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Issue 17, 2013
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Targeting of peptide conjugated magnetic nanoparticles to urokinase plasminogen activator receptor (uPAR) expressing cells

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Abstract

Ultrasmall superparamagnetic iron oxide (USPIO) nanoparticles are currently being used as a magnetic resonance imaging (MRI) contrast agent in vivo, mainly by their passive accumulation in tissues of interest. However, a higher specificity can ideally be achieved when the nanoparticles are targeted towards cell specific receptors and this may also facilitate specific drug delivery by an enhanced target-mediated endocytosis. We report efficient peptide-mediated targeting of magnetic nanoparticles to cells expressing the urokinase plasminogen activator receptor (uPAR), a surface biomarker for poor patient prognosis shared by several cancers including breast, colorectal, and gastric cancers. Conjugation of a uPAR specific targeting peptide onto polyethylene glycol (PEG) coated USPIO nanoparticles by click chemistry resulted in a five times higher uptake in vitro in a uPAR positive cell line compared to nanoparticles carrying a non-binding control peptide. In accordance with specific receptor-mediated recognition, a low uptake was observed in the presence of an excess of ATF, a natural ligand for uPAR. The uPAR specific magnetic nanoparticles can potentially provide a useful supplement for tumor patient management when combined with MRI and drug delivery.

Graphical abstract: Targeting of peptide conjugated magnetic nanoparticles to urokinase plasminogen activator receptor (uPAR) expressing cells

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Publication details

The article was received on 26 Sep 2012, accepted on 16 Jun 2013 and first published on 09 Jul 2013


Article type: Paper
DOI: 10.1039/C3NR32922D
Nanoscale, 2013,5, 8192-8201

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    Targeting of peptide conjugated magnetic nanoparticles to urokinase plasminogen activator receptor (uPAR) expressing cells

    L. Hansen, E. K. Unmack Larsen, E. H. Nielsen, F. Iversen, Z. Liu, K. Thomsen, M. Pedersen, T. Skrydstrup, N. Chr. Nielsen, M. Ploug and J. Kjems, Nanoscale, 2013, 5, 8192
    DOI: 10.1039/C3NR32922D

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