Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors
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Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors

First published on December 2, 2012

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  • Editor: Terry Kenakin
  • eBook ISBN: 9780123947918
  • Hardcover ISBN: 9780123945877

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Description

In this thematic volume of Progress in Molecular Biology and Translational Science, researchers reflect on recent developments and research surrounding G protein-coupled receptors. The chapters cover a large breadth of research, including GPCR role in stem cell function and pharmacology. Authors explore in-depth research techniques and applications of GPCR usage, covering theory, laboratory approaches, and unique qualities that make GPCRs a crucial tool in microbiological and cancer research.

Readership

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

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

Product details

  • No. of pages: 488
  • Language: English
  • Copyright: © Academic Press 2013
  • Published: December 2, 2012
  • Imprint: Academic Press
  • eBook ISBN: 9780123947918
  • Hardcover ISBN: 9780123945877

About the Serial Volume Editor

Terry Kenakin

Terry Kenakin
Dr. Terry Kenakin is Professor of Pharmacology at the University of North Carolina School of Medicine. Prior to this, he spent 7 years in drug discovery at Burroughs-Wellcome. He then moved to GlaxoSmithKline for 25 years. Dr. Kenakin has written 11 books on Pharmacology, is the Editor in Chief of the Journal of Receptors and Signal Transduction, is on numerous Editorial Boards. He is the Editor-in-Chief of Comprehensive Pharmacology (Elsevier, 2022). He 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, and the 2020 Goodman and Gilman Award in Receptor Pharmacology from ASPET.

Affiliations and Expertise

Professor, Pharmacology, University of North Carolina, USA

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