Details

G Protein-Coupled Receptors as Drug Targets

Analysis of Activation and Constitutive Activity
Methods & Principles in Medicinal Chemistry, Band 24 1. Aufl.

von: Roland Seifert, Thomas Wieland, Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
214,99 €
Verlag:	Wiley-VCH
Format:	PDF
Veröffentl.:	12.05.2006
ISBN/EAN:	9783527606955
Sprache:	englisch
Anzahl Seiten:	304

In den Warenkorb

DRM-geschütztes eBook, Sie benötigen z.B. Adobe Digital Editions und eine Adobe ID zum Lesen.

Beschreibungen

Titelbeschreibung

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.

Inhaltsverzeichnis

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.

Rezension

"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.

Autorenportrait

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 Gunter 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.

Back cover copy

G protein-coupled receptors (GPCRs) are important conformational "switches" in transmembrane signal transduction and represent the largest gene family in the human genome reflecting the importance of GPCRs as targets for hormones, neurotransmitters and local mediators in virtually any cell type of the human body. Since GPCRs discriminate well between natural and synthetic ligands and because of their localization in the plasma membrane, they are the single most important class of drug targets. With its particular emphasis on the constitutive activity of GPCRs, this book recognizes a biological process that has not yet been covered by existing books on GPCRs. An international team of highly distinguished authors discusses current models and concepts in detail, introducing the advances made in our understanding GPCR activation and constitutive activity. In addition, the text provides an overview on the methods of investigating GPCR activity. From the contents: PART I: GENERAL CONCEPTS Models of constitutive activity Molecular mechanisms of GPCR activation Impact of G proteins on constitutive GPCR activity Physiological and therapeutic relevance of constitutive GPCR activity Methodological Approaches PART II: SELECTED GPCR SYSTEMS Chemokine receptors and human disease a-Adrenoceptors ?-Adrenoceptors Muscarinic Acetylcholine Receptors Histamine receptors 5-HT receptors Virally pirated Chemokine receptors and human disease Illustrated by numerous experimental examples, schemes and methodological advice for analyzing GPCRs, this is a highly practical reference for pharmaceutical chemists, physiologists and medical researchers in academia and industry.