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

Roland Seifert (Editor), Thomas Wieland (Editor), Raimund Mannhold (Series Editor), Hugo Kubinyi (Series Editor), Gerd Folkers (Series Editor)
ISBN: 978-3-527-30819-4
304 pages
December 2005
G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity, Volume 24 (3527308199) cover image
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.
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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.
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Roland Seifert was born in 1960 in Berlin, Germany. He was fellow of the Merit Scholar Foundation of Germany and earned his MD degree at the Free University of Berlin in 1986. From 1986-1995 he worked in the group of Professor Günter Schultz in the Department of Pharmacology of the Free University of Berlin. From 1995-1998, he worked with Dr. Brian Kobilka at Stanford University, CA, USA. From 1998-2004 he was Associate Professor in the Department of Pharmacology and Toxicology of The University of Kansas, Lawrence, KS, USA before taking over the Chair of Pharmacology and Toxicology at The University of Regensburg, Germany. His research focuses on the molecular mechanisms of GPCR-activation, G-protein function and adenylyl cyclase regulation.

Thomas Wieland was born in 1960 in Karlsruhe, Germany. He studied Pharmacy at the University of Heidelberg where he obtained his PhD in Pharmacology in 1989. From 1990-1996 he worked in the group of Professor Karl H. Jakobs in the Department of Pharmacology of the Universities of Heidelberg and Essen, Germany. From 1996 -1997, he was a research fellow with Dr. Melvin I. Simon at the California Institute of Technology, Pasadena, CA, USA. From 1997 - 2002 he was Professor in the Department of Pharmacology and Toxicology of the University of Hamburg, Germany. Since July 2002 he is Professor of Pharmacology and Toxicology at the University of Heidelberg, Germany. His research focuses on the GPCR induced activation of heterotrimeric G-proteins and monomeric GTPases and the regulation of these processes by accessory proteins.
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"In conclusion, this volume can be highly useful resource for pharmaceuticals chemists, physiologists and medical researchers working both in academia and industry."
International Journal of Biological Macromolecules

"...extremely informative and generally easy to read and understand. It is an important reference book for researchers (medicinal chemists, physiologists, and pharmacologists) working on the most favorite group of drug targets - the GPCRs."
ChemMedChem

"This book is an excellent review of the body of evidence describing constitutive GPCR activity. It is of general interest to pharmacologists, structural biologists, biochemists, and medicinal chemists with an interest in GPCR signaling pathways and as such would be a good addition to personal or departmental libraries of many basic scientists."
Journal of Medicinal Chemistry

"I can strongly recommend this book as the concepts and examples have mostly been poorly taken into account with the daily work in the laboratory. The book would have great use in pharmacologically oriented laboratories in academics as well as different stages in drug development in pharmaceutical industry. It is more or less a "must" in the libraries in academia and in industry looking on all kinds of GPCR research."
Arch. Pharm. Chem. Life Sci.
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