G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity, Volume 24

With its particular emphasis on the constitutive activity of G-protein-coupled receptors (GPCRs)s, this book comprehensively discusses an important biological process that has not yet been covered in such depth in any other existing books on GPCRs. The international team of highly distinguished authors addresses in detail current models and concepts, to introduce medicinal chemists, physiologists, pharmacologists, and medical researchers into the advances in the understanding of GPCR activation and constitutive activity. In addition, the book provides an overview on methods of investigating constitutive GPCR activity. The text is well illustrated by selected experimental data and schemes._The chaptes are all cross-referenced with each other and cover general mechnisms, methodological approaches and cover selected important GPCR sysstems, the consequences for drug action, including, side effects, and rational drug design for GPCR targets. A highly recommended reference for researchers in academia and industry.
authors addresses in detail current models and concepts, so as to introduce pharmaceutical chemists, physiologists and medical researchers to the advances in the understanding of GPCR activation and constitutive activity, and provides an overview of the methods of investigating GPCR activity. The text is backed by abundant case studies and methodological advice for analyzing GPCRs, covering selected pharmacologically relevant GPCR systems, the consequences for drug action, including unwanted side effects, and rational drug design for GPCR targets.
A highly practical reference for researchers in academia and industry.Content:
Chapter 1 Historical Background and Introduction (pages 1–10): Richard A. Bond and Robert J. Lefkowitz
Chapter 2 The Nature of Constitutive Activity and Inverse Agonism (pages 11–26): Terry Kenakin
Chapter 3 Molecular Mechanisms of GPCR Activation (pages 27–42): Soren G. F. Rasmussen and Ulrik Gether
Chapter 4 Molecular and Cellular Determinants of GPCR Splice Variant Constitutive Activity (pages 43–54): Joel Bockaert, Sylvie Claeysen, Lara Joubert, Laurent Fagni and Aline Dumuis
Chapter 5 Naturally Occurring Constitutively Active Receptors: Physiological and Pharmacological Implications (pages 55–61): Alan S. Kopin and Martin Beinborn
Chapter 6 The Impact of G Proteins on Constitutive GPCR Activity (pages 63–70): Graeme Milligan
Chapter 7 (Patho)physiological and Therapeutic Relevance of Constitutive Activity and Inverse Agonism at G Protein?Coupled Receptors (pages 71–80): Lutz Hein
Chapter 8 Methodological Approaches (pages 81–120): Prof. Thomas Wieland and Prof. Roland Seifert
Chapter 9 Constitutive Activity of ??Adrenoceptors: Analysis in Membrane Systems (pages 121–140): Prof. Roland Seifert
Chapter 10 Constitutive Activity of ??Adrenoceptors: Analysis by Physiological Methods (pages 141–157): Ursula Ravens, Clive J. Lewis and Sian E. Harding
Chapter 11 Constitutive Activity at the ?1?Adrenoceptors: Past and Future Implications (pages 159–176): Susanna Cotecchia, Francesca Fanelli, Alexander Scheer and Tommaso Costa
Chapter 12 Constitutive Activity of Muscarinic Acetylcholine Receptors: Implications for Receptor Activation and Physiological Relevance (pages 177–193): Ethan S. Burstein and Tracy A. Spalding
Chapter 13 Constitutively Active Histamine Receptors (pages 195–222): Remko A. Bakker and Rob Leurs
Chapter 14 Constitutively Active Serotonin Receptors (pages 223–241): Katharine Herrick?Davis
Chapter 15 Virally Encoded Constitutively Active Chemokine Receptors (pages 243–264): Barbara Moepps and Peter Gierschik