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Multivalent Effects of RGD Peptides Obtained by Nanoparticle Display

Montet, Xavier ; Funovics, Martin ; Montet-Abou, Karin ; Weissleder, Ralph ; Josephson, Lee

Journal of medicinal chemistry, 2006-10, Vol.49 (20), p.6087-6093 [Periódico revisado por pares]

Washington, DC: American Chemical Society

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Título:
Multivalent Effects of RGD Peptides Obtained by Nanoparticle Display
Autor: Montet, Xavier ; Funovics, Martin ; Montet-Abou, Karin ; Weissleder, Ralph ; Josephson, Lee
Assuntos: Animals ; Biological and medical sciences ; Cell Adhesion ; Cell Line, Tumor ; Endothelial Cells - metabolism ; Endothelium, Vascular - cytology ; Half-Life ; Humans ; In Vitro Techniques ; Integrin alphaVbeta3 - metabolism ; Investigative techniques, diagnostic techniques (general aspects) ; Medical sciences ; Mice ; Mice, Nude ; Miscellaneous ; Miscellaneous. Technology ; Nanostructures ; Oligopeptides - blood ; Oligopeptides - chemistry ; Oligopeptides - metabolism ; Pathology. Cytology. Biochemistry. Spectrometry. Miscellaneous investigative techniques ; Pharmacology. Drug treatments ; Protein Binding ; Protein Conformation
É parte de: Journal of medicinal chemistry, 2006-10, Vol.49 (20), p.6087-6093
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Descrição: The binding of RGD peptides to integrins offers an excellent system to study the multivalent mediated changes in affinity that arise when peptides, displayed on the surface of a nanoparticle carrier, bind to integrins displayed on the cell membrane. The IC50 of an RGD nanoparticle for endothelial adhesion was 1.0 nM nanoparticle or 20 nM peptide (20 peptide/nanoparticle) and was associated with strong multivalent effects, defined as a multivalent enhancement factor (MVE) of 38 (MVE = IC50 (peptide)/IC50 (peptide when displayed by nanoparticle)). The attachment of RGD peptides to nanoparticles resulted in an extension of the peptide blood half-life from 13 to 180 min. Based on the multivalent enhancement of affinity and extension of blood half-life, multivalent RGD nanoparticle-sized materials should be potent inhibitors of the alpha(V)beta(3) function on endothelial cells in vivo.
Editor: Washington, DC: American Chemical Society
Idioma: Inglês

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Multivalent Effects of RGD Peptides Obtained by Nanoparticle Display

Montet, Xavier ; Funovics, Martin ; Montet-Abou, Karin ; Weissleder, Ralph ; Josephson, Lee

Washington, DC: American Chemical Society

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