4.6 Article

In Cellulo Generation of Fluorescent Probes for Live-Cell Imaging of Cylooxygenase-2

Journal

CHEMISTRY-A EUROPEAN JOURNAL
Volume 27, Issue 10, Pages 3326-3337

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.202003315

Keywords

cancer; drug design; fluorescence; fluorogenic click chemistry; imaging agents; live cell imaging

Funding

  1. Dianne and Irving Kipnes Foundation
  2. Canadian Institute for Health Research (CIHR)
  3. National Science and Engineering Research Council of Canada (NSERC)
  4. 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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