RAM, an RGDS Analog, Exerts Potent Anti-Melanoma Effects In Vitro and In Vivo

摘要: Peptides containing the RGD sequence are under continuous investigation given their ability to control cell adhesion and apoptosis. Since small peptides quickly metabolized degraded in vivo, developing analogs resistant serum-induced degradation is a challenging task. developed so far known as molecules mostly inhibiting adhesion; this feature may reduce proliferation tumor development but not induce regression of tumors or metastases already formed. In current study, carried out melanoma vitro vivo models, we show that RAM, an RGD-non-peptide Analog-Molecule, strongly inhibits cells onto plastic, vitronectin, fibronectin, laminin von Willebrand Factor while it does inhibit collagen IV, similarly RGDS template peptide. It also proliferation, migration DNA-synthesis, increases apoptosis reduces survivin expression. All such effects were observed IV seeded cells, therefore most likely independent from anti adhesive properties. Further, RAM more stable than RGDS; fact maintains its anti-proliferation anti-adhesion after long serum exposure almost completely loses upon exposure. mouse metastatic model, increasing doses significantly up about 80% lung development, comparable less potent. conclusion these data potent inhibitor growth vitro, represents novel candidate for further investigations cancer treatment field.