1. In Cellulo Generation of Fluorescent Probes for Live-Cell Imaging of Cylooxygenase-2.
- Author
-
Kaur J, Bhardwaj A, and Wuest F
- Subjects
- Azides, Cyclooxygenase 2, Diagnostic Imaging, Click Chemistry, Fluorescent Dyes chemistry
- Abstract
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 biomarker 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., (© 2020 Wiley-VCH GmbH.)
- Published
- 2021
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