Theranostics 2013; 3(7):507-515. doi:10.7150/thno.5557


Urokinase Plasminogen Activator Receptor (uPAR) Targeted Nuclear Imaging and Radionuclide Therapy

Dan Li1, 2, Shuanglong Liu1, Hong Shan2, Peter Conti1, Zibo Li1 ✉

1. Molecular Imaging Center, University of Southern California, Los Angeles, CA 90033, USA.
2. Department of Radiology, the Third Affiliated Hospital of Sun Yat-sen University, Guangzhou 510630, China.

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Li D, Liu S, Shan H, Conti P, Li Z. Urokinase Plasminogen Activator Receptor (uPAR) Targeted Nuclear Imaging and Radionuclide Therapy. Theranostics 2013; 3(7):507-515. doi:10.7150/thno.5557. Available from

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Urokinase-type plasminogen activator receptor (uPAR) is a glycosylphosphatidylinositol (GPI)-anchored protein. Besides regulating proteolysis, uPAR could also activate many intracellular signaling pathways that promote cell motility, invasion, proliferation, and survival through cooperating with transmembrane receptors. uPAR is overexpressed across a variety of tumors and is associated with cancer invasion and metastasis. In order to meet the demand for a rapid development and potential clinical application of anti-cancer therapy based on uPA/uPAR system, it is desirable to develop non-invasive imaging methods to visualize and quantify uPAR expression in vivo. In this review, we will discuss recent advances in the development of uPAR-targeted nuclear imaging and radionuclide therapy agents. The successful development of molecular imaging probes to visualize uPAR expression in vivo would not only assist preclinical researches on uPAR function, but also eventually impact patient management.

Keywords: uPAR, PET, SPECT, radionuclide therapy.