The G Protein-Coupled Receptors Handbook
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The G Protein-Coupled Receptors Handbook

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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

Product details

  • Hardback | 412 pages
  • 160 x 233.7 x 33mm | 839.16g
  • Humana Press Inc.
  • Totowa, NJ, United States
  • English
  • 2005 ed.
  • 9 Illustrations, color; 47 Illustrations, black and white; XVI, 412 p. 56 illus., 9 illus. in color.
  • 1588293653
  • 9781588293657

Back cover copy

G protein-coupled receptors (GPCRs) are involved in many processes in the human body relevant to health and disease, and consequently are the targets of approximately 70% of pharmacological therapeutics and a major source of new drug candidates. In The G Protein-Coupled Receptors Handbook, leading academic researchers comprehensively survey the many recent advances that have occurred in the GPCR field. 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 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. They also discuss the most recent developments that could lead to new 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. Authoritative and cutting-edge, The G Protein-Coupled Receptors Handbook offers pharmacologists, biochemists, and neuroscientists an exhaustive review of the progress made in understanding how GPCRs are activated and regulated, key factors in exploiting GPCRs for drug development.show more

Review quote

"...provides an excellent resource to introduce the reader to many of the diverse areas and questions that drive research in the GCPR field." -TRENDS in Endocrinology and Metablosimshow more

Table of 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 Indexshow more

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