Synthesis, analysis and biological evaluation of new RGD mimetics

The amino acid sequence L-arginyl-glycyl-L-aspartic acid (RGD) is a part of many extracellular proteins. It is a specific recognition site by integrins. Some synthetic RGD analogues bind specifically with integrin receptors on the cell membrane, which are over-expressed on the surface of various malignant human tumour and angiogenic endothelial cells. These peptides exert dual role by: inhibiting proliferation and migration of tumour cells and on the other hand by inhibiting angiogenesis. In recent years, many RGD cytotoxic agents have been developed, that showed promising results in vitro and in vivo. Herein we present the synthesis, analysis and biological evaluation of two new RGD analogues, modified in position 1 with Arg mimetics (Agb or Agp). Our pilot studies on their cytotoxicity were presented in comparison to parent RGD as standard.