Biological ActivityObtustatin is a highly 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.
(Modifications: Disulfide bridges: 1-10, 6-29, 7-34, 19-36)
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Amino acid sequence and homology modeling of obtustatin, a novel non-RGD-containing short disintegrin isolated from the venom of Vipera lebetina obtusa.
Moreno-Murciano et al.
Protein Sci., 2003;12:366
Obtustatin: a potent and selective inhibitor of α1β1 integrin in vitro and angiogenesis in vivo.
Marcinkiewicz et al.
Cancer Res., 2003;63:2020
Angiostatic activity of obtustatin as α1β1 integrin inhibitor in experimental melanoma growth.
Brown et al.
Citations for Obtustatin
The citations listed below are publications that use Tocris products. Selected citations for Obtustatin include:
2 Citations: Showing 1 - 2
Collagen Type 1 accelerates healing of ruptured fetal membranes.
Sci Rep 2018;8(1):696
Reciprocal signalling by Notch-Collagen V-CALCR retains muscle stem cells in their niche
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10 μg/ml treat 24h and 48h