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GPCRs

GPCRs Book
Author : Beata Jastrzebska,Paul S.-H. Park
Publisher : Academic Press
Release : 2019-09-11
ISBN : 0128167289
Language : En, Es, Fr & De

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Book Description :

GPCRS: Structure, Function, and Drug Discovery provides a comprehensive overview of recent discoveries and our current understanding of GPCR structure, signaling, physiology, pharmacology and methods of study. In addition to the fundamental aspects of GPCR function and dynamics, international experts discuss crystal structures, GPCR complexes with partner proteins, GPCR allosteric modulation, biased signaling through protein partners, deorphanization of GPCRs, and novel GPCR-targeting ligands that could lead to the development of new therapeutics against human diseases. GPCR association with, and possible therapeutic pathways for, retinal degenerative diseases, Alzheimer’s disease, Parkinson’s disease, cancer and diabetic nephropathy, among other illnesses, are examined in-depth. Addresses our current understanding and novel advances in the GPCR field, directing readers towards recent finding of key significance for translational medicine Combines a thorough discussion of structure and function of GPCRs with disease association and drug discovery Features chapter contributions from international experts in GPCR structure, signaling, physiology and pharmacology

G Protein Coupled Receptors

G Protein Coupled Receptors Book
Author : Anonim
Publisher : Academic Press
Release : 2019-01-05
ISBN : 0128151080
Language : En, Es, Fr & De

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Book Description :

G-Protein-Coupled Receptors, Part B, 2nd Edition, Volume 149, the latest release in the Methods in Cell Biology series, continues the legacy of this premier serial with quality chapters authored by leaders in the field. This volume covers Optical Approaches for Visualization of Arrestin Binding to Muscarinic Receptors, Luciferase Reporter Assay for Unlocking Ligand-mediated Signaling of GPCRs, Assays to Measure GPCR Dependent Cellular Migration, Characterization of the Frizzled GPCRs, Binding Assays for Bradykinin and Angiotensin Receptors, Detection of Misfolded Rhodopsin Aggregates in Cells, Measuring GPCR Ubiquitination and Trafficking, Culture of Primary Neurons and its Use in Studying GPCR Trafficking, and much more. Covers the increasingly appreciated cell biology field of G-protein-coupled receptors Includes both established and new technologies Contributed by experts in the field

GPCRs From Deorphanization to Lead Structure Identification

GPCRs  From Deorphanization to Lead Structure Identification Book
Author : H. Bourne,Richard Horuk,J. Kuhnke,H. Michel
Publisher : Springer Science & Business Media
Release : 2007-05-23
ISBN : 3540489827
Language : En, Es, Fr & De

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Book Description :

This book offers an insight into the approaches taken by industry and academia to address GPCRs and depict how mature this target class-oriented research has become in the last decade. Coverage also reflects the actual trends in the fast-emerging field of GPCR research in academia and industry. It is based on the international workshop GPCRs: From Deorphanisation to Lead Structure Identification, held in Berlin in May 2006.

Modelling of GPCRs

Modelling of GPCRs Book
Author : Andrea Strasser,Hans-Joachim Wittmann
Publisher : Springer Science & Business Media
Release : 2012-08-13
ISBN : 9400745966
Language : En, Es, Fr & De

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Book Description :

G protein coupled receptors (GPCRs) comprise an important protein family, which is involved in signal transduction in the cell. Besides that a large number of drugs, available on market, address GPCRs. For an efficient and improved development of appropriate drugs, molecular modelling of GPCRs is – in order to understand the ligand-receptor interactions and functionality of GPCRs on molecular level - an important tool. The book “Modelling of GPCRs – a practical handbook” is focussed onto a practical introduction into molecular modelling of GPCRs. This book is very useful for beginners in GPCR modelling, but also addresses the advanced GPCR modeller: On the one hand, the book introduces principles of GPCR modelling, including extensive examples. On the other hand, detailed outlooks onto advanced GPCR modelling techniques are presented. Furthermore, the book includes important data, like information about crystal structures in a summarized manner or amino acid sequences, which are essential for GPCR modelling in general. Due to an increase in efficacy and data handling most modellers use LINUX as operating system. To address this, a summary of most important LINUX commands with examples is presented within the book.

