Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors - 1st Edition - ISBN: 9780123945877, 9780123947918

Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors, Volume 115

1st Edition

Serial Volume Editors: Terry Kenakin
Hardcover ISBN: 9780123945877
eBook ISBN: 9780123947918
Imprint: Academic Press
Published Date: 28th February 2013
Page Count: 488
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Table of Contents

  • Contributors
  • Preface
  • Chapter One. Approaches for Probing Allosteric Interactions at 7 Transmembrane Spanning Receptors
    • 1 Introduction
    • 2 General Considerations for Assays Designed to Identify and Characterize Allosteric Modulators
    • 3 General Workflow Used in Identifying and Characterizing Allosteric Modulators
    • 4 Data Analysis: General Features for Allosteric Interactions
    • 5 Kinetic Assays to Measure Allosteric Interactions at 7TMRs
    • 6 Label-Free Technology
    • 7 Endpoint Assays
    • 8 Radioligand Binding Assays for Allosteric Interactions
    • 9 Competitive or Not Competitive
    • 10 Conclusions and Future Directions
    • References
  • Chapter Two. Pharmacology of Metabotropic Glutamate Receptor Allosteric Modulators
    • Abbreviations
    • 1 Introduction
    • 2 Physiology and Pharmacology of mGlus
    • 3 Allosteric Modulation of mGlus
    • 4 Location of Allosteric Sites
    • 5 Therapeutic Indications for Allosteric Modulators
    • 6 Concluding Remarks
    • References
  • Chapter Three. Mining the Potential of Label-Free Biosensors for Seven-Transmembrane Receptor Drug Discovery
    • 1 Introduction
    • 2 Promises of Label-Free Screening
    • 3 Challenges of Label-Free Screening
    • 4 The Value Proposition of Label-Free to Drug Discovery
    • 5 Concluding Remarks
    • References
  • Chapter Four. G Protein-Coupled Receptors in Cancer
    • 1 General Introduction
    • 2 Biochemical Interactions
    • 3 Drug Design
    • References
  • Chapter Five. GPCRs in Stem Cell Function
    • Abbreviations
    • 1 Introduction
    • 2 Types of Stem Cells
    • 3 GPCRs in Embryonic Stem Cells
    • 4 GPCRs in Induced Pluripotent Stem Cells
    • 5 GPCRs in Adult Stem Cells
    • 6 GPCRs in Cancer Stem Cells
    • 7 Summary
    • References
  • Chapter Six. Application of Receptor Theory to Allosteric Modulation of Receptors
    • 1 Introduction
    • 2 The Allosteric Two-State Model
    • 3 Operational Models of Receptor Activation with Constitutive Activity
    • 4 Further Exploration of the cTCM
    • 5 Summary
    • References
  • Chapter Seven. What Ligand-Gated Ion Channels Can Tell Us About the Allosteric Regulation of G Protein-Coupled Receptors
    • 1 Introduction
    • 2 Drug-Induced Conformational Changes in Receptor Activity
    • 3 Ligand-Gated Ion Channels
    • 4 G Protein-Coupled Receptors
    • 5 Conclusions
    • References
  • Chapter Eight. Modeling Cooperativity Effects in Dimeric G Protein-Coupled Receptors
    • 1 Introduction
    • 2 Modeling Cooperativity Effects in Monomeric GPCRs: The Allosteric Two-State Model
    • 3 Modeling Cooperativity Effects in Dimeric GPCRs
    • 4 Conclusions
    • References
  • Chapter Nine. Chemokine Receptor Oligomerization and Allostery
    • 1 Introduction
    • 2 Background: Chemokine Structure and Interactions with Receptors
    • 3 Evidence for Hetero- and Homo-Oligomerization of Chemokine Receptors
    • 4 Functional Effects of Chemokine Receptor Hetero-Oligomerization on Ligand Binding
    • 5 Effects of Chemokine Hetero- and Homo-Oligomerization on Signaling
    • 6 Heterodimerization of Chemokine Receptors with Nonchemokine Receptors
    • 7 Other Sources of Allostery in Chemokine Receptor Signaling: Chemokine Oligomerization
    • 8 Conclusions and Future Perspectives
    • References
  • Chapter Ten. Fine-Tuning of GPCR Signals by Intracellular G Protein Modulators
    • 1 Introduction: Heterotrimeric G Proteins and Their Binding Partners
    • 2 Organization of G Protein-Mediated Signals
    • 3 RGS Proteins
    • 4 GPSM Proteins
    • 5 Nonreceptor GEFs
    • 6 Interactions Between G Protein Modulatory Domains
    • 7 Conclusions
    • References
  • Index

