Department of Oncology, University of Alberta, Edmonton, Alberta, T6G 1Z2, Canada.
Curr Med Chem. 2013;20(35):4350-69. doi: 10.2174/09298673113206660260.
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.
环氧化酶（COX）酶负责形成包括前列腺素、前列环素和血栓素在内的重要生物介质，从而引发许多生理和病理生理反应。COX 有两种不同的同工酶形式，一种是组成型表达形式（COX-1），另一种是诱导型形式（COX-2）。COX-2 参与了身体对炎症和疼痛的反应。此外，研究还表明，COX-2 在许多人类癌症中过度表达，并且 COX-2 参与了各种神经退行性疾病，如帕金森病和阿尔茨海默病。COX-2 抑制剂是治疗慢性和急性疼痛和炎症最广泛使用的治疗方法之一。通过正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT）等核分子成像技术对 COX-2 功能表达进行非侵入性监测，可能为在疾病表现和进展过程中获得 COX-2 表达水平的数据提供独特的机会，以研究 COX-2 在各种病理条件下的潜在作用。本综述总结了最近在设计和合成放射性示踪剂作为分子探针方面的研究进展，重点介绍了 COX-2 成像。
