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.
A new radiotracer [68Ga]Ga-THP-tetrazine for bioorthogonal click radiochemistry is presented. Its ability for pretargeted imaging of long-circulating liposomal nanomedicines was tested in vitro and in vivo in both healthy and tumour murine models.
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.
This review highlights the mechanisms underlying the unique fluorogenic properties of tetrazine-functionalized labels and proposes new strategies to enhance fluorogenicity in the near-infrared region.