"This text 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 first chapters of this book illustrate the history of GPCRs based on distinct species and genomic information. This is followed by discussion of the homo- and hetero-oligomerization features of GPCRs, including receptors for glutamate, GABAB, dopamine, and chemokines. Several chapters aredevoted to the key signaling features of GPCRs. The authors take time to detail the importance of the pathophysiological function and drug targeting of GPCRs, specifically -adrenoceptors in cardiovascular and respiratory diseases, metabotropic glutamate receptors in CNS disorders, S1P receptors in the immune system, and Wnt/Frizzled receptors in osteoporosis"--Provided by publisher.
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"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
Muu info
Comprehensive overview of recent discoveries, the current understanding of the biology of GPCRs and their validity as drug targets.
Part I. Advances in GPCR Protein Research:
1. The evolution of the
repertoire and structure of G protein-coupled receptors Torsten Schoenberg,
Kristin Schroeck, Claudia Staeubert and Andreas Russ;
2. Functional studies
of isolated GPCR-G protein complexes in the membrane bilayer of lipoprotein
particles Adam J. Kuszak, Xiao Jie Yao, Sören G. F. Rasmussen, Brian K.
Kobilka and Roger K. Sunahara; Part II. Oligomerization of GPCRs:
3. GPCR-G
protein fusions: use in functional dimerization analysis Graeme Milligan;
4.
Time-resolved FRET approaches to study GPCR complexes Jean Phillipe Pin,
Damien Maurell, Laetitia Comps-Agrar, Carine Monnier, Marie-Laure Rives,
Etienne Doumazane, Philippe Rondard, Thierry Durroux, Laurent Prézeau and
Erin Trinquet;
5. Signaling of dopamine receptor homo- and hetero-oligomers
Ahmed Hasbi, Brian F. O'Dowd and Susan R. George;
6. Functional consequences
of chemokine receptor dimerization Mario Mellado, Carlos Martinez-A. and Jose
Miguel Rodgriguez-Frade; Part III. GPCR Signaling Features:
7. G protein
functions identified using genetic mouse models Stefan Offermanns;
8.
Kinetics of GPCR, G protein and effector activation Peter Hein;
9.
RGS-RhoGEFs and other RGS multidomain proteins as effector molecules in
GPCR-dependent and GPCR-independent cell signaling José Vázquez-Prado and J.
Silvio Gutkind;
10. Adenylyl cyclase isoform-specific signaling of GPCRs
Karin F. K. Ejendal, Julie A. Przybyla and Val J. Watts;
11. G
protein-independent and arrestin-dependent GPCR signaling Zhongzhen Nie and
Yehia Daaka;
12. Assays to read GPCR modulation and signaling Ralf Heilker
and Michael Wolff; Part IV. Ligand Pharmacology of GPCRs:
13. Quantifying
allosteric ligand-receptor interactions Ivan Toma Vranesic and Daniel Hoyer;
14. 7TM Receptor functional selectivity Terry Kenakin; Part V. Physiological
Functions and Drug Targeting of GPCRs:
15. Beta adrenergic receptors in
cardiovascular and respiratory diseases Michele Ciccarelli, J. Kurt Chuprun
and Walter J. Koch;
16. Role of metabotropic glutamate receptors in CNS
disorders Richard M. O'Connor and John F. Cryan;
17. S1P receptor agonists, a
novel generation of immunosuppressants Rosa Lopez Almagro, Gema Tarrason and
Nuria Godessart;
18. Wnt/Frizzled receptor signaling in osteoporosis Georges
Rawadi.
Dr Siehler is a Research Investigator at the Novartis Institute 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 Milligan is Professor of Molecular Pharmacology at the University of Glasgow. He is actively involved in numerous associations, such as the Biochemical Society and British Pharmacological Society. Dr Milligan was awarded the Ariens Award for Pharmacology from the Dutch Pharmacological Society in 2006.
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