This work was supported by The Skaggs Institue for Chemical Biology, Pfizer, Inc., and the NIH (RR021886). We are grateful to Matthias Park for assistance with the synthesis of 3.
Analysis and Optimization of Copper-Catalyzed Azide–Alkyne Cycloaddition for Bioconjugation†
Article first published online: 26 NOV 2009
Copyright © 2009 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Angewandte Chemie International Edition
Volume 48, Issue 52, pages 9879–9883, December 21, 2009
How to Cite
Hong, V., Presolski, Stanislav I., Ma, C. and Finn, M. G. (2009), Analysis and Optimization of Copper-Catalyzed Azide–Alkyne Cycloaddition for Bioconjugation. Angew. Chem. Int. Ed., 48: 9879–9883. doi: 10.1002/anie.200905087
- Issue published online: 15 DEC 2009
- Article first published online: 26 NOV 2009
- Manuscript Received: 10 SEP 2009
- The Skaggs Institue for Chemical Biology
- NIH. Grant Number: RR021886
How to click with biomolecules: Copper-catalyzed azide–alkyne cycloaddition has been optimized for use with biological molecules. The key development is the addition of two reagents that allow ascorbate to be used as reducing agent whilst eliminating problems caused by copper ascorbate side reactions. The result is a robust, rapid, and convenient procedure for the modification of proteins, DNA, RNA, and other biomolecules (see scheme).