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 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ 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.

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.

References:
[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.