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Fast and Sensitive Pretargeted Labeling of Cancer Cells through a Tetrazine/trans-Cyclooctene Cycloaddition


  • We thank Dr. Ned Keliher for helpful advice. This research was supported in part by NIH grants U01-HL080731 and T32-CA79443.


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A label for six, please! A fluorescent tetrazine derivative was used to image trans-cyclooctene-modified affinity ligands on live cancer cells through a bioorthogonal cycloaddition with a reaction rate of approximately 6000±200 M−1 s−1 in serum at 37 °C (see scheme). To maximize the fluorescence signal, up to six trans-cyclooctene moieties were attached to the antibody used to pretarget cells for labeling.

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