Obtustatin

Obtustatin Property

form 

Solid

color 

White to off-white

Sequence

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 (Disulfide bridge: Cys1-Cys10, Cys6-Cys29, Cys7-Cys34, Cys19-Cys36)

Hazard and Precautionary Statements (GHS)

Obtustatin Chemical Properties,Usage,Production

Uses

Obtustatin is a non-RGD disintegrin of 41 residues. Obtustatin can be isolated from Vipera lebetina obtusa venom. Obtustatin is a potent and selective inhibitor of the adhesion of integrin α1β1 to collagen IV. Obtustatin inhibits angiogenesis, and can be used for research of cancer[1][2].

Enzyme inhibitor

This 41-residue disintegrin (FW = 4401 g/mol; Sequence CTTGPCCRQ CKLKPAGTTCWKTSLTSHYCTGKSCDCPLYPG, with disulfide bonds at Cys1-Cys10, Cys6-Cys29, Cys7-Cys34, and Cys19-Cys36) from the venom of the blunt-nosed viper Vipera lebetina obtusa exhibits tight binding to integrins, inhibiting platelet aggregation, IC50 = 2 nM. It is the shortest polypeptide to contain an integrin-recognition loop. Target(s): Obtustatin is a highly potent integrin α1β1 inhibitor (IC50 = 0.8 nM for α1β1 binding to type IV collagen), displaying specificity for α1β1 over α2β1, αIIbβ3, αvβ3, α4β1, α5β6, α9β1 and α4β7.

References

[1] Paz Moreno-Murciano M, et al. NMR solution structure of the non-RGD disintegrin obtustatin. J Mol Biol. 2003 May 23;329(1):135-45. DOI:10.1016/s0022-2836(03)00371-1
[2] Marcinkiewicz C, et al. Obtustatin: a potent selective inhibitor of alpha1beta1 integrin in vitro and angiogenesis in vivo. Cancer Res. 2003 May 1;63(9):2020-3. PMID:12727812