G Protein-Coupled Receptors: Structure, Signaling, and Physiology

doi:10.1017/CBO9780511760334

Provides a comprehensive overview of recent discoveries and current understandings of G protein-coupled receptors (GPCRs). Recent advances include the first mammalian non-rhodopsin GPCR structures and reconstitution of purified GPCRs into membrane discs for defined studies, novel signaling features including oligomerization, and advances in understanding the complex ligand pharmacology and physiology of GPCRs, in new assay technologies and drug targeting. The authors take time to detail the importance of the pathophysiological function and drug targeting of GPCRs, specifically β-adrenoceptors in cardiovascular and respiratory diseases, metabotropic glutamate receptors in CNS disorders, S1P receptors in the immune system, and Wnt/Frizzled receptors in osteoporosis. This book will be invaluable to researchers and graduate students in academia and industry who are interested in the GPCR field.

"The editors of G Protein-Coupled Receptors: Structure, Signaling, and Physiology successfully synthesize decades of research into a well-organized reference textbook. The layout of this text is one of its best features... the strengths of this text would be most appreciated by the structural pharmacologist hoping to gain a comprehensive overview of GPCR biology. The well-outlined chapters balance the abundance and often overwhelming supply of references, while the simple figures and summary tables provide valuable information for the GPCR novice."
Alexandra Teixeira, Yale Journal of Biology and Medicine

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Contents

Frontmatter
pp i-iv
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Contents
pp v-vi
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List of Figures
pp vii-x
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List of Tables
pp xi-xii
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List of Contributors
pp xiii-xvi
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Introduction
pp 1-4
- By Sandra Siehler, Novartis Institutes for Biomedical Research, Graeme Milligan, University of Glasgow
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PART I - ADVANCES IN GPCR PROTEIN RESEARCH
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1 - The evolution of the repertoire and structure of G protein-coupled receptors
pp 5-31
- By Torsten Schöneberg, University of Leipzig, Kristin Schröck, University of Leipzig, Claudia Stäubert, University of Leipzig, Andreas Russ, University of Oxford
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2 - Functional studies of isolated GPCR-G protein complexes in the membrane bilayer of lipoprotein particles
pp 32-52
- By Adam J. Kuszak, University of Michigan, Xiao Jie Yao, Stanford University, Sören G.F. Rasmussen, Stanford University, Brian K. Kobilka, Stanford University, Roger K. Sunahara, University of Michigan
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PART II - OLIGOMERIZATION OF GPCRS
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3 - GPCR-G protein fusions: Use in functional dimerization analysis
pp 53-66
- By Graeme Milligan, University of Glasgow
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4 - Time-resolved FRET approaches to study GPCR complexes
pp 67-89
- By Jean Philippe Pin, Institut de Génomique Fonctionnelle, Damien Maurel, Ecole Polytechnique Fédérale de Lausane, Laetitia Comps-Agrar, Institut de Génomique Fonctionnelle, Carine Monnier, Institut de Génomique Fonctionnelle, Marie-Laure Rives, Columbia University, Etienne Doumazane, Institut de Génomique Fonctionnelle, Philippe Rondard, Institut de Génomique Fonctionnelle, Thierry Durroux, Institut de Génomique Fonctionnelle, Laurent Prézeau, Institut de Génomique Fonctionnelle, Erin Trinquet, Parc technologique Marcel Boiteux
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5 - Signaling of dopamine receptor homo- and heterooligomers
pp 90-110
- By Ahmed Hasbi, University of Toronto, Brian F. O'Dowd, University of Toronto, Susan R. George, University of Toronto
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6 - Functional consequences of chemokine receptor dimerization
pp 111-124
- By Mario Mellado, Centro Nacional de Biotecnologia, Carlos Martínez-A, Centro Nacional de Biotecnologia, José Miguel Rodríguez-Frade, Centro Nacional de Biotecnologia
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PART III - GPCR SIGNALING FEATURES
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7 - G protein functions identified using genetic mouse models
pp 125-144
- By Stefan Offermanns, Max-Planck Institute for Heart and Lung Research
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8 - Kinetics of GPCR, G protein, and effector activation
pp 145-158
- By Peter Hein, University of California at San Francisco
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9 - RGS-RhoGEFs and other RGS multidomain proteins as effector molecules in GPCR-dependent and GPCR-independent cell signaling
pp 159-188
- By José Vázquez-Prado, National Polytechnic Institute, J. Silvio Gutkind, National Institutes of Health
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10 - Adenylyl cyclase isoform-specific signaling of GPCRs
pp 189-216
- By Karin F. K. Ejendal, Purdue University, Julie A. Przybyla, Purdue University, Val J. Watts, Purdue University
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11 - G protein-independent and β arrestin-dependent GPCR signaling
pp 217-230
- By Zhongzhen Nie, University of Florida, Yehia Daaka, University of Florida
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12 - Assays to read GPCR modulation and signaling
pp 231-246
- By Ralf Heilker, Boehringer Ingelheim Pharma GmbH & Co. KG, Michael Wolff, Boehringer Ingelheim Pharma GmbH & Co. KG
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PART IV - LIGAND PHARMACOLOGY OF GPCRS
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13 - Assessing allosteric ligand-receptor interactions
pp 247-269
- By Ivan Toma Vranesic, Novartis Institutes for BioMedical Research, Daniel Hoyer, Novartis Institutes for BioMedical Research
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14 - 7TM receptor functional selectivity
pp 270-286
- By Terry Kenakin, GlaxoSmithKline Research and Development
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PART V - PHYSIOLOGICAL FUNCTIONS AND DRUG TARGETING OF GPCRS
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15 - β-Adrenoceptors in cardiovascular and respiratory diseases
pp 287-320
- By Michele Ciccarelli, Thomas Jefferson University, J. Kurt Chuprun, Thomas Jefferson University, Walter J. Koch, Thomas Jefferson University
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16 - Role of metabotropic glutamate receptors in CNS disorders
pp 321-379
- By Richard M. O'Connor, University College Cork, John F. Cryan, University College Cork
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17 - S1P receptor agonists, a novel generation of immunosuppressants
pp 380-397
- By Rosa López Almagro, Almirall, Barcelona, Gema Tarrasón, Almirall, Barcelona, Nuria Godessart, Almirall Laboratories, Llobregat
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18 - Wnt/Frizzled receptor signaling in osteoporosis
pp 398-414
- By Georges Rawadi, Galapagos, Romainville
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Index
pp 415-430
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G Protein-Coupled Receptors

Structure, Signaling, and Physiology

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