Neuropeptide GPCRs in neuroendocrinology

Neuropeptide GPCRs in neuroendocrinology Book
Author : Jae Young Seong,Hubert Vaudry
Publisher : Frontiers E-books
Release : 2014-11-07
ISBN : 2889192679
Language : En, Es, Fr & De

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Book Description :

The human genome encompasses ˜ 860 G protein-coupled receptors (GPCRs) including 374 non-chemosensory GPCRs. Half of these latter GPCRs recognize (neuro)peptides as natural ligands. GPCRs thus play a pivotal role in neuroendocrine communication. In particular, GPCRs are involved in the neuroendocrine control of feeding behavior, reproduction, growth, hydromineral homeostasis and stress response. GPCRs are also major drug targets and hence possess a strong potential for the development of innovative pharmaceuticals. The aim of this Research Topic was to assemble a series of review articles and original research papers on neuropeptide GPCRs and their ligands that would illustrate the different facets of the studies currently conducted in this domain.

GPCRs as Therapeutic Targets

GPCRs as Therapeutic Targets Book
Author : Annette Gilchrist
Publisher : John Wiley & Sons
Release : 2022-09-19
ISBN : 1119564727
Language : En, Es, Fr & De

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Book Description :

A thorough discussion of the structure, pharmacology, function, and role of G protein-coupled receptors In GPCRs as Therapeutic Agents, distinguished researcher Dr. Annette Gilchrist delivers an authoritative and in-depth compendium of a vibrant and active area of academic and industrial drug discovery. The book serves as an important reference for new and experienced researchers studying G protein-coupled receptors and discusses the molecular pharmacology of this important target class. It also includes up-to-date material on GPCR structures and structure-based drug design. The book explores the role of GPCRs in the treatment of disease and novel approaches to their study. In addition to providing information on the structure, pharmacology, and function of GPCRs, it discusses their role in disease states, and advances new methods for measuring GPCR activity in an accessible and engaging way. The book includes: A thorough introduction to the molecular pharmacology of G protein-coupled receptors, including up-to-date material on GPCR structures and structure-based drug design In-depth discussions of the evolving pharmacology for GPCRs, intracellular trafficking, and subcellular GPCR signaling Comprehensive explorations of allosteric modulation, receptor dimerization, deorphanization, and ubiquitination Fulsome treatments of the role played by GPCRs in the treatments of cancer, substance use disorders, cerebrovascular diseases, and metabolic diseases Perfect for researchers in biochemistry, cell biology, and pharmacology, GPCRs as Therapeutic Agents will also earn a place in the libraries of professionals working in medicinal chemistry, structural biology, and clinical pharmacology.

Structure and Function of GPCRs

Structure and Function of GPCRs Book
Author : Guillaume Lebon
Publisher : Springer
Release : 2019-08-01
ISBN : 3030245918
Language : En, Es, Fr & De

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Book Description :

This book introduces readers to the latest advances in G protein-coupled receptor (GPCR) biology. It reviews our current understanding of the structural basis of ligand binding and allosteric mechanisms, following a decade of technological breakthroughs. Several examples of structure-based drug discovery are presented, together with the future challenges involved in designing better drugs that target GPCRs. In turn, the book illustrates the important concept of GPCR biased signaling in physiological contexts, and presents fluorescent- and light-based methodologies frequently used to measure GPCR signaling or to trace their dynamics in cells upon ligand activation. Taken together, the chapters provide an essential overview and toolkit for new scientific investigators who plan to develop GPCR projects. All chapters were written by experts in their respective fields, and share valuable insights and powerful methodologies for the GPCR field.

