Obtustatin is a highly potent and selective inhibitor of the binding of α1β1 integrin to collagen IV, however, does not show inhibitory activity toward other integrins, including α2β1, αIIbβ3, αvβ3, α4β1, α5β1, α6β1, and α9β1, α4β7 integrins. It displays antitumor efficacy.

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SequenceOne Letter Code: CTTGPCCRQCKLKPAGTTCWKTSLTSHYCTGKSCDCPLYPG(Disulfide bridge: Cys1 and Cys10, Cys6 and Cys29, Cys7 and Cys34, Cys19 and Cys36)
Biological ActivityHighly potent integrin α1β1 inhibitor (IC50 = 0.8 nM for α1β1 binding to type IV collagen). Selective for α1β1 over α2β1, αIIbβ3, αvβ3, α4β1, α5β6, α9β1 and α4β7. Inhibits FGF2-stimulated angiogenesis in the chicken chorioallantoic model. Displays antitumor efficacy in a synergistic mouse model of Lewis lung carcinoma; blocks human melanoma growth in nude mice.
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