Radiotracers for molecular imaging of cyclooxygenase-2 (COX-2) enzyme.
Cyclooxygenase (COX) enzyme is responsible for the formation of important biological mediators including prostaglandins, prostacyclin and thromboxane to trigger many physiological and patho-physiological responses. COXs exist in two distinct isoforms, a constitutively expressed form (COX-1) and an inducible form (COX-2). COX-2 is involved in the body's response to inflammation and pain. Moreover, it has also been shown that COX-2 is overexpressed in many human cancers, and that COX-2 is involved in various neurodegenerative diseases such as Parkinson's and Alzheimer's disease. COX-2 inhibitors are among the most widely used therapeutics for the treatment of chronic and acute pain and inflammation. Non-invasive monitoring of COX-2 functional expression by means of nuclear molecular imaging techniques like positron emission tomography (PET) and single photon emission computed tomography (SPECT) might provide unique opportunities to obtain data on COX-2 expression levels during disease manifestation and progression to study potential roles of COX-2 under various pathological conditions. The present review summarizes recent research efforts directed to the design and synthesis of radiotracers as molecular probes with special emphasis on COX-2 imaging.
Department of Oncology, University of Alberta, Edmonton, Alberta, T6G 1Z2, Canada. wuest@ualberta.ca.
O
O
Tietz
A
A
Marshall
M
M
Wuest
M
M
Wang
F
F
Wuest
D000818:Animals; D051546:Cyclooxygenase 2 / Q000032:analysis*; D006801:Humans; D009369:Neoplasms / Q000000981:diagnostic imaging*; D019636:Neurodegenerative Diseases / Q000000981:diagnostic imaging*; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D014018:Tissue Distribution
D019275:Radiopharmaceuticals; D051546:Cyclooxygenase 2