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Signaling mechanisms of GPCR ligands

Strange, P. G. (2008) Signaling mechanisms of GPCR ligands. Current Opinion in Drug Discovery & Development, 11 (2). pp. 196-202. ISSN 1367-6733

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Abstract/Summary

G protein-coupled receptors constitute one of the major classes of drug targets, so understanding the mechanisms of signaling through these receptors is of great importance. This review covers some of the recent advances in G protein-coupled receptor signaling. A high resolution structure of the beta(2)-adrenergic receptor has been reported, as well as several molecular switches involved in receptor activation. It has also been realised that receptors and G proteins and their subunits may not always separate upon receptor activation. The definition of the ability of these receptors to signal has been expanded considerably with the realisation that some signaling may occur independently of G proteins, that some signaling events may differ in their pharmacological profiles and that formation of heterodimers of these receptors may provide new avenues for both signaling and drug design.

Item Type:Article
Refereed:Yes
Divisions:Faculty of Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy
ID Code:13632
Uncontrolled Keywords:conformational change, efficacy, G protein-coupled receptors, heterodimer, signaling mechanisms, structure and organization, PROTEIN-COUPLED-RECEPTOR, RESONANCE ENERGY-TRANSFER, LIVING CELLS, CRYSTAL-STRUCTURE, ADRENERGIC-RECEPTOR, INVERSE AGONISM, BETA-ARRESTIN, BRET ANALYSIS, ACTIVATION, BINDING

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