Adhesion GPCRs

Adhesion   GPCRs Book
Author : Simon Yona,Martin Stacey
Publisher : Springer Science & Business Media
Release : 2011-06-26
ISBN : 1441979131
Language : En, Es, Fr & De

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Book Description :

Upon completion of the human genome project over 800 G protein-coupled receptor 1 (GPCR) genes, subdivided into five categories, were identified. These receptors sense a diverse array of stimuli, including peptides, ions, lipid analogues, light and odour, in a discriminating fashion. Subsequently, they transduce a signal from the ligand–receptor complex into numerous cellular responses. The importance of GPCRs is further reflected in the fact that they constitute the most common target for therapeutic drugs across a 2 wide range of human disorders. Phylogenetic analysis of GPCRs produced the GRAFS classification system, which subdivides GPCRs into five discrete families: glutamate, rhodopsin, adhesion, frizzled/taste2 and secretin receptors. The adhesion-GPCR family 2 can be further subdivided into eight groups. The field of adhesion-GPCR biology has indeed become large enough to require a volume dedicated solely to this field. The contributors to this book have made a courageous effort to address the key concepts of adhesion-GPCR biology, including the evolution and biochemistry of adhesion-GPCRs; there are extensive discussions on the functional nature of these receptors during development, the immune response and tumourgenesis. Finally, there are chapters dedicated to adhesion-GPCR signalling, an area of intense investigation.

Monitoring endogenous GPCRs lessons for drug design

Monitoring endogenous GPCRs  lessons for drug design Book
Author : Dominique Massotte
Publisher : Frontiers Media SA
Release : 2015-10-07
ISBN : 2889196518
Language : En, Es, Fr & De

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Book Description :

G protein-coupled receptors (GPCRs) are integral membrane proteins forming the fourth largest superfamily in the human genome. Many of these receptors play key physiological roles and several pathologies have been associated with receptor functional abnormalities. GPCRs therefore represent important goals for drug design in pharmaceutical companies since they constitute the target of about one third of the drugs currently on the market. However, endogenous GPCRs are most often difficult to study because of a lack of tools to target them specifically and single out their response to physiological or drug-elicited stimulations. Hence, studies mostly focused on recombinant receptors expressed in a variety of cellular models that do not always closely reflect the receptor natural environment and often deal with levels of expression exceeding by far physiological ranges. Recent technological developments combining for example genetically modified animals and advanced imaging approaches have improved our ability to visualize endogenous GPCRs. To date, trailing receptor activation, subsequent intracellular redistribution, changes in signaling cascade up to integrated response to a drug-elicited stimulation is at hand though the impact of a physiological challenge on receptor dynamics remains a major issue. Data however suggest that the receptor may embrace a different fate depending on the type of stimulation in particular if sustained or repeated. This suggests that current drugs may only partially mimic the genuine response of the receptor and may explain, at least in part, their secondary effects. Commonalities and specificities between physiological and drug-induced activation can thus represent valuable guidelines for the design of future drugs.

Metabotropic GPCRs TGR5 and P2Y Receptors in Health and Diseases

Metabotropic GPCRs  TGR5 and P2Y Receptors in Health and Diseases Book
Author : Senthilkumar Rajagopal,Murugavel Ponnusamy
Publisher : Springer
Release : 2018-11-19
ISBN : 981131571X
Language : En, Es, Fr & De

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Book Description :

This book will provide current understandings about two ubiquitously expressed metabotropic GPCRs, G-coupled purinoreceptor type 2 (P2Y) and Takeda G-protein-coupled bile acid receptor 5 (TGR5). G protein coupled receptors (GPCRs) are the largest family of proteins implicated in majority of cellular responses. The two receptor sub-families play a central role in many physiological functions as well as in many pathological conditions. This book offers up-to-date information on the physiological functions, signaling pathways and regulatory mechanisms of P2Y and TGR5 receptors. In addition, this book provides a comprehensive overview about the abnormalities of P2Y/TGR5 receptors and their contribution in the development and progression of pathological conditions. It also covers the currently available natural, chemical and pharmacological agents targeting these two receptor families and their therapeutic implications in P2Y and TGR5 associated disorders. This book is a valuable source for beginners and researchers to follow the rapidly progressing field of these two GPCR subfamily members.

