ANGIOGENESIS INHIBITION ACTIVITY OF A CYCLIC RGD-B-LACTAM PENTAPEPTIDE

摘要

Theαvβ3 integrin receptors play an important role in human tumor metastasis and growth. The inhibition of these receptors by antibodies or by cyclic peptides containing the Arg-Gly-Asp( RGD) sequence may be used as selectively treatment to suppress the disease. Our research group has previously described that the formal introduction of a single carbon atom to bridge the C~α (i) and N(i+1) contiguous residues of a linear or cyclic peptide leads to α-amino-β-lactam peptidomimetics containing predictably placed β-turn and γ-turn motifs, respectively. The combination of these results with the well-known capacity of RGD tripeptide for inhibition of the biological answer in integrin led us to the design of the following cyclic peptide.