Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 55, Issue 50, Pages 15662-15666Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201609837
Keywords
bioorthogonal chemistry; copper; heterogeneous catalysis; prodrugs
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Funding
- Rosetrees Trust [A865]
- British Heart Foundation Centre of Research Excellence
- Wellcome Trust Multi User Equipment Grant [WT104915MA]
- Engineering and Physical Sciences Research Council [EP/I016627/1] Funding Source: researchfish
- Rosetrees Trust [M498] Funding Source: researchfish
- EPSRC [EP/I016627/1] Funding Source: UKRI
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The copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction has proven to be a pivotal advance in chemical ligation strategies with applications ranging from polymer fabrication to bioconjugation. However, application in vivo has been limited by the inherent toxicity of the copper catalyst. Herein, we report the application of heterogeneous copper catalysts in azide-alkyne cycloaddition processes in biological systems ranging from cells to zebrafish, with reactions spanning from fluorophore activation to the first reported in situ generation of a triazole-containing anticancer agent from two benign components, opening up many new avenues of exploration for CuAAC chemistry.
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