Pharmacology of G Protein Coupled Receptors, Volume 62

1st Edition

Serial Volume Editors: S. J. Enna
Hardcover ISBN: 9780123859525
eBook ISBN: 9780123859532
Imprint: Academic Press
Published Date: 19th September 2011
Page Count: 408
250.86 + applicable tax
190.00 + applicable tax
151.00 + applicable tax
249.00 + applicable tax
Unavailable
Compatible Not compatible
VitalSource PC, Mac, iPhone & iPad Amazon Kindle eReader
ePub & PDF Apple & PC desktop. Mobile devices (Apple & Android) Amazon Kindle eReader
Mobi Amazon Kindle eReader Anything else

Institutional Access


Table of Contents

Contributors

Preface

The Use of GPCR Structures in Drug Design

Abbreviations

I. Introduction

II. Technology Developments Enabling GPCR Structure Determination

III. GPCR Structures

IV. GPCR Structures in Drug Discovery

V. Conclusion

Acknowledgments

Allosteric Modulation of Metabotropic Glutamate Receptors

Abbreviations

I. Introduction

II. Metabotropic Glutamate Receptors

III. Pharmacological Profiles of mGlu Allosteric Modulators

IV. Quantifying Allosteric Interactions

V. Structural Determinants of mGlu Allosteric Modulator Binding

VI. Functional Selectivity of mGlu Allosteric Modulation

VII. Therapeutic Potential of mGlu Allosteric Modulators

VIII. Conclusion

Acknowledgments

Refining Efficacy

Abbreviations

I. Introduction

II. GPCRs as Conformational Ensembles

III. The Pluridimensional Nature of GPCR Efficacy

IV. Functionally Selective GPCR Agonism

V. Functional Selectivity and Pharmaceutical Development

VI. Functional Selectivity at the Parathyroid Hormone Receptor

VII. Conclusion

Acknowledgments

Pharmacological Chaperones for Misfolded Gonadotropin-Releasing Hormone Receptors

Abbreviations

I. Introduction

II. The Endoplasmic Reticulum Quality Control System

III. Misfolding of GPCRs and Disease

IV. Mutations in the Human GnRHR

V. Rescue of Misfolded hGnRHR Mutants with Pharmacoperones

VI. Mechanism of Action of Pharmacoperones

VII. The Dominant-Negative Effect of hGnRHR Mutants and Receptor Rescue

VIII. Conclusion

Acknowledgments

Regulation of Stability and Trafficking of Calcium-Sensing Receptors by Pharmacologic Chaperones

Abbreviations

I. Introduction


Description

G protein coupled receptors remain the most important class of therapeutic targets in medicine. In the last 5 years, tremendous advances have been made in our understanding of the structure and mechanism of this critical family of drug targets. The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors. It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones. In addition, emerging drug targets such as receptor families for fatty acids, carboxylic acids, lipid mediators, etc. are included. Final chapters cover novel mechanisms of signal regulation through PDZ domains and RGS proteins. This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists.

Key Features

  • The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors
  • It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones
  • This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists

Readership

Pharmacologists, immunologists, and biochemists


Details

No. of pages:
408
Language:
English
Copyright:
© Academic Press 2011
Published:
Imprint:
Academic Press
eBook ISBN:
9780123859532
Hardcover ISBN:
9780123859525

About the Serial Volume Editors

S. J. Enna Serial Volume Editor

Dr. S. J. Enna received his B.A. degree (1965, Biology) from Rockhurst University, Kansas City, Missouri and both his M.S. (1967, Pharmacology) and Ph.D. (1970, Pharmacology) degrees from the University of Missouri-Kansas City. Postdoctoral training in pharmacology was completed at the University of Texas Southwestern Medical School in Dallas, at F. Hoffmann La Roche in Basel, Switzerland, and the Department of Pharmacology and Experimental Therapeutics at Johns Hopkins University School of Medicine in Baltimore. Dr. Enna spent 10 years on the faculty at the University of Texas Medical School at Houston in the Departments of Pharmacology and Neurobiology. While at the University of Texas Dr. Enna was also a consultant for ICI USA, Inc., Merck, Sharp and Dohme Research Laboratories, Bristol Myers Corporation, and Panlabs, Inc. From 1986 1990, Dr. Enna was Senior Vice President and Scientific Director of Nova Pharmaceutical Corporation in Baltimore, and Executive Vice President from 1990 1992. He is currently Associate Dean for Research and Graduate Education as well as Professor of Physiology and of Pharmacology at the University of Kansas Medical School. Dr. Enna served as chair of the Department of Pharmacology, Toxicology and Therapeutics at the University of Kansas Medical School from 1992 to 2003. Other previous academic appointments include Lecturer in the Department of Neuroscience at The Johns Hopkins University School of Medicine in Baltimore and Adjunct Professor of Pharmacology at Tulane University School of Medicine in New Orleans. Dr. Enna served for six years as editor of The Journal of Pharmacology and Experimental Therapeutics, and is currently co-editor of Current Protocols in Pharmacology. He is also Editor-in-Chief of Biochemical Pharmacology, Executive Editor-in-Chief of Pharmacology and Therapeutics and Series Editor of Advances in Pharmacology. Besides his editorships, Dr. Enna serves on the editorial boards of Brain Research, Life Sci

Affiliations and Expertise

Department of Pharmacology, Toxicology and Therapeutics, University of Kansas Medical Center, USA