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Updated: Apr 13, 2026

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
Published on: September 13, 2013
Rational Modification of the Biological Profile of GPCR Ligands through Combination with Other Biologically Active
Guozheng Huang1, Martin Nimczick1, Michael Decker1
1Pharmazeutische und Medizinische Chemie, Institut für Pharmazie und Lebensmittelchemie, Julius-Maximilians-Universität Würzburg, Würzburg, Germany.
Abstract:
In recent years, G protein-coupled receptor (GPCR) ligands have not only been modified by conducting structure-activity relationship studies of leads and known ligands, but several new approaches have emerged in which GPCR ligands were connected or merged with other biologically active molecules. Identical or related ligands were combined to bivalent ones. Orthosteric ligands were combined with allosteric ligands, sometimes leading to dualsteric ones, and also chemical structures were merged to dual-acting or multifunctional compounds. In this article, we want to present some representative examples for these approaches at different GPCRs, showing the versatility of this approach, with a focus on our own work and references to related articles and reviews.
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