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Cleavable linkers and their application in MS-based target identification.

Hester A Beard¹, Dimitris Korovesis, Suyuan Chen

¹KU Leuven, Department of Cellular and Molecular Medicine, Laboratory of Chemical Biology, Herestr. 49 box 802, 3000 Leuven, Belgium. steven.verhelst@kuleuven.be.

Molecular Omics

|January 28, 2021

Summary

This summary is machine-generated.

Cleavable linkers enhance chemical biology probes for identifying protein targets and modification sites. This improves understanding of post-translational modifications, enzyme function, and drug action.

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Area of Science:

Chemical Biology
Proteomics

Background:

Covalent chemical probes are essential tools in chemical biology.
These probes include post-translational modification (PTM)-derived metabolic probes, activity-based probes, and photoaffinity labels.
Target identification typically relies on tandem mass spectrometry-based proteomics.

Purpose of the Study:

To review different types of cleavable linkers used in chemical biology.
To discuss the benefits and limitations of cleavable linker technologies.
To illustrate the application of cleavable linkers in probe target identification.

Main Methods:

Review of scientific literature on cleavable linker technologies.
Analysis of tandem mass spectrometry-based proteomics workflows.
Case studies demonstrating the application of cleavable linkers.

Main Results:

Cleavable linkers have been integrated into proteomics workflows over the last fifteen years.
These linkers enable probe target identification with reduced background and increased confidence.
Linker technologies facilitate the identification of specific modification sites.

Conclusions:

Cleavable linkers significantly advance chemical biology by improving target identification and site localization.
The use of these linkers enhances knowledge of PTMs, enzyme function, and drug mechanisms.
This review provides a comprehensive overview of cleavable linkers and their impact on the field.