G protein coupled receptors remain the most important class of therapeutic targets in medicine. In the last 5 years, tremendous advances have been made in our understanding of the structure and mechanism of this critical family of drug targets. The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors. It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones. In addition, emerging drug targets such as receptor families for fatty acids, carboxylic acids, lipid mediators, etc. are included. Final chapters cover novel mechanisms of signal regulation through PDZ domains and RGS proteins. This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists.


Pharmacologists, immunologists, and biochemists

Included in series
Advances in Pharmacology

Hardbound, 408 Pages

Published: September 2011

Imprint: Academic Press

ISBN: 978-0-12-385952-5


    1. The Use of GPCR Structures in Drug Design
      Miles Congreve, Christopher Langmead and Fiona Marshall
    2. Allosteric Modulation of Metabotropic Glutamate Recetors
      Douglas J. Sheffler, Karen J. Gregory, Jerri M. Rook, and P. Jeffrey Conn
    3. Refining Efficacy: Exploiting Functional Selectivity for Drug Discovery
      Diane Gesty-Palmer and Louis M. Luttrell
    4. Pharmacoperones for Misfolded Gonadotropin - Releasing Hormone Receptors
      P. Michael Conn and Alfredo Ulloa-Aguirre
    5. Regulation of Stability and Trafficking of Calcium Sensing Receptors by Pharmacologic Chaperones
      Ying Huang, Alice Cavanaugh, and Gerda E. Breitwieser
    6. Experimental Challenges to Targeting Poorly Characterised GPCRs: Therapeutic Potential for Free Fatty Acid Receptor
      Brian D. Hudson, Nicola J. Smith and Graeme Milligan
    7. Biological and Pharmacological Roles of HCA Receptors
      Clara Blad, Kashan Ahmed, Ad IJzerman, and Stefan Offermanns
    8. Pharmacology, Signaling and Physiological Relevance of the G Protein-Coupled Receptor 55 (GPR55)
      Nariman Balenga, Julia Kargl and Maria Waldhoer
    9. Role of PDZ Proteins in Regulating Signaling, Trafficking, and Function of GPCRs
      Paul Temkin, Mark von Zastrow, Peter A. Friedman, and Guillermo Romero
    10. Regulator of G Protein Signaling Proteins as Drug Targets: Current State and Future Possibilities
      Benita Sjögren
    11. GPCR-Interacting Proteins, Major Players in GPCR Function
      Pascal Maurice, Maud Kamal, Avais Daulat, Jean-Luc Guillaume, and Ralf Jockers


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