Multivalent Effects of RGD Peptides Obtained by Nanoparticle Display Export

@article{citeulike:2371673, abstract = {Abstract: 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.}, address = {Department of Radiology, Geneva Hospital, Geneva, Switzerland, Department of Angiography and Interventional Radiology, Vienna Medical University, Vienna, Austria, and Center for Molecular Imaging Research, Massachusetts General Hospital and Harvard Medical School, Charlestown, Massachusetts}, author = {Montet, X. and Funovics, M. and Montet-Abou, K. and Weissleder, R. and Josephson, L.}, citeulike-article-id = {2371673}, citeulike-linkout-0 = {http://dx.doi.org/10.1021/jm060515m}, citeulike-linkout-1 = {http://pubs.acs.org/doi/abs/10.1021/jm060515m}, day = {5}, doi = {10.1021/jm060515m}, journal = {J. Med. Chem.}, keywords = {acid, alpha-nu-beta3-integrin, antiadhesion-assay, bt-20-tumor-cells, ccne-grant, crgd, crgd-clio-nanoparticle, cyclic-arginineglycineaspartic-acid, dextran-coated-aminated-clio, human-umbilical-vein-endothelial-cells, integrin, mit-mgh-ccne, rgd-peptide, superparamagnetic-iron-oxide-nanoparticle, uptake-assay}, month = {October}, number = {20}, pages = {6087--6093}, posted-at = {2008-02-13 21:53:45}, priority = {2}, title = {Multivalent Effects of RGD Peptides Obtained by Nanoparticle Display}, url = {http://dx.doi.org/10.1021/jm060515m}, volume = {49}, year = {2006} }

TY - JOUR ID - citeulike:2371673 L3 - citeulike-article-id:2371673 N2 - Abstract: 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. IS - 20 JF - J. Med. Chem. AD - Department of Radiology, Geneva Hospital, Geneva, Switzerland, Department of Angiography and Interventional Radiology, Vienna Medical University, Vienna, Austria, and Center for Molecular Imaging Research, Massachusetts General Hospital and Harvard Medical School, Charlestown, Massachusetts EP - 6093 TI - Multivalent Effects of RGD Peptides Obtained by Nanoparticle Display VL - 49 SP - 6087 KW - acid KW - alpha-nu-beta3-integrin KW - antiadhesion-assay KW - bt-20-tumor-cells KW - ccne-grant KW - crgd KW - crgd-clio-nanoparticle KW - cyclic-arginineglycineaspartic-acid KW - dextran-coated-aminated-clio KW - human-umbilical-vein-endothelial-cells KW - integrin KW - mit-mgh-ccne KW - rgd-peptide KW - superparamagnetic-iron-oxide-nanoparticle KW - uptake-assay AU - Montet, X AU - Funovics, M AU - Montet-Abou, K AU - Weissleder, R AU - Josephson, L PY - 2006/10/05/ UR - http://dx.doi.org/10.1021/jm060515m ER -