Main description:

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.

Contents:

Part I. GPCRs: Structure and Function

Structure-Function Relationships in G Protein-Coupled Receptors: Ligand Binding and Receptor Activation
Dominique Massotte 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 GPCRs
James N. Hislop and Mark von Zastrow

Part II. GPCR Activity and Its Regulators

Heterotrimeric G Proteins and Their Effector Pathways
Tracy Nguyen Hwangpo 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 GPCR Activity: The Arrestins
Louis M. Luttrell

GPCR Interacting Proteins: Classes, Assembly, and Functions
Hongyan Wang, Catherine B. Willmore, and Jia Bei Wang

Part III. GPCR Dimerization/Oligomerization

Biophysical and Biochemical Methods to Study GPCR Oligomerization
Karen M. Kroeger, Kevin D. G. Pfleger, and Karin 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 the Analysis of GPCR 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

Receptor Oligomerization and Trafficking
Selena E. Barlett and Jennifer L. Whistler

Modulation of Receptor Pharmacology byG 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 GPCR Interactions in Pain/Analgesia
Andrew P. Smith and Nancy M. Lee

Conformational Plasticity of GPCR Binding Sites: Structural Basis for Evolutionary Diversity in Ligand Recognition
Xavier Deupi, Cedric Govaerts, Lei Shi, Jonathan A. Javitch, Leonardo Pardo, and Juan Ballesteros

De-Orphanizing GPCRs and Drug Development
Rainer K. Reinscheid and Olivier Civelli

Index