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Humana Press The G Protein-Coupled Receptors Handbook by Lakshmi A. Devi
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.show more Part I. GPCRs: Structure and FunctionStructure-Function Relationships in G Protein-Coupled Receptors: Ligand Binding and Receptor ActivationDominique Massotte and Brigitte L. KiefferMolecular Mechanisms Involved in the Activation of Rhodopsin-Like Seven-Transmembrane ReceptorsPeng Huang and Lee-Yuan Liu-ChenGPCR Folding and Maturation: The Effect of Pharmacological ChaperonesUlla E. Petaja-Repo and Michel BouvierRegulated Membrane Trafficking and Proteolysis of GPCRsJames N. Hislop and Mark von ZastrowPart II. GPCR Activity and Its RegulatorsHeterotrimeric G Proteins and Their Effector PathwaysTracy Nguyen Hwangpo and Ravi IyengarRGS Proteins: Orchestration of Multiple Signaling PathwaysRyan W. Richman and Maria A. Diverse-PierluissiG Protein-Coupled Receptor KinasesLan Ma, Jingxia Gao, and Xiaoqing ChenRegulators of GPCR Activity: The ArrestinsLouis M. LuttrellGPCR Interacting Proteins: Classes, Assembly, and FunctionsHongyan Wang, Catherine B. Willmore, and Jia Bei WangPart III. GPCR Dimerization/OligomerizationBiophysical and Biochemical Methods to Study GPCR OligomerizationKaren M. Kroeger, Kevin D. G. Pfleger, and Karin A. EidneOligomerization Domains of G Protein-Coupled Receptors: Insights Into the Structural Basis of GPCR AssociationMarta Filizola, Wen Guo, Jonathan A. Javitch, and Harel WeinsteinFunctional Complementation and the Analysis of GPCR DimerizationGraeme Milligan, Juan J. Carrillo, and Geraldine PascalThe Role of Oligomerization in G Protein-Coupled Receptor MaturationMichael M. C. Kong, Christopher H. So, Brian F. O'Dowd, and Susan R. GeorgeReceptor Oligomerization and TraffickingSelena E. Barlett and Jennifer L. WhistlerModulation of Receptor Pharmacology byG Protein-Coupled Receptor DimerizationNoura S. Abul-Husn, Achla Gupta, Lakshmi A. Devi and Ivone GomesPart IV. Recent Developments in Drug DiscoveryRole of Heteromeric GPCR Interactions in Pain/AnalgesiaAndrew P. Smith and Nancy M. LeeConformational Plasticity of GPCR Binding Sites: Structural Basis for Evolutionary Diversity in Ligand RecognitionXavier Deupi, Cedric Govaerts, Lei Shi, Jonathan A. Javitch, Leonardo Pardo, and Juan BallesterosDe-Orphanizing GPCRs and Drug DevelopmentRainer K. Reinscheid and Olivier CivelliIndex