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Aim: αvβ3 integrin has been reported as a promising therapeutic target for angiogenesis.Numerous αvβ3 antagonists have been developed, one of which, cilengitide, is in Phase Ⅱ clinical trials.In the present study, we tested the antiangiogenic activity of 3-[3-(6-guanidino-1-oxoisoindolin-2-yl)propanamido]-3-(pyridin-3-yl)propanoic acid dihydrochloride (GOPPP), a novel non-peptide αvβ3 antagonist.