In this review, recent progress in tetrazine-based fluorogenic probes for bioorthogonal chemistry is comprehensively analyzed, with a focus on advancements in probe design and their imaging applications for molecular processes in live cells.
Peptides were radiolabeled with [18F]AmBF3-Tz using IEDDA-based tetrazine ligation, producing radiopeptides in different oxidation states. In this study, the formed tautomers were rapidly (10 min) converted to the stable oxidized radiopeptides.
We developed a hydrophilic 18F-labeled a-TCO derivative [18F]3 through a readily available precursor and a single-step radiofluorination reaction.[18F]3 can be used to construct multiple small molecule- and protein-based imaging probes.
Micellar nanoreactors based on the self-assembly of an IEDDA reactive unit bearing amphiphilic polymers are reported. The deployment of the nanoreactors for cancer chemotherapy via prodrug activation by the IEDDA reaction is also demonstrated.
Click-triggered reactivation of caged cytokine constructs at the tumour site via a Diels–Alder–pyridazine-elimination cascade restores signalling and immune activation. This approach reduces systemic toxicity of immunocytokine therapies.