Bioconjugation by copper(I)-catalyzed azide-alkyne [3+2] cycloaddition
Bioconjugation by copper(I)-catalyzed azide-alkyne [3+2] cycloaddition
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DOI：
10.1021/ja021381e
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发表时间：
2003-03-19
影响因子：
15
通讯作者：
Finn, MG
中科院分区：
文献类型：
--
作者：
Wang, Q;Chan, TR;Finn, MG
铜催化叠氮化物与炔之间的环加成反应在三（三唑）胺配体存在的水溶液中有效地起作用。该过程已被用于快速和可靠的共价连接到微摩尔浓度的蛋白质修饰的任何一个反应部分。螯合配体在稳定Cu(I)氧化态和保护蛋白质免受Cu（三唑）诱导变性方面起着至关重要的作用。由于叠氮化物和炔基本身与蛋白质残基或其他生物分子不发生反应，因此它们的连接作为一种通用的生物偶联方法具有潜在的实用性。
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.