Abstract
Bioorthogonal prodrug activation: The cover feature illustrates the release of a phenolic drug triggered by the reaction of a trans-cyclooctene (TCO) conjugate with a tetrazine molecule (Tz). Key to the structural design is the incorporation of a self-immolative linker (SIL) that ‘dissolves’ upon TCO/Tz click, enabling the development of bis(carbamate)-linked conjugates with substantially improved stability under physiological conditions. Applying this strategy, we demonstrate the bioorthogonal cleavage of a TCO-SIL-caged prodrug via in situ reaction with Tz. Thereby, we achieved controlled release of an antimitotic drug that induces depolymerization of microtubules, leading to a >200-fold ‘turn-on’ in cytotoxicity. More information can be found in the Research Article by H. Mikula et al.
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