Multivalent RGD synthetic peptides as potent alphaVbeta3 integrin ligands |
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Authors: | Garanger Elisabeth Boturyn Didier Coll Jean-Luc Favrot Marie-Christine Dumy Pascal |
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Affiliation: | Ingénierie Moléculaire et Chimie Bioorganique, LEDSS, CNRS UMR 5616, ICMG FR 2607, Université Joseph Fourier, BP 53, 38041 Grenoble Cedex 9, France. |
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Abstract: | 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. |
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