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Updated: May 29, 2026

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates

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Published on: March 6, 2019

Staudinger ligation as a method for bioconjugation.

Sander S van Berkel¹, Mark B van Eldijk, Jan C M van Hest

¹Department of Bioorganic Chemistry, Radboud University Nijmegen, Heyendaalseweg 135, NL-6525 AJ Nijmegen, The Netherlands.

Angewandte Chemie (International Ed. in English)

|September 3, 2011

Summary

This summary is machine-generated.

The Staudinger ligation, a bio-orthogonal reaction between azides and phosphines, enables versatile bioconjugation. This review highlights recent advancements and applications in labeling biomolecules and synthesizing biopolymers.

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Area of Science:

Chemical Biology
Organic Chemistry

Background:

The Staudinger ligation, first described in 1919, involves the reaction between azides and phosphines.
Recognized for its bioconjugation potential by Bertozzi and co-workers, it is a bio-orthogonal reaction.
Its bio-orthogonal nature allows applications in complex biological systems.

Purpose of the Study:

To review recent developments in Staudinger ligation.
To highlight new applications of Staudinger ligation in bioconjugation.

Main Methods:

Utilizing the Staudinger ligation for labeling glycans, lipids, DNA, and proteins.
Employing Staudinger ligation as a synthetic strategy for glycopeptides, microarrays, and biopolymers.

Main Results:

Staudinger ligation has found numerous applications in labeling diverse biomolecules.
It serves as a key synthetic method for constructing complex biostructures.
The reaction has established a high standard in bio-orthogonal ligation strategies.

Conclusions:

The Staudinger ligation is a powerful and versatile bio-orthogonal tool.
Recent advancements continue to expand its utility in chemical biology and beyond.
It remains a benchmark for emerging bio-orthogonal ligation techniques.