Multivalent RGD synthetic peptides as potent αVβ3 integrin ligands

Elisabeth Garanger; Didier Boturyn; Jean-Luc Coll; Marie-Christine Favrot; Pascal Dumy

doi:10.1039/B517706E

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Multivalent RGD synthetic peptides as potent α_Vβ₃ integrin ligands†

Elisabeth Garanger,^ab Didier Boturyn,^a Jean-Luc Coll,^b Marie-Christine Favrot^b and Pascal Dumy*^a

Author affiliations

* Corresponding authors

^a Ingénierie Moléculaire et Chimie Bioorganique, LEDSS, CNRS UMR 5616, ICMG FR 2607, Université Joseph Fourier, BP 53, France
E-mail: Pascal.Dumy@ujf-grenoble.fr
Fax: (+33) 476-514-946
Tel: (+33) 476-635-545

^b Groupe de Recherche sur le Cancer du Poumon, INSERM U578, Institut Albert Bonniot IFR 73, Domaine de la Merci, France

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.

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Supplementary files

RP-HPLC chromatograms and ESI-MS spectra of purified peptides and conjugated compounds PDF (982K)

Article information

DOI: https://doi.org/10.1039/B517706E
Article type: Paper
Submitted: 13 Dec 2005
Accepted: 14 Feb 2006
First published: 03 Apr 2006

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Org. Biomol. Chem., 2006,4, 1958-1965

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Multivalent RGD synthetic peptides as potent α_Vβ₃ integrin ligands

E. Garanger, D. Boturyn, J. Coll, M. Favrot and P. Dumy, Org. Biomol. Chem., 2006, 4, 1958 DOI: 10.1039/B517706E

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Organic & Biomolecular Chemistry