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Radiolabeled COX-2 Inhibitors for Non-Invasive Visualization of COX-2 Expression and Activity — A Critical Update

1
Department Radiopharmaceutical and Chemical Biology, Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf, Bautzner Landstrasse 400, 01328 Dresden, Germany
2
Department of Chemistry and Food Chemistry, Technische Universität Dresden, 01062 Dresden, Germany
*
Author to whom correspondence should be addressed.
Molecules 2013, 18(6), 6311-6355; https://doi.org/10.3390/molecules18066311
Received: 29 March 2013 / Revised: 16 May 2013 / Accepted: 24 May 2013 / Published: 29 May 2013
(This article belongs to the Special Issue PET Chemistry in Molecular Imaging)
Cyclooxygenase-2 (COX-2) is a key player in inflammation. Its overexpression is directly associated with various inflammatory diseases and, additionally, with several processes of carcinogenesis. The development of new selective COX-2 inhibitors (COXIBs) for use in cancer treatment is in the focus of the medicinal chemistry research field. For this purpose, a set of methods is available to determine COX-2 expression and activity in vitro and ex vivo but it is still a problem to functionally characterize COX-2 in vivo. This review focusses on imaging agents targeting COX-2 which have been developed for positron emission tomography (PET) and single photon emission computed tomography (SPECT) since 2005. The literature reveals that different radiochemical methods are available to synthesize COXIBs radiolabeled with fluorine-18, carbon-11, and isotopes of radioiodine. Unfortunately, most of the compounds tested did not show sufficient stability in vivo due to de[18F]fluorination or de[11C]methylation or they failed to bind specifically in the target region. So, suitable stability in vivo, matching lipophilicity for the target compartment and both high affinity and selectivity for COX-2 were identified as prominent criteria for radiotracer development. Up to now, it is not clear what approach and which model is the most suited to evaluate COX-2 targeting imaging agents in vivo. However, for proof of principle it has been shown that some radiolabeled compounds can bind specifically in COX-2 overexpressing tissue which gives hope for future work in this field. View Full-Text
Keywords: cyclooxygenase; inhibitor; imaging; visualization; radionuclide; fluorine-18; carbon-11; radioiodine; COXIB; NSAID cyclooxygenase; inhibitor; imaging; visualization; radionuclide; fluorine-18; carbon-11; radioiodine; COXIB; NSAID
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Laube, M.; Kniess, T.; Pietzsch, J. Radiolabeled COX-2 Inhibitors for Non-Invasive Visualization of COX-2 Expression and Activity — A Critical Update. Molecules 2013, 18, 6311-6355.

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