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Synthesis of RGD amphiphilic cyclic peptide as fibrinogen or fibronectin antagonist

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Abstract

This paper investigates the effect of the incorporation of adiazaethylene glycol derivative (Deg, 2) into a cyclic peptide containingthe tripeptide sequence Arg-Gly-Asp (RGD). This motif is a common structuralelement of many integrin ligands. The synthesis of cyclo-(Arg-Gly-Asp-Deg)(7) has been accomplished in solution using standard peptide chemistry. Theintent was to improve the bioavailability of this new RGD cyclic peptide,which is shown to interact with αIIbΒ3β3or α5 β1 receptors. A preliminary stepfor the conformational study of peptide 7 was done in DMSO-d6using nuclear magnetic resonance spectroscopy techniques.

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Authors and Affiliations

  1. Laboratoire des Aminoacides, Peptides et Protéines CNRS ESA 5075, Université de Montpellier II, F-34095, Montpellier Cedex, France

    Mamadou Amadou Sow, Frédéric Lamaty & René Lazaro

  2. Laboratoire Etude de l'Adhésion Cellulaire, CNRS UMR 5538, Institut Albert Bonniot, F-38706, La Tronche, France

    Annie Molla

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  1. Mamadou Amadou Sow
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  2. Annie Molla
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  3. Frédéric Lamaty
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  4. René Lazaro
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Sow, M.A., Molla, A., Lamaty, F. et al. Synthesis of RGD amphiphilic cyclic peptide as fibrinogen or fibronectin antagonist. Letters in Peptide Science 4, 455–461 (1997). https://doi.org/10.1023/A:1008844117525

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