Multivalent RGD synthetic peptides as potent αVβ3 integrin ligands

Abstract

We study herein the multivalency effect of a cluster of α_Vβ₃-ligands held on a cyclodecapeptide template. An array of RAFT(c[-RGDfK-])_n derivatives containing from one to sixteen clustered RGD motifs were synthesized and comparatively assayed in vitro on α_Vβ₃-expressing cells. Efficient inhibition of the α_Vβ₃-specific 23C6 monoclonal antibody fixation was observed with ligands displaying three and four copies of the cyclo[-RGDfK-] peptide.