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

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

Roland Seifert (Editor), Thomas Wieland (Editor), Raimund Mannhold (Series Editor), Hugo Kubinyi (Series Editor), Gerd Folkers (Series Editor)

ISBN: 978-3-527-60734-1

Apr 2006

304 pages

Description

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.
GENERAL CONCEPTS
Historical Background and Introduction.
The Nature of Constitutive Activity and Inverse Agonism.
Molecular Mechanisms of GPCR Activation.
Molecular and Cellular Determinants of GPCR Splice Variant Constitutive Activity.
Naturally Occurring Constitutively Active Receptors: Physiologic and Pharmacologic Implications.
The Impact of G-Proteins on Constitutive GPCR Activity.
(Patho)physiological and Therapeutic Relevance of Constitutive GPCR Activity.
Methodological Approaches.

CONSTITUTIVE ACITVITY OF SELECTED GPCR SYSTEMS
Constitutive Activity of -Adrenoceptors: Analysis in Membrane Systems.
Constitutive Activity of -Adrenoceptors: Analysis by Physiological Methods.
Constitutive Activity at the 1-Adrenoceptors: Past and Future Implications.
Constitutive Activity of Muscarinic Acetylcholine Receptors: Implications for Receptor Activation and Physiological Relevance.
Constitutively Active Histamine Receptors.
Constitutively Active Serotonin Receptors.
Virally Encoded Constitutively Active Chemokine Receptors.