Description

  • Contributors
  • Preface
  • Chapter One. Approaches for Probing Allosteric Interactions at 7 Transmembrane Spanning Receptors
    • 1 Introduction
    • 2 General Considerations for Assays Designed to Identify and Characterize Allosteric Modulators
    • 3 General Workflow Used in Identifying and Characterizing Allosteric Modulators
    • 4 Data Analysis: General Features for Allosteric Interactions
    • 5 Kinetic Assays to Measure Allosteric Interactions at 7TMRs
    • 6 Label-Free Technology
    • 7 Endpoint Assays
    • 8 Radioligand Binding Assays for Allosteric Interactions
    • 9 Competitive or Not Competitive
    • 10 Conclusions and Future Directions
    • References
  • Chapter Two. Pharmacology of Metabotropic Glutamate Receptor Allosteric Modulators
    • Abbreviations
    • 1 Introduction
    • 2 Physiology and Pharmacology of mGlus
    • 3 Allosteric Modulation of mGlus
    • 4 Location of Allosteric Sites
    • 5 Therapeutic Indications for Allosteric Modulators
    • 6 Concluding Remarks
    • References
  • Chapter Three. Mining the Potential of Label-Free Biosensors for Seven-Transmembrane Receptor Drug Discovery
    • 1 Introduction
    • 2 Promises of Label-Free Screening
    • 3 Challenges of Label-Free Screening
    • 4 The Value Proposition of Label-Free to Drug Discovery
    • 5 Concluding Remarks
    • References
  • Chapter Four. G Protein-Coupled Receptors in Cancer
    • 1 General Introduction
    • 2 Biochemical Interactions
    • 3 Drug Design
    • References
  • Chapter Five. GPCRs in Stem Cell Function
    • Abbreviations
    • 1 Introduction
    • 2 Types of Stem Cells
    • 3 GPCRs in Embryonic Stem Cells
    • 4 GPCRs in Induced Pluripotent Stem Cells
    • 5 GPCRs in Adult Stem Cells
    • 6 GPCRs in Cancer Stem Cells
    • 7 Summary
    • References
  • Chapter Six. Application of Receptor Theory to Allosteric Modulation of Receptors
    • 1 Introduction
    • 2 The Allosteric Two-State Model
    • 3 Operational Models of Receptor Activation with Constitutive Activity
    • 4 Further Exploration of the cTCM
    • 5 Summary
    • References
  • Chapter Seven. What Ligand-Gated Ion Channels Can Tell Us About the Allosteric Regulation of G Protein-Coupled Receptors
    • 1 Introduction
    • 2 Drug-Induced Conformational Changes in Receptor Activity
    • 3 Ligand-Gated Ion Channels
    • 4 G Protein-Coupled Receptors
    • 5 Conclusions
    • References
  • Chapter Eight. Modeling Cooperativity Effects in Dimeric G Protein-Coupled Receptors
    • 1 Introduction
    • 2 Modeling Cooperativity Effects in Monomeric GPCRs: The Allosteric Two-State Model
    • 3 Modeling Cooperativity Effects in Dimeric GPCRs
    • 4 Conclusions
    • References
  • Chapter Nine. Chemokine Receptor Oligomerization and Allostery
    • 1 Introduction
    • 2 Background: Chemokine Structure and Interactions with Receptors
    • 3 Evidence for Hetero- and Homo-Oligomerization of Chemokine Receptors
    • 4 Functional Effects of Chemokine Receptor Hetero-Oligomerization on Ligand Binding
    • 5 Effects of Chemokine Hetero- and Homo-Oligomerization on Signaling
    • 6 Heterodimerization of Chemokine Receptors with Nonchemokine Receptors
    • 7 Other Sources of Allostery in Chemokine Receptor Signaling: Chemokine Oligomerization
    • 8 Conclusions and Future Perspectives
    • References
  • Chapter Ten. Fine-Tuning of GPCR Signals by Intracellular G Protein Modulators
    • 1 Introduction: Heterotrimeric G Proteins and Their Binding Partners
    • 2 Organization of G Protein-Mediated Signals
    • 3 RGS Proteins
    • 4 GPSM Proteins
    • 5 Nonreceptor GEFs
    • 6 Interactions Between G Protein Modulatory Domains
    • 7 Conclusions
    • References
  • Index

Key Features

  • Contributions from leading authorities
  • Informs and updates on all the latest developments in the field

Readership

Researchers of G-protein receptors, molecular biology, and translational science


Details

No. of pages:
488
Language:
English
Copyright:
© Academic Press 2013
Published:
Imprint:
Academic Press
eBook ISBN:
9780123947918
Hardcover ISBN:
9780123945877

Reviews

Praise for the series:
"Full of interest not only for the molecular biologist-for whom the numerous references will be invaluable-but will also appeal to a much wider circle of biologists, and in fact to all those who are concerned with the living cell." --British Medical Journal


About the Serial Volume Editors

Terry Kenakin Serial Volume Editor

Terry P. Kenakin is the recipient of the 2008 Poulsson Medal for Pharmacology awarded by the Norwegian Society of Pharmacology for achievements in basic and clinical pharmacology and toxicology. He has also been awarded the 2011 Ariens Award from the Dutch Pharmacological Society and the 2014 Gaddum Memorial Award from the British Pharmacological Society. Having been involved in drug discovery for over 30 years, his interests include the optimal design of drug activity assays systems and quantitative drug receptor theory. He is a member of numerous editorial boards as well as Editor-in-Chief of the Journal of Receptors and Signal Transduction and Current Opinion in Pharmacology. In addition, Dr. Kenakin has authored numerous articles and has also written a number of books on pharmacology.

Affiliations and Expertise

Professor of Pharmacology, The University of North Carolina School Of Medicine, Chapel Hill, NC, USA