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

1st Edition

Serial Volume Editors: Terry Kenakin
Print ISBN: 9780123945877
eBook ISBN: 9780123947918
Imprint: Academic Press
Published Date: 28th February 2013
Page Count: 488
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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.

Key Features

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


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


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© Academic Press 2013
Academic Press
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About the Serial Volume Editor

Terry Kenakin

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


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