Fluorine-18 Labelled Radioligands for PET Imaging of Cyclooxygenase-2 |
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| Authors: | Jatinder Kaur Atul Bhardwaj Frank Wuest |
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| Affiliation: | 1.Department of Oncology, University of Alberta, Edmonton, AB T6G 1Z2, Canada;2.Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, AB T6G 1Z2, Canada;3.Department of Chemistry, University of Alberta, Edmonton, AB T6G 1Z2, Canada |
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| Abstract: | Molecular imaging probes enable the early and accurate detection of disease-specific biomarkers and facilitate personalized treatment of many chronic diseases, including cancer. Among current clinically used functional imaging modalities, positron emission tomography (PET) plays a significant role in cancer detection and in monitoring the response to therapeutic interventions. Several preclinical and clinical studies have demonstrated the crucial involvement of cyclooxygenase-2 (COX-2) isozyme in cancer development and progression, making COX-2 a promising cancer biomarker. A variety of COX-2-targeting PET radioligands has been developed based on anti-inflammatory drugs and selective COX-2 inhibitors. However, many of those suffer from non-specific binding and insufficient metabolic stability. This article highlights examples of COX-2-targeting PET radioligands labelled with the short-lived positron emitter 18F, including radiosynthesis and PET imaging studies published in the last decade (2012–2021). |
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| Keywords: | COX-2 inhibitor radiotracer fluorine-18 radionuclide radiolabelling radioligands PET imaging and biomarker |
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