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Updated: May 16, 2026

Efficient and Site-specific Antibody Labeling by Strain-promoted Azide-alkyne Cycloaddition
Published on: December 23, 2016
Chemoselective Azidation of Cysteine Coupled with Traceless Staudinger Ligation Enables Site-Specific Acylation of
Tingting Cui1, Jian Sun1, Na Liu1
1School of Food and Biological Engineering, Engineering Research Center of Bio-process, Ministry of Education, Key Laboratory of Animal Source of Anhui Province, Hefei University of Technology, Hefei 230009, China.
Abstract:
We report a novel strategy for site-specific acylation of recombinant proteins that proceeds via chemoselective azidation of cysteine residues using a vinyl thianthrenium salt and sodium azide, followed by traceless Staudinger ligation with acyl-functionalized phosphinoester reagents. The utility of this method is exemplified by the efficient preparation of a panel of site-specifically acylated ubiquitin variants and a crotonylated histone, providing a practical tool for accessing homogeneous acylated proteins to advance mechanistic studies of lysine acylation.
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