RGD(Arg-Gly-Asp)肽是一种三肽,可有效触发细胞粘附、定位某些细胞系并引发特定的细胞反应;与整合素结合。
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Synthetic peptides containing the arginine-glycine-aspartate (RGD) were extensively used as inhibitors of integrin-ligand interactions in studies of cell adhesion, migration, growth and differentiation, since the RGD motif is an integrin-recognition motif found in many ligands.
In vitro: RGD peptide can induce apoptosis in the absence of signals and integrin-mediated cell clustering. Previous study demonstrates that RGD peptides promote apoptosis through activation of conformation changes enhancing pro-caspase-3 activation and autoprocessing [1].
In vivo: Anima study suggested that the RGD-4C-FITC-peptide bound to both endothelial and tumor cells in vivo and that peptide targeting should allow the delivery of therapeutic drugs to both endothelial and tumor cells [2].
Clinical trials: Currenlty no clinical data are available.
参考文献:
[1] Nature.? 1999 Feb 11;397(6719):534-9.
RGD peptides induce apoptosis by direct caspase-3 activation.?
Buckley CD1, Pilling D, Henriquez NV, Parsonage G, Threlfall K, Scheel-Toellner D, Simmons DL, Akbar AN, Lord JM, Salmon M.?
[2] Cancer Res.? 2002 Sep 15;62(18):5139-43. Arginine-glycine-aspartic acid (RGD)-peptide binds to both tumor and tumor-endothelial cells in vivo.? Zitzmann S1, Ehemann V, Schwab M.??
Cell experiment [1]: | |
Cell lines |
Lung fibroblasts |
Preparation method |
The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
Reacting condition |
1 mM; 24 hrs |
Applications |
In lung fibroblasts, RGD peptides induced apoptosis and caspase-3 activation. Moreover, in both adherent and detached cells, RGD peptides resulted in pro-caspase-3 cleavage. Thus, RGD-containing peptides can induce apoptosis before the adherent cells detach from their substrates. |
参考文献: [1]. Buckley CD, Pilling D, Henriquez NV, Parsonage G, Threlfall K, Scheel-Toellner D, Simmons DL, Akbar AN, Lord JM, Salmon M. RGD peptides induce apoptosis by direct caspase-3 activation. Nature. 1999 Feb 11;397(6719):534-9. |
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