G Protein-coupled Receptors as Drug Targets

Beschreibung

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 ß-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.
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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Roland Seifert

Themen in »G Protein-coupled Receptors as Drug Targets«

Biochemie Biowissenschaften Chemie Chemistry Drug Discovery & Development Endocrinology Endokrinologie Enzyme u. Rezeptoren Enzymes & Receptors Life Sciences Medical Science Medizin Medizinische Chemie Molecular Biology Molekularbiologie

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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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"Anders als bei anderen vergleichsweisen Buchveröffentlichungen hat man hier immer das Gefühl der Homogenität und Harmonie der Darstellungen der verschiedenen Autoren in den verschiedenen Kapiteln. Gute und ausführliche Quellenhinweise, einwandfreie Abbildungen und Darstellungen sowie das hilfreiche Abkürzungsglossar zu Anfang machen dieses Buch zu einer Pflichtlektüre für Zellbiologen, Pharmakologen und fachinteressierte Studierende." Umwelt & Gesundheit
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