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Updated: Mar 30, 2026

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
Published on: September 13, 2013
Glycan-Mediated, Ligand-Controlled Click Chemistry for Drug-Target Identification
Henning Stöckmann1, Violeta L Marin2, Paul Nimmer2
1Discovery Chemistry and Technology, Oncology Discovery, Integrated Sciences and Technology, AbbVie Inc., 1 North Waukegan Road, North Chicago, IL, 60064, USA. henning.stoeckmann@abbvie.com.
Abstract:
Membrane-bound proteins are important pharmaceutical drug targets, yet few strategies exist for the identification of small-molecule-targeted membrane proteins in live-cell systems. By exploiting metabolic glycan engineering of cell membrane proteins, we have developed an in situ glycan-mediated ligand-controlled click ("GLiCo-Click") chemistry methodology that enables the attachment of small-molecule chemical probes to their receptor protein through glycans on live cells. In addition to enabling receptor enrichment from cell lysates, this strategy can be used to demonstrate target receptor engagement and enables the molecular characterization of receptors.
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