Angiogenesis, the sprouting of new blood vessels from pre-existing vessels, is a remarkable feature of tumours growth and metastasis. The in vivo inhibition of this receptor by cyclic peptides containing RGD sequence may be used to selectively suppress these disease¹. Our research group has developed a new methodology² for the evaluation of new antiangiogenic compounds, based in the genetic expression analysis using CGH array system. The RGD mimetics activity can be modified by the presence of ester-bond³, Therefore, we decided to prepare some depsipeptides analogous to the RGD-β-lactam compounds and evaluate their activity performing a genetic expression analysis. We also have evaluated the activity of open-chain compounds without RGD formal structure. The cyclic depsipeptides have demonstrated a very effective inhibitory activity. In the other hand the open-chain compounds have a surprising behavior, demonstrating a similar gene activation. This way, we call into question the essential need of RGD sequence to have an interaction between ligand and the receptor of the integrin^{4, 5}.

1. da Ressurreicao, A. S. M.; Vidu, A.; Civera M.; Belvisi L.; Potenza, D.; Manzoni, L.; Ongeri, S.; Gennari, C.; Piarulli, U.; Eur. 2009, 15, 12184.
2. Aizpurua, J. M.; Ganboa, J. I.; Palomo, C.; Loinaz, I.; Oyarbide, J.; Fernandez, X.; Belentová, E.; Fratila, R. M.; Jiménez A.; Miranda, J. I.; Laso, A.; Ávila, S.; Castrillo, J. L.; ChemBioChem, 2001, 11, 401.
3. Cupido, T.; Spengler, J.; Ruiz-Rodriguez, J.; Adan, J.; Mitjans, F.; Puilats, J.; Albericio, F.; Chem. Int. Ed., 2010, 49, 2732.
4. Xiong, J. P.; Stehle, T.; Zhang, R.; Joachimiak, A.; Frech, M.; Goodman, S. L.; Arnaout, M. A.; Science, 2002, 296, 151.
5. Craig, D.; Gao, M.; Schulten, K.; Vogel, V.; Structure, 2004, 12, 2049.