with CD61 and is a hallmark of activated endothelium during angiogenesis. It binds RGD-containing ligands including vitronectin, fibrinogen, von Willebrand factor and osteopontin, and it is highly expressed on osteoclasts, where it is required for bone resorption. On tumor and angiogenic endothelial cells the receptor is strongly upregulated relative to quiescent vessels, making it one of the most exploited targets in vascular imaging: radiolabeled cyclic RGD peptides localize alpha V beta 3 for PET imaging of tumors. Therapeutically, cilengitide, a cyclic RGD peptidomimetic blocking alpha V beta 3 and alpha V beta 5, reached phase III trials in glioblastoma.