Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 20, Pages 6087-6093Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm060515m
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Funding
- NCI NIH HHS [P50 CA86355, R24 CA92782] Funding Source: Medline
- NIBIB NIH HHS [R01 EB00662] Funding Source: Medline
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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.
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