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

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Comparing dendritic and self-assembly strategies to multivalency-RGD peptide-integrin interactions. / Welsh, Daniel J.; Smith, David K.

In: Organic and Biomolecular Chemistry, Vol. 9, No. 13, 07.07.2011, p. 4795-4801.

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Harvard

Welsh, DJ & Smith, DK 2011, 'Comparing dendritic and self-assembly strategies to multivalency-RGD peptide-integrin interactions', Organic and Biomolecular Chemistry, vol. 9, no. 13, pp. 4795-4801. https://doi.org/10.1039/c1ob05241a

APA

Welsh, D. J., & Smith, D. K. (2011). Comparing dendritic and self-assembly strategies to multivalency-RGD peptide-integrin interactions. Organic and Biomolecular Chemistry, 9(13), 4795-4801. https://doi.org/10.1039/c1ob05241a

Vancouver

Welsh DJ, Smith DK. Comparing dendritic and self-assembly strategies to multivalency-RGD peptide-integrin interactions. Organic and Biomolecular Chemistry. 2011 Jul 7;9(13):4795-4801. https://doi.org/10.1039/c1ob05241a

Author

Welsh, Daniel J. ; Smith, David K. / Comparing dendritic and self-assembly strategies to multivalency-RGD peptide-integrin interactions. In: Organic and Biomolecular Chemistry. 2011 ; Vol. 9, No. 13. pp. 4795-4801.

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@article{a9b47bf6a68c4f7bba0039d548719e6f,
title = "Comparing dendritic and self-assembly strategies to multivalency-RGD peptide-integrin interactions",
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.",
keywords = "GENE DELIVERY, CELL-ADHESION, ALPHA(V)BETA(3) ANTAGONISTS, SUPRAMOLECULAR CHEMISTRY, BIOLOGICAL EVALUATION, SIGNAL-TRANSDUCTION, ENDOTHELIAL-CELLS, CASCADE POLYMERS, DRUG-DELIVERY, DNA-BINDING",
author = "Welsh, {Daniel J.} and Smith, {David K.}",
year = "2011",
month = jul,
day = "7",
doi = "10.1039/c1ob05241a",
language = "English",
volume = "9",
pages = "4795--4801",
journal = "Organic and Biomolecular Chemistry",
issn = "1477-0520",
publisher = "The Royal Society of Chemistry",
number = "13",

}

RIS (suitable for import to EndNote) - Download

TY - JOUR

T1 - Comparing dendritic and self-assembly strategies to multivalency-RGD peptide-integrin interactions

AU - Welsh, Daniel J.

AU - Smith, David K.

PY - 2011/7/7

Y1 - 2011/7/7

N2 - 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.

AB - 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.

KW - GENE DELIVERY

KW - CELL-ADHESION

KW - ALPHA(V)BETA(3) ANTAGONISTS

KW - SUPRAMOLECULAR CHEMISTRY

KW - BIOLOGICAL EVALUATION

KW - SIGNAL-TRANSDUCTION

KW - ENDOTHELIAL-CELLS

KW - CASCADE POLYMERS

KW - DRUG-DELIVERY

KW - DNA-BINDING

UR - http://www.scopus.com/inward/record.url?scp=79959795769&partnerID=8YFLogxK

U2 - 10.1039/c1ob05241a

DO - 10.1039/c1ob05241a

M3 - Article

VL - 9

SP - 4795

EP - 4801

JO - Organic and Biomolecular Chemistry

JF - Organic and Biomolecular Chemistry

SN - 1477-0520

IS - 13

ER -