G protein-coupled receptors : structure, signaling, and physiology

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.

Author Notes

Dr. Sandra Siehler is a Research Investigator at the Novartis Institutes for BioMedical Research in Basel, Switzerland. Dr. Siehler is a member of the American Society for Pharmacology and Experimental Therapeutics and the British Pharmacological Society.
Dr. Graeme Milligan is Professor of Molecular Pharmacology at the University of Glasgow. He is actively involved in numerous associations, such as the Biochemical Society and the British Pharmacology Society. Dr. Milligan was awarded the Ariens Award for Pharmacology from the Dutch Pharmacological Society in 2006.

Torsten Schöneberg and Kristin Schröck and Claudia Stäubert and Andreas RussAdam J. Kuszak and Xiao Jie Yao and Sören G. F. Rasmussen and Brian K. Kobilka and Roger K. SunaharaGraeme MilliganJean Phillipe Pin and Damien Maurel and Laetitia Comps-Agrar and Carine Monnier and Marie-Laure Rives and Etienne Doumazane and Philippe Rondard and Thierry Durroux and Laurent Prézeau and Erin TrinquetAhmed Hasbi and Brian F. O'Dowd and Susan R. GeorgeMario Mellado and Carlos Martínez-A and José Miguel Rodríguez-FradeStefan OffermannsPeter HeinJosé Vázquez-Prado and J. Silvio GutkindKarin F.K. Ejendal and Julie A. Przybyla and Val J. WattsZhongzhen Nie and Yehia DaakaRalf Heilker and Michael WolffIvan Toma Vranesic and Daniel HoyerTerry KenakinMichele Ciccarelli and J. Kurt Chuprun and Walter J. KochRichard M. O'Connor and John F. CryanRosa López Almagro and Gema Tarrasón and Nuria GodessartGeorges Rawadi

List of Figures	p. vii
List of Tables	p. xi
List of Contributors	p. xiii
Introduction	p. 1
Part I Advances in GPCR Protein Research
1 The evolution of the repertoire and structure of G protein-coupled receptors	p. 5
2 Functional studies of isolated GPCR-G protein complexes in the membrane bilayer of lipoprotein particles	p. 32
Part II Oligomerization of GPCRs
3 GPCR-G protein fusions: Use in functional dimerization analysis	p. 53
4 Time-resolved FRET approaches to study GPCR complexes	p. 67
5 Signaling of dopamine receptor homo-and heterooligomers	p. 90
6 Functional consequences of chemokine receptor dimerization	p. 111
Part III GPCR Signaling Features
7 G protein functions identified using genetic mouse models	p. 125
8 Kinetics of GPCR, G protein, and effector activation	p. 145
9 RGS-RhoGEFs and other RGS multidomain proteins as effector molecules in GPCR-dependent and GPCR-independent cell signaling	p. 159
10 Adenylyl cyclase isoform-specific signaling of GPCRs	p. 189
11 G protein-independent and ß arrestin-dependent GPCR signaling	p. 217
12 Assays to read GPCR modulation and signaling	p. 231
Part IV Ligand Pharmacology of GPCRS
13 Assessing allosteric ligand-receptor interactions	p. 247
14 7TM receptor functional selectivity	p. 270
Part V Physiological Functions and Drug Targeting of GPCRS
15 ß-Adrenoceptors in cardiovascular and respiratory diseases	p. 287
16 Role of metabotropic glutamate receptors in CNS disorders	p. 321
17 S1P receptor agonists, a novel generation of immunosuppressants	p. 380
18 Wnt/Frizzled receptor signaling in osteoporosis	p. 398
Index	p. 415

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Table of Contents