| Sequence | H-Cys-Thr-Thr-Gly-Pro-Cys-Cys-Arg-Gln-Cys-Lys-Leu-Lys-Pro-Ala-Gly-Thr-Thr-Cys-Trp-Lys-Thr-Ser-Leu-Thr-Ser-His-Tyr-Cys-Thr-Gly-Lys-Ser-Cys-Asp-Cys-Pro-Leu-Tyr-Pro-Gly-OH(Disulfide bridges: 1-10, 6-29, 7-34, 19-36) |
| Sequence Single | CTTGPCCRQCKLKPAGTTCWKTSLTSHYCTGKSCDCPLYPG(Disulfide bridges: 1-10, 6-29, 7-34, 19-36) |
| Molecular Formula | C184H284N52O57S8 |
| Molecular Weight | 4393.07 |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Description | Obtustatin is a highly potent integrin α1β1 inhibitor (IC50 = 0.8 nM for α1β1 binding to type IV collagen). Obtustatin is selective for α1β1 over α2β1, αIIbβ3, αvβ3, α4β1, α5β6, α9β1 and α4β7. Obtustatin inhibits FGF2-stimulated angiogenesis in the chicken chorioallantoic model. Obtustatin displays antitumor efficacy in a synergistic mouse model of Lewis lung carcinoma; Obtustatin blocks human melanoma growth in nude mice. |
| References | 1. 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 (2003). Protein Sci. 12 366 PMID: 12538900 2. Obtustatin: a potent and selective inhibitor of α1β1 integrin in vitro and angiogenesis in vivo. Marcinkiewicz et al (2003). Cancer Res. 63 2020 PMID: 12727812 3. Angiostatic activity of obtustatin as α1β1 integrin inhibitor in experimental melanoma growth. Brown et al (2008). Int.J.Cancer 123 2195 PMID: 18712720 |