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J C R Cardoso, M S Clark, F A Viera, P D Bridge, A Gilles, and D M Power

Introduction The G-protein-coupled receptors (GPCRs) are one of the largest known groups of proteins, comprising up to 80% of the total number of receptors identified in cells ( Bockaert 1991 , Bockaert et al. 2002 ). There are

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Bice Chini and Marco Parenti

G-protein-coupled receptors–cholesterol interactions Eighty-ninety per cent of whole-cell cholesterol is contained within the plasma membrane, where it accounts for 20–25% of lipid molecules ( Lange 1991 , Simons & Ikonen 2000 ). Cholesterol, which

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Davide Calebiro, Viacheslav O Nikolaev, and Martin J Lohse

Introduction G protein-coupled receptors (GPCRs) constitute the major family of cell surface receptors. They comprise receptors for light, taste, and smell as well as receptors for ions, small transmitters, peptides, and large protein hormones

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Patricia M Lenhart, Stefan Broselid, Cordelia J Barrick, L M Fredrik Leeb-Lundberg, and Kathleen M Caron

Introduction Receptor activity-modifying proteins (RAMPs) are single-pass transmembrane-accessory proteins that interact with G-protein-coupled receptors (GPCRs) to modulate their trafficking, ligand-binding specificity, and downstream signaling

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Aqfan Jamaluddin and Caroline M Gorvin

Introduction G protein-coupled receptors (GPCRs) are the largest family of transmembrane proteins and are involved in the regulation of diverse physiological processes including regulation of the cardiovascular, nervous and endocrine systems

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Ying Zhang, Mingtong Xu, Shaoling Zhang, Li Yan, Chuan Yang, Wensheng Lu, Yan Li, and Hua Cheng

protect against the proapoptotic effects of saturated fatty acids ( Eitel et al. 2002 , Maedler et al. 2003 ). The mechanism underlying these actions is not well understood. G protein-coupled receptor 40 (GPR40), which is a member of GPRs, has

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J Shaik Mohamed, Abby D Benninghoff, G Joan Holt, and Izhar A Khan

Introduction Considerable evidence has accumulated in the past few years demonstrating that the G protein-coupled receptor 54 (GPR54) plays a critical role in the control of gonadotropin-releasing hormone (GnRH) release at the onset

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LM Luttrell

A growing body of data supports the conclusion that G protein-coupled receptors can regulate cellular growth and differentiation by controlling the activity of MAP kinases. The activation of heterotrimeric G protein pools initiates a complex network of signals leading to MAP kinase activation that frequently involves cross-talk between G protein-coupled receptors and receptor tyrosine kinases or focal adhesions. The dominant mechanism of MAP kinase activation varies significantly between receptor and cell type. Moreover, the mechanism of MAP kinase activation has a substantial impact on MAP kinase function. Some signals lead to the targeting of activated MAP kinase to specific extranuclear locations, while others activate a MAP kinase pool that is free to translocate to the nucleus and contribute to a mitogenic response.

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B Chini and M Parenti

This review describes the advances in our understanding of the role of G-protein coupled receptor (GPCR) localisation in membrane microdomains known as lipid rafts and caveolae. The growing interest in these specialised regions is due to the recognition that they are involved in the regulation of a number of cell functions, including the fine-tuning of various signalling molecules. As a number of GPCRs have been found to be enriched in lipid rafts and/or caveolae by means of different experimental approaches, we first discuss the pitfalls and uncertainties related to the use of these different procedures. We then analyse the addressing signals that drive and/or stabilise GPCRs in lipid rafts and caveolae, and explore the role of rafts/caveolae in regulating GPCR trafficking, particularly in receptor exo- and endocytosis. Finally, we review the growing evidence that lipid rafts and caveolae participate in the regulation of GPCR signalling by affecting both signalling selectivity and coupling efficacy.

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Flavia Giannone, Giorgio Malpeli, Veronica Lisi, Silvia Grasso, Priyanka Shukla, Dunia Ramarli, Silvia Sartoris, Vladia Monsurró, Mauro Krampera, Eliana Amato, Giuseppe Tridente, Marco Colombatti, Marco Parenti, and Giulio Innamorati

best known for its ability to create a functional link between hundreds of different G protein-coupled receptors (GPCRs) and the β isoform of phospholipase C (PLCβ; Milligan et al . 1996 ). For this reason, G15 has often served as a versatile readout