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Tietz O, Kamaly N, Smith G, et al. Design, synthesis and in vitro characterization of fluorescent and paramagnetic CXCR4-targeted imaging agents. Am J Nucl Med Mol Imaging. 2013;3(4):372-83
Tietz, O., Kamaly, N., Smith, G., Shamsaei, E., Bhakoo, K. K., Long, N. J., & Aboagye, E. O. (2013). Design, synthesis and in vitro characterization of fluorescent and paramagnetic CXCR4-targeted imaging agents. American journal of nuclear medicine and molecular imaging, 3(4), 372-83.
Tietz, Ole, et al. "Design, synthesis and in vitro characterization of fluorescent and paramagnetic CXCR4-targeted imaging agents." American journal of nuclear medicine and molecular imaging vol. 3,4 (2013): 372-83.
Tietz O, Kamaly N, Smith G, Shamsaei E, Bhakoo KK, Long NJ, Aboagye EO. Design, synthesis and in vitro characterization of fluorescent and paramagnetic CXCR4-targeted imaging agents. Am J Nucl Med Mol Imaging. 2013 Jul 10;3(4):372-83. Print 2013. PMID: 23901361; PMCID: PMC3715781.
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Am J Nucl Med Mol Imaging. 2013 Jul 10;3(4):372-83. Print 2013.

Design, synthesis and in vitro characterization of fluorescent and paramagnetic CXCR4-targeted imaging agents.

American journal of nuclear medicine and molecular imaging

Ole Tietz, Nazila Kamaly, Graham Smith, Elham Shamsaei, Kishore K Bhakoo, Nicholas J Long, Eric O Aboagye

Affiliations

  1. Department of Surgery and Cancer, Comprehensive Cancer Imaging Centre, Hammersmith Hospital, Imperial College London London, W12 0NN, UK.

PMID: 23901361 PMCID: PMC3715781

Abstract

The G-protein coupled C-X-C chemokine receptor type 4 (CXCR4) is highly overexpressed in a range of cancers and is therefore an excellent biomarker for cancer imaging. To this end targeted iron oxide nanoparticles were developed and utilised for in vitro imaging of MDA-MB-231 breast cancer cells overexpressing the CXCR4 receptor. Nanoparticles comprising an iron oxide core, encapsulated in a stabilising epichlorohydrin crossed-linked dextran polymer, were conjugated to a cyclopentapeptide with affinity to the CXCR4 receptor. The particles were characterized for their size, surface charge and r2 relaxivity at 4.7 T. MR imaging of the CXCR4 receptor with targeted iron oxide nanoparticles revealed an approximately 3-fold increase in T2 signal enhancement of MDA-MB-231 cells compared to non-targeted controls. Prussian blue staining of labeled MDA-MB-231 cells revealed darker and more intense staining of the cellular membrane. This study demonstrates the potential of targeted iron oxide nanoparticles for the imaging of the CXCR4 receptor by magnetic resonance imaging (MRI).

Keywords: CXCR4; T2 imaging; cyclopentapeptide; iron oxide nanoparticles; targeted nanoparticles; tumor MRI

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