Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 27, Issue 10, Pages 3326-3337Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.202003315
Keywords
cancer; drug design; fluorescence; fluorogenic click chemistry; imaging agents; live cell imaging
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Funding
- Dianne and Irving Kipnes Foundation
- Canadian Institute for Health Research (CIHR)
- National Science and Engineering Research Council of Canada (NSERC)
- Alberta Cancer Foundation (ACF)
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The study introduces a new chemical toolbox for precise visualization and tracking of COX-2 in live cells with superior sensitivity in the visible range. By in cellulo assembly of fluorescent probes, COX-2 imaging was successfully achieved and protein-ligand interactions were investigated.
Live-cell imaging with fluorescent probes is an essential tool in chemical biology to visualize the dynamics of biological processes in real-time. Intracellular disease bio-marker imaging remains a formidable challenge due to the intrinsic limitations of conventional fluorescent probes and the complex nature of cells. This work reports the in cellulo assembly of a fluorescent probe to image cyclooxygenase-2 (COX-2). We developed celecoxib-azide derivative 14, possessing favorable biophysical properties and excellent COX-2 selectivity profile. In cellulo strain-promoted fluorogenic click chemistry of COX-2- engaged compound 14 with non/weakly-fluorescent compounds 11 and 17 formed fluorescent probes 15 and 18 for the detection of COX-2 in living cells. Competitive binding studies, biophysical, and comprehensive computational analyses were used to describe protein-ligand interactions. The reported new chemical toolbox enables precise visualization and tracking of COX-2 in live cells with superior sensitivity in the visible range.
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