A comprehensive survey of the advances in the field of G protein-coupled receptors (GPCR). This work describes the knowledge of GPCR receptor structure and function, the different mechanisms involved in the regulation of GPCR function, and the role of pharmacological chaperones in GPCR folding and maturation.

This work is a comprehensive survey of the many recent advances in the field of G protein-coupled receptors (GPCR). The authors describe the current knowledge of GPCR receptor structure and function, the different mechanisms involved in the regulation of GPCR function, and the role of pharmacological chaperones in GPCR folding and maturation. They also present new findings about how GPCR dimerization/oligomerization modifies the properties of individual receptors and show how recent developments are leading to significant advances in drug discovery, such as the detection of ligands for orphan GPCRs. Also discussed are the most recent developments that could lead to new drug discoveries: the role of GPCRs in mediating pain, the development of receptor-type selective drugs based on the structural plasticity of receptor activation, and the identification of natural ligands of orphan GPCRs (deorphanization) as possible drug targets.

Part I. GPCRs: Structure and Function
Structure Function Relationships in G Protein-Coupled Receptors: Ligand Binding and Receptor Activation
Dominique Massote and Brigitte L. Kieffer
Molecular Mechanisms Involved in the Activation of Rhodopsin-Like Seven Transmembrane Receptors
Peng Huang and Lee-Yuan Liu-Chen
GPCR Folding and Maturation: The Effect of Pharmacological Chaperones
Ulla E. Petaja-Repo and Michel Bouvier
Regulated Membrane Trafficking and Proteolysis of G Protein-Coupled Receptors
MarK von Zastrow
Part II. GPCR Activity and Its Regulators
Heterotrimeric G Proteins and Their Effector Pathways
Tracy Nguyen Hwang po and Ravi Iyengar
RGS Proteins: Orchestration of Multiple Signaling Pathways
Ryan W. Richman and Maria A. Diverse-Pierluissi
G Protein-Coupled Receptor Kinases
Lan Ma, Jingxia Gao, and Xiaoqing Chen
Regulators of G Protein-Coupled Receptor Activity: The Arrestins
Louis M. Luttrell
G Protein-Coupled Receptor Interacting Proteins: Class, Assembly, and Function
Hongyan Wang, Catherine B. Willmore, and Jia Bei Wang
Part III. GPCR Dimerization/Oligomerization
Biophysical and Biochemical Methods to Study G Protein-Coupled Receptor Oligomerization
Karen M. Kroeger, Kevin D. G. Pfleger, and Karen A. Eidne
Oligomerization Domains of G Protein-Coupled Receptors: Insights into the Structural Basis of GPCR Association
Marta Filizola, Wen Guo, Jonathan A. Javitch, and Harel Weinstein
Functional Complementation and Analysis of G Protein-Coupled Receptor Dimerization
Graeme Milligan, Juan J. Carrillo, and Geraldine Pascal
The Role of Oligomerization in G Protein-Coupled Receptor Maturation
Michael M. C. Kong, Christopher H. So, Brian F. O'Dowd, and Susan R. George
GPCR Oligomerization and Trafficking
Selena E. Barlett and Jennifer L. Whistler
Modulation of Receptor Pharmacology by G Protein-Coupled Receptor Dimerization
Noura S. Abul-Husn, Achla Gupta, Lakshmi A. Devi, and Ivone Gomes
Part IV. Recent Developments in Drug Discovery
Role of Heteromeric G Protein-Coupled Receptor Interactions in Pain/Analgesia
Andrew P. Smith and Nancy M. Lee
Conformational Plasticity of G Protein-Coupled Receptor Binding Sites: Structural Basis for Evolutionary Diversity in Ligand Recognition
Xavier Deupi, Cedric Govaerts, Lei Shi, Jonathan A. Javitch, Leonardo Pardo, and Juan Ballesteros
Deorphanizing G Protein-Coupled Receptors and Drug Development
Rainer K. Reinscheid and Olivier Civelli