Structure and Function of GPCRs

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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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.

• Aminoacids Incorporation
• Class C GPRC activation mechanism
• Endocytic Pathway
• Femtosecond Crystallography
• GPCR Activation
• GPCR Agonists
• GPCR Ligands
• Pharmacochaperons
• Rhodopsin
• Time resolved fluorescence microscopy

• 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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