Angiostatin is known to bind many proteins, especially to angiomotin and endothelial cell surface ATP synthase but also integrins, annexin II, C-met receptor, NG2 proteoglycan, tissue-type plasminogen activator, chondroitin sulfate proteoglycans, and CD26. Additionally, smaller fragments of angiostatin may bind several other proteins. There is still considerable uncertainty on its mechanism of action, but it seems to involve inhibition of endothelial cell migration,proliferation and induction of apoptosis. It has been proposed that angiostatin activity is related, among other things, to the coupling of its mechanical and redox properties.
^O'Reilly MS, Holmgren L, Shing Y et al. (October 1994). "Angiostatin: a novel angiogenesis inhibitor that mediates the suppression of metastases by a Lewis lung carcinoma". Cell79 (2): 315–28. doi:10.1016/0092-8674(94)90200-3. PMID7525077.
^Redlitz A, Daum G, Sage EH (1999). "Angiostatin diminishes activation of the mitogen-activated protein kinases ERK-1 and ERK-2 in human dermal microvascular endothelial cells". Journal of Vascular Research36 (1): 28–34. doi:10.1159/000025623. PMID10050071.
^Grandi F, Sandal M, Guarguaglini G, Capriotti E, Casadio R, Samorì B (November 2006). "Hierarchical mechanochemical switches in angiostatin". Chembiochem : a European Journal of Chemical Biology7 (11): 1774–82. doi:10.1002/cbic.200600227. PMID16991168.