首页|Discovery of a Redox-Activatable Chemical Probe for Detection of Cyclooxygenase-2 in Cells and Animals
Discovery of a Redox-Activatable Chemical Probe for Detection of Cyclooxygenase-2 in Cells and Animals
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NSTL
Amer Chemical Soc
Cyclooxygenase-2 (COX-2) expression is up -regulated in inflammatory tissues and many premalignant and malignant tumors. Assessment of COX-2 protein in vivo, therefore, promises to be a powerful strategy to distinguish pathologic cells from normal cells in a complex disease setting. Herein, we report the first redox-activatable COX-2 probe, fluorocoxib Q (FQ), for in vivo molecular imaging of pathogenesis. FQ inhibits COX-2 selectively in purified enzyme and cell-based assays. FQ exhibits extremely low fluorescence and displays time-and concentration-dependent fluorescence enhancement upon exposure to a redox environment. FQ enters the cells freely and binds to the COX-2 enzyme. FQ exhibits high circulation half-life and metabolic stability sufficient for target site accumulation and demonstrates COX-2-targeted uptake and retention in cancer cells and pathologic tissues. Once taken up, it undergoes redox-mediated transformation into a fluorescent compound fluorocoxib Q-H that results in high signal-to-noise contrast and differentiates pathologic tissues from non-pathologic tissues for real-time in vivo imaging.
Uddin, Md. Jashim、Lo, Justin Han-Je、Oltman, Connor G.、Crews, Brenda C.、Huda, Tamanna、Liu, Justin、Kingsley, Philip J.、Lin, Shuyang、Milad, Mathew、Aleem, Ansari M.、Asaduzzaman, Abu、McIntyre, J. Oliver、Duvall, Craig L.、Marnett, Lawrence J.
NSTL
Amer Chemical Soc
