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

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Abstract

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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Supplementary files

Article information


Submitted
13 Jun 2018
Accepted
12 Jul 2018
First published
12 Jul 2018

This article is Open Access
All publication charges for this article have been paid for by the Royal Society of Chemistry

Chem. Sci., 2018,9, 7198-7203
Article type
Edge Article

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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