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Keywords:

  • alkynes;
  • azides;
  • bioconjugation;
  • cycloaddition;
  • copper
Thumbnail image of graphical abstract

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).