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Structure and Function of GPCRs

  • Book
  • © 2019

Overview

Editors:
  1. Guillaume Lebon

    1. Institut de Génomique Fonctionnelle Centre National de la Recherche Scientifique (CNRS), Institut National de la Santé et de la Recherche Médicale (INSERM), University of Montpellier, Montpellier, France

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  • Reviews the structural basis of ligand binding and allosteric mechanisms
  • Presents concrete examples of structure-based drug discovery
  • Illustrates GPCR biased signaling in physiological contexts

Part of the book series: Topics in Medicinal Chemistry (TMC, volume 30)

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Table of contents (10 chapters)

  1. Front Matter

    Pages i-xiv
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  2. Structures of Non-rhodopsin GPCRs Elucidated Through X-Ray Crystallography

    • Chady Nasrallah, Guillaume Lebon
    Pages 1-26

  3. NMR Spectroscopy for the Characterization of GPCR Energy Landscapes

    • Marina Casiraghi, Jean-Louis Banères, Laurent J. Catoire
    Pages 27-52

  4. Structure and Activation Mechanism of GPCRs

    • A. J. Venkatakrishnan
    Pages 53-64

  5. Structure-Based Discovery of GPCR Ligands from Crystal Structures and Homology Models

    • Anirudh Ranganathan, David Rodríguez, Jens Carlsson
    Pages 65-99

  6. Integration on Ligand and Structure Based Approaches in GPCRs

    • Anil K. Saxena, Shome S. Bhunia, Mridula Saxena
    Pages 101-161

  7. Biased Agonist Pharmacochaperones: Small Molecules in the Toolbox for Selectively Modulating GPCR Activity

    • Bernard Mouillac, Christiane Mendre
    Pages 163-180

  8. Endosomal PTH Receptor Signaling Through cAMP and Its Consequence for Human Medicine

    • Ieva Sutkeviciute, Frederic G. Jean-Alphonse, Jean-Pierre Vilardaga
    Pages 181-193

  9. Structure and Function Studies of GPCRs by Site-Specific Incorporation of Unnatural Amino Acids

    • Meilin Tian, Qian Wang, Chonggang Yuan, Shixin Ye
    Pages 195-215

  10. Fluorescent-Based Strategies to Investigate G Protein-Coupled Receptors: Evolution of the Techniques to a Better Understanding

    • Orestis Faklaris, Joyce Heuninck, Amandine Falco, Elise Goyet, Jurriaan M. Zwier, Jean-Philippe Pin et al.
    Pages 217-252

  11. Modulation of Metabotropic Glutamate Receptors by Orthosteric, Allosteric, and Light-Operated Ligands

    • Cyril Goudet, Xavier Rovira, Philippe Rondard, Jean-Philippe Pin, Amadeu Llebaria, Francine Acher
    Pages 253-284

  12. Back Matter

    Pages 285-289
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Keywords

About this book

This book introduces readers to the latest advances in G protein-coupled receptor (GPCR) biology. It reviews our current understanding of the structural basis of ligand binding and allosteric mechanisms, following a decade of technological breakthroughs. Several examples of structure-based drug discovery are presented, together with the future challenges involved in designing better drugs that target GPCRs. In turn, the book illustrates the important concept of GPCR biased signaling in physiological contexts, and presents fluorescent- and light-based methodologies frequently used to measure GPCR signaling or to trace their dynamics in cells upon ligand activation. 


Taken together, the chapters provide an essential overview and toolkit for new scientific investigators who plan to develop GPCR projects. All chapters were written by experts in their respective fields, and share valuable insights and powerful methodologies for the GPCR field.

Editors and Affiliations

  • Institut de Génomique Fonctionnelle Centre National de la Recherche Scientifique (CNRS), Institut National de la Santé et de la Recherche Médicale (INSERM), University of Montpellier, Montpellier, France

    Guillaume Lebon

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