Tetrazine Carbon Nanotubes for Pretargeted In Vivo “Click‐to‐Release” Bioorthogonal Tumour Imaging

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  • He Li
    Department of Chemistry University of Cambridge Lensfield Road Cambridge CB2 1EW UK
  • João Conde
    Instituto de Medicina Molecular Faculdade de Medicina da Universidade de Lisboa Av. Prof. Egas Moniz 1649-028 Lisboa Portugal
  • Ana Guerreiro
    Instituto de Medicina Molecular Faculdade de Medicina da Universidade de Lisboa Av. Prof. Egas Moniz 1649-028 Lisboa Portugal
  • Gonçalo J. L. Bernardes
    Department of Chemistry University of Cambridge Lensfield Road Cambridge CB2 1EW UK

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<jats:title>Abstract</jats:title><jats:p>The bioorthogonal inverse‐electron‐demand Diels–Alder (IEDDA) cleavage reaction between tetrazine and <jats:italic>trans</jats:italic>‐cyclooctene (TCO) is a powerful way to control the release of bioactive agents and imaging probes. In this study, a pretargeted activation strategy using single‐walled carbon nanotubes (SWCNTs) that bear tetrazines (TZ@SWCNTs) and a TCO‐caged molecule was used to deliver active effector molecules. To optimize a turn‐on signal by using in vivo fluorescence imaging, we developed a new fluorogenic near‐infrared probe that can be activated by bioorthogonal chemistry and image tumours in mice by caging hemicyanine with TCO (tHCA). With our pretargeting strategy, we have shown selective doxorubicin prodrug activation and instantaneous fluorescence imaging in living cells. By combining a tHCA probe and a pretargeted bioorthogonal approach, real‐time, non‐invasive tumour visualization with a high target‐to‐background ratio was achieved in a xenograft mice tumour model. The combined advantages of enhanced stability, kinetics and biocompatibility, and the superior pharmacokinetics of tetrazine‐functionalised SWCNTs could allow application of targeted bioorthogonal decaging approaches with minimal off‐site activation of fluorophore/drug.</jats:p>

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