© 2019

Structure and Function of GPCRs

  • Guillaume Lebon

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

Table of contents

  1. Front Matter
    Pages i-xiv
  2. Marina Casiraghi, Jean-Louis Banères, Laurent J. Catoire
    Pages 27-52
  3. A. J. Venkatakrishnan
    Pages 53-64
  4. Anirudh Ranganathan, David Rodríguez, Jens Carlsson
    Pages 65-99
  5. Anil K. Saxena, Shome S. Bhunia, Mridula Saxena
    Pages 101-161
  6. Ieva Sutkeviciute, Frederic G. Jean-Alphonse, Jean-Pierre Vilardaga
    Pages 181-193
  7. Meilin Tian, Qian Wang, Chonggang Yuan, Shixin Ye
    Pages 195-215
  8. Orestis Faklaris, Joyce Heuninck, Amandine Falco, Elise Goyet, Jurriaan M. Zwier, Jean-Philippe Pin et al.
    Pages 217-252
  9. Cyril Goudet, Xavier Rovira, Philippe Rondard, Jean-Philippe Pin, Amadeu Llebaria, Francine Acher
    Pages 253-284
  10. Back Matter
    Pages 285-289

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.


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

Editors and affiliations

  • Guillaume Lebon
    • 1
  1. 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 MontpellierMontpellierFrance

Bibliographic information

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