Tetrazine‐responsive self‐immolative linkers

Neumann, Kevin and Jain, Sarthak and Gambardella, Alessia and Walker, Sarah E. and Valero, Elsa and Lilienkampf, Annamaria and Bradley, Mark (2017) Tetrazine‐responsive self‐immolative linkers. Chembiochem, 18 (1). pp. 91-95. ISSN 1439-4227 (https://doi.org/10.1002/cbic.201600560)

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Molecules that undergo activation or modulation following the addition of benign external small‐molecule chemical stimuli have numerous applications. Here, we report the highly efficient “decaging” of a variety of moieties by activation of a “self‐immolative” linker, by application of water‐soluble and stable tetrazine, including the controlled delivery of doxorubicin in a cellular context.