Stereoisomerism and Biological Activity of the Selective and Superactive α_vβ_3 Integrin Inhibitor cyclo(-RGDfV-) and Its Retro-Inverso Peptide

摘要

The cyclic pentapeptide cyclo(-Arg-Gly-Asp-D-Phe-Val-) is a highly potent and selective inhibitor for the α_vβ_3 integrin and is a prospective anticancer drug by acting to inhibit angiogenesis and by inducing apoptosis in vascular cells. The cyclic retro-inverso peptides as well as the inverso and the cyclic retro peptide analogs of the four cyclic Arg-Gly-Asp-D-Phe-Val peptides with one amino acid in the D configuration and the corresponding all-L peptide have been synthesized.