| Autor: |
Md. Jashim Uddin, Justin Han-Je Lo, Connor G. Oltman, Brenda C. Crews, Tamanna Huda, Justin Liu, Philip J. Kingsley, Shuyang Lin, Mathew Milad, Ansari M. Aleem, Abu Asaduzzaman, J. Oliver McIntyre, Craig L. Duvall, Lawrence J. Marnett |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
ACS chemical biology. 17(7) |
| ISSN: |
1554-8937 |
| Popis: |
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. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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