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G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and
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G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity Hardcover - 2006

by Roland Seifert (Editor); Thomas Wieland (Editor); Raimund Mannhold (Editor)


From the publisher

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.

From the rear cover

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.

Details

  • Title G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity
  • Author Roland Seifert (Editor); Thomas Wieland (Editor); Raimund Mannhold (Editor)
  • Binding Hardcover
  • Edition Volume 24
  • Pages 304
  • Volumes 1
  • Language ENG
  • Publisher Wiley-Vch
  • Date January 9, 2006
  • Illustrated Yes
  • ISBN 9783527308194 / 3527308199
  • Weight 1.5 lbs (0.68 kg)
  • Dimensions 9.6 x 6.9 x 0.8 in (24.38 x 17.53 x 2.03 cm)
  • Library of Congress subjects G proteins, Drug targeting
  • Library of Congress Catalog Number 2006295093
  • Dewey Decimal Code 615.7

About the author

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.
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G-protein-coupled receptors as drug targets; analysis of activation and constitutive activity
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G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity (Methods and Principles in Medicinal Chemistry) (v. 24)

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

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G PROTEIN-COUPLED RECEPTORS AS DRUG TARGETS, V 24
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G PROTEIN-COUPLED RECEPTORS AS DRUG TARGETS, V 24

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G PROTEIN-COUPLED RECEPTORS AS DRUG TARGETS, V 24
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G PROTEIN-COUPLED RECEPTORS AS DRUG TARGETS, V 24

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