4.4 Article

Tetrazine-Responsive Self-immolative Linkers

Journal

CHEMBIOCHEM
Volume 18, Issue 1, Pages 91-95

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbic.201600560

Keywords

Diels-Alder reaction; doxorubicin; nanoparticles; prodrugs; tetrazine

Funding

  1. European Research Council [ADREEM ERC-2013-340469]
  2. Edinburgh Global Research Scholarship
  3. School of Chemistry Tercentenary International PhD Scholarship (University of Edinburgh)
  4. EU Marie Curie Intra-European Fellowship for career development [FP7-PEOPLE-2012-IEF-327903-CLEDEPOLY]

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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.

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