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Molecular Pharmacology Fast Forward
First published on August 23, 2007; DOI: 10.1124/mol.107.040923

0026-895X/07/7205-1097-1099$20.00
Mol Pharmacol 72:1097-1099, 2007

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Perspectives

Ligand-Directed Signaling: 50 Ways to Find a Lover

Martin C. Michel, and Astrid E. Alewijnse

Department of Pharmacology and Pharmacotherapy, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands

Abstract

In contrast to earlier concepts, it seems that distinct ligands acting on the same receptor may elicit qualitative different response patterns, a phenomenon given many names, including "functional selectivity," "agonist-directed trafficking," "biased agonism," "protean agonism," or "ligand-directed signaling." In this issue of Molecular Pharmacology, Sato et al. (p. 1359) extend this concept to beta3-adrenergic receptors and report that distinct ligands can activate a single distal response via different signaling pathways. Moreover, they demonstrate that expression density can affect how distinct ligands acting on the same receptor differentially induce cellular responses. We discuss the underlying concepts for such findings and their implications for drug discovery.

Received August 15, 2007; accepted August 21, 2007

Address correspondence to: Prof. Martin C. Michel, Dept. Pharmacology and Pharmacotherapy, Academic Medical Center, University of Amsterdam, 1105 AZ Amsterdam, Netherlands. E-mail: m.c.michel{at}amc.uva.nl


Related articles in MolPharm:

Ligand-Directed Signaling at the beta3-Adrenoceptor Produced by 3-(2-Ethylphenoxy)-1-[(1,S)-1,2,3,4-tetrahydronapth-1-ylamino]-2S-2-propanol oxalate (SR59230A) Relative to Receptor Agonists
Masaaki Sato, Takahiro Horinouchi, Dana S. Hutchinson, Bronwyn A. Evans, and Roger J. Summers
MolPharm 2007 72: 1359-1368. [Abstract] [Full Text]  





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