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Comparing dendritic and self-assembly strategies to multivalency-RGD peptide-integrin interactions

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JournalOrganic and Biomolecular Chemistry
DatePublished - 7 Jul 2011
Issue number13
Volume9
Number of pages7
Pages (from-to)4795-4801
Original languageEnglish

Abstract

This paper compares covalent and non-covalent approaches for the organisation of ligand arrays to bind integrins. In the covalent strategy, linear RGD peptides are conjugated to first and second generation dendrons, and using a fluorescence polarisation competition assay, the first generation compound is demonstrated to show the most effective integrin binding, with an EC50 of 125 mu M (375 mu M per peptide unit). As such, this dendritic compound is significantly more effective than a monovalent ligand, which does not bind integrin, even at concentrations as high as 1 mM. However, the second generation compound is significantly less effective, demonstrating that there is an optimum ligand density for multivalency in this case. In the non-covalent approach to multivalency, the same RGD peptide is functionalised with a hydrophobic C12 chain, giving rise to a lipopeptide which is demonstrated to be capable of self-assembly. This lipopeptide is capable of effective integrin binding at concentrations of 200 mu M. These results therefore demonstrate that covalent (dendritic) and non-covalent (micellar self-assembly) approaches have, in this case, comparable efficiency in terms of achieving multivalent organisation of a ligand array.

    Research areas

  • GENE DELIVERY, CELL-ADHESION, ALPHA(V)BETA(3) ANTAGONISTS, SUPRAMOLECULAR CHEMISTRY, BIOLOGICAL EVALUATION, SIGNAL-TRANSDUCTION, ENDOTHELIAL-CELLS, CASCADE POLYMERS, DRUG-DELIVERY, DNA-BINDING

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