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Updated: Dec 12, 2025

Bioorthogonal Chemical Imaging of Cell Metabolism Regulated by Aromatic Amino Acids
Published on: May 12, 2023
Bond-Breaking Bio-orthogonal Chemistry Efficiently Uncages Fluorescent and Therapeutic Compounds under Physiological
Xunshen Wu1, Kui Wu1, Fatima Gaye1
1Department of Chemistry, University at Albany,, 1400 Washington Avenue, Albany, New York 12222, United States.
Abstract:
Bond-breaking bio-orthogonal chemistry, consisting of a "click" reaction between trans-cyclooctene and tetrazine, followed by an intramolecular cyclization-driven uncaging step is described. The two-step process allows activation of caged compounds in biological media at neutral pH. The feasibility of this chemistry has been illustrated using NMR, while kinetics and pH-dependence were studied by fluorescence spectroscopy using caged coumarin. The practicality of the strategy is illustrated by activation of an anticancer drug, etoposide.
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