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Issue 36, 2018
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Tetrazine-mediated bioorthogonal prodrug–prodrug activation

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The selective and biocompatible activation of prodrugs within complex biological systems remains a key challenge in medical chemistry and chemical biology. Herein we report, for the first time, a dual prodrug activation strategy that fully satisfies the principle of bioorthogonality by the symbiotic formation of two active drugs. This dual and traceless prodrug activation strategy takes advantage of the INVDA chemistry of tetrazines (here a prodrug), generating a pyridazine-based miR21 inhibitor and the anti-cancer drug camptothecin and offers a new concept in prodrug activation.

Graphical abstract: Tetrazine-mediated bioorthogonal prodrug–prodrug activation

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The article was received on 13 Jun 2018, accepted on 12 Jul 2018 and first published on 12 Jul 2018

Article type: Edge Article
DOI: 10.1039/C8SC02610F
Citation: Chem. Sci., 2018,9, 7198-7203
  • Open access: Creative Commons BY-NC license
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    Tetrazine-mediated bioorthogonal prodrug–prodrug activation

    K. Neumann, A. Gambardella, A. Lilienkampf and M. Bradley, Chem. Sci., 2018, 9, 7198
    DOI: 10.1039/C8SC02610F

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