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Class A G-Protein-Coupled Receptor (GPCR) Dimers and Bivalent Ligands

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Department of Chemistry and Pharmacy, Emil Fischer Center, Friedrich Alexander University, Schuhstraße 19, 91052 Erlangen, Germany
*Phone: +49 9131 85-29383. Fax: +49 9131 85-22585. E-mail: [email protected]
Cite this: J. Med. Chem. 2013, 56, 17, 6542–6559
Publication Date (Web):May 16, 2013
Copyright © 2013 American Chemical Society

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    G-protein-coupled receptors (GPCRs) represent the largest family of membrane proteins involved in cellular signal transduction and are activated by various different ligand types including photons, peptides, proteins, but also small molecules like biogenic amines. Therefore, GPCRs are involved in diverse physiological processes and provide valuable drug targets for numerous diseases. Emerging body of evidence suggests that GPCRs exist as monomers or cross-react forming dimers and higher-ordered oligomers. In this Perspective we will review current biochemical and biophysical techniques to visualize GPCR dimerization, functional consequences of homo- and heterodimers, and approaches of medicinal chemists to target these receptor complexes with homo- and heterobivalent ligands.

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