Tetrazine-mediated bioorthogonal prodrug-prodrug activation
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Date
2018-09-28
Publication Type
Journal Article
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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.
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published
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Journal / series
Volume
9 (36)
Pages / Article No.
7198 - 7203
Publisher
Royal Society of Chemistry