Part I. GPCRs: Structure and Functionn n Structure-Function Relationships in G Protein-Coupled Receptors: Ligand Binding and Receptor Activationn Dominique Massotte and Brigitte L. Kieffern n Molecular Mechanisms Involved in the Activation of Rhodopsin-Like Seven-Transmembrane Receptorsn Peng Huang and Lee-Yuan Liu-Chenn n GPCR Folding and Maturation: The Effect of Pharmacological Chaperonesn Ulla E. Petäjä-Repo and Michel Bouviern n Regulated Membrane Trafficking and Proteolysis of GPCRsn James N. Hislop and Mark von Zastrown n Part II. GPCR Activity and Its Regulatorsn n Heterotrimeric G Proteins and Their Effector Pathwaysn Tracy Nguyen Hwangpo and Ravi Iyengarn n RGS Proteins: Orchestration of Multiple Signaling Pathwaysn Ryan W. Richman and Mariá A. Diversé-Pierluissin n G Protein-Coupled Receptor Kinasesn Lan Ma, Jingxia Gao, and Xiaoqing Chenn n Regulators of GPCR Activity: The Arrestinsn Louis M. Luttrelln n GPCR Interacting Proteins: Classes, Assembly, and Functionsn Hongyan Wang, Catherine B. Willmore, and Jia Bei Wangn n Part III. GPCR Dimerization/Oligomerizationn n Biophysical and Biochemical Methods to Study GPCR Oligomerizationn Karen M. Kroeger, Kevin D. G. Pfleger, and Karin A. Eidnen n Oligomerization Domains of G Protein-Coupled Receptors: Insights Into the Structural Basis of GPCR Associationn Marta Filizola, Wen Guo, Jonathan A. Javitch, and Harel Weinsteinn n Functional Complementation and the Analysis of GPCR Dimerizationn Graeme Milligan, Juan J. Carrillo, and Geraldine Pascaln n The Role of Oligomerization in G Protein-Coupled Receptor Maturationn Michael M. C. Kong, Christopher H. So, Brian F. O'Dowd, and Susan R. Georgen n Receptor Oligomerization and Traffickingn Selena E. Barlett and Jennifer L. Whistlern n Modulation of Receptor Pharmacology byG Protein-Coupled Receptor Dimerizationn Noura S. Abul-Husn, Achla Gupta, Lakshmi A. Devi and Ivone Gomesn n Part IV. Recent Developments in Drug Discoveryn n Role of Heteromeric GPCR Interactions in Pain/Analgesian Andrew P. Smith and Nancy M. Leen n Conformational Plasticity of GPCR Binding Sites: Structural Basis for Evolutionary Diversity in Ligand Recognitionn Xavier Deupi, Cedric Govaerts, Lei Shi, Jonathan A. Javitch, Leonardo Pardo, and Juan Ballesterosn n De-Orphanizing GPCRs and Drug Developmentn Rainer K. Reinscheid and Olivier Civellin n Index
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.