title: Structure-driven design of radionuclide tracers for non-invasive imaging of uPAR and targeted radiotherapy. The tale of a synthetic peptide antagonist.
abstract: Research performed during the last two decades has provided a wealth of information to highlight the role of the urokinase-type plasminogen activator receptor (uPAR) in the progression and dissemination of invasive and metastatic cancer. In parallel, our perception of the structure-function relationships in uPAR has been refined to such a level that a rational design of uPAR function as well as compounds specifically targeting defined functions of uPAR are now realistic options. This knowledge opens new avenues for developing therapeutic intervention regimens targeting uPAR as well as for monitoring the effects of such treatments by non-invasive imaging using e.g. positron emission tomography. This mini-review will focus on recent advancements in translational research devoted to non-invasive targeting of uPAR, with a view to molecular imaging of its expression in live individuals as well as specific eradication of these cells by targeted radiotherapy.
authors.affiliation: Finsen Laboratory, Rigshospitalet & Biotech Research and Innovation Centre (BRIC), Copenhagen Biocenter, Ole Maaløes Vej 5, DK-2200 Copenhagen N, Denmark. m-ploug@finsenlab.dk
authors.forename: Michael
authors.initials: M
authors.lastname: Ploug
mesh_terms: D000818:Animals; D006801:Humans; D009369:Neoplasms / Q000000981:diagnostic imaging* / Q000235:genetics / Q000378:metabolism / Q000532:radiotherapy; D010455:Peptides / Q000737:chemistry* / Q000627:therapeutic use; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000737:chemistry* / Q000627:therapeutic use; D055293:Receptors, Urokinase Plasminogen Activator / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D014568:Urokinase-Type Plasminogen Activator / Q000737:chemistry / Q000378:metabolism
chemical_list: D010455:Peptides; D019275:Radiopharmaceuticals; D055293:Receptors, Urokinase Plasminogen Activator; D014568:Urokinase-Type Plasminogen Activator
keywords: CD87; PET imaging.; PLAUR; cancer; plasminogen activation; urokinase receptor