Bioconjugation by copper(I)-catalyzed azide-alkyne [3 + 2] cycloaddition - PubMed (original) (raw)

. 2003 Mar 19;125(11):3192-3.

doi: 10.1021/ja021381e.

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Bioconjugation by copper(I)-catalyzed azide-alkyne [3 + 2] cycloaddition

Qian Wang et al. J Am Chem Soc. 2003.

Abstract

The copper-catalyzed cycloaddition reaction between azides and alkynes functions efficiently in aqueous solution in the presence of a tris(triazolyl)amine ligand. The process has been employed to make rapid and reliable covalent connections to micromolar concentrations of protein decorated with either of the reactive moieties. The chelating ligand plays a crucial role in stabilizing the Cu(I) oxidation state and protecting the protein from Cu(triazole)-induced denaturation. Because the azide and alkyne groups themselves are unreactive with protein residues or other biomolecules, their ligation is of potential utility as a general bioconjugation method.

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