Multivalent RGD synthetic peptides as potent alphaVbeta3 integrin ligands.
We study herein the multivalency effect of a cluster of alphaVbeta3-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 alphaVbeta3-expressing cells. Efficient inhibition of the alphaVbeta3-specific 23C6 monoclonal antibody fixation was observed with ligands displaying three and four copies of the cyclo[-RGDfK-] peptide.
Garanger
Elisabeth
E
Ingénierie Moléculaire et Chimie Bioorganique, LEDSS, CNRS UMR 5616, ICMG FR 2607, Université Joseph Fourier, BP 53, 38041 Grenoble Cedex 9, France.
Boturyn
Didier
D
Coll
Jean-Luc
JL
Favrot
Marie-Christine
MC
Dumy
Pascal
P