Trafficking of GPCRs

Trafficking of GPCRs Book
Author : Guangyu Wu
Publisher : Academic Press
Release : 2015-06-05
ISBN : 0128029552
Language : En, Es, Fr & De

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Book Description :

G protein-coupled receptors (GPCRs) constitute the largest superfamily of cell surface receptors that regulate a variety of cell functions. Over the past few decades great progress has been made in defining the roles of intracellular trafficking in controlling the functionality of the receptors as well as in the development of various human diseases. This volume of Progress in Molecular Biology and Translational Science reviews the recent understanding of GPCR trafficking regulators and molecular mechanisms. Written by future leaders in the pain field Covers a wide range of targets Contains provocative ideas about GPCR trafficking

The Physiology and Pharmacology of Leucine rich Repeat GPCRs

The Physiology and Pharmacology of Leucine rich Repeat GPCRs Book
Author : Brian J. Arey,James A. Dias
Publisher : Frontiers Media SA
Release : 2016-08-05
ISBN : 2889199584
Language : En, Es, Fr & De

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Book Description :

G protein-coupled receptors (GPCRs) represent a large and physiologically important class of cell surface receptors. There are approximately 750 known GPCRs present in the human genome that can be subdivided into general classes based upon sequence homology within their transmembrane domains. Therapeutically, GPCRs represent a fertile source for the development of therapies as they are a significant percentage of our current pharmacopeia. Among the three subclasses of GPCRs, the Class A (rhodopsin-like) receptors are by far the most prevalent and extensively studied. However, within the Class A receptors, sub-families of receptors can be distinguished based upon common sequence motifs within the transmembrane domains as well as extracellular and intracellular domains. One such family of Class A receptors is characterized by multiple leucine- rich repeats within their amino- terminal domains (the Leucine-rich Repeat family (LRR)). This family of GPCRs are best represented by the glycoprotein hormone receptors (LHR, FSHR and TSHR) which have been studied extensively but also includes receptors for the peptide hormone relaxin (RXFP1 and RXFP2 (RXFP2 also binds insulin-like peptide 3)) and three other receptors (LGR4, LGR5 and LGR6). LGR4-6 were, until recently, considered orphan receptors. However, emerging data have revealed that these proteins are the receptors for a family of growth factors called R-spondins. Over the last 20 years much has been learned about LRR receptors, including the development of synthetic agonists and antagonists, new insights into signaling (including signaling bias) and the physiological role these receptors play in regulating the function of many tissues. This topic will focus on what is known concerning the regulation of these receptors, their signaling pathways, functional consequences of activation and pharmacology.

Ligand Design for G Protein coupled Receptors Volume 30

Ligand Design for G Protein coupled Receptors  Volume 30 Book
Author : Didier Rognan,Raimund Mannhold,Hugo Kubinyi,Gerd Folkers
Publisher : John Wiley & Sons
Release : 2006-03-10
ISBN : 9783527312849
Language : En, Es, Fr & De

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Book Description :

1. G protein-coupled receptors in the human genome -- 2. Why G protein-coupled receptors databases are needed -- 3. A novel drug screening assay for G protein-coupled receptors -- 4. Importance of GPCR dimerization for function : the case of the class C GPCRs -- 5. Molecular mechanisms of GPCR activation -- 6. Allosteric properties and regulation of G protein-coupled receptors -- 7. Chemogenomics approaches to ligand design -- 8. Strategies for the design of pGPCR-targeted libraries -- 9. Ligand-based rational design : virtual screening -- 10. 3-D structure of G protein-coupled receptors --11. 7TM models in structure-based drug design -- 12. Receptor-based rational design : virtual screening.

G Protein Coupled Receptors in Immune Response and Regulation

G Protein Coupled Receptors in Immune Response and Regulation Book
Author : Anonim
Publisher : Academic Press
Release : 2017-09-23
ISBN : 0128124040
Language : En, Es, Fr & De

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Book Description :

G Protein-Coupled Receptors in Immune Response and Regulation, Volume 136 presents emerging concepts related to the role of GPCRs in immune response and regulation. Users will find updated chapters on a variety of topics, including Beta-adrenergic signaling in the onset and progression of asthma, the Emerging roles of Regulators of G protein signaling (RGS) proteins in the immune system, information on Kinin receptors in immune response and pathogenic infections, and sections on GPCR signaling in C. elegans and its implications in immune response, GPCR Kinases in Inflammatory response and signaling, and GRK2 in Inflammation: Regulation of T cell receptors and IgE signaling. Chapters in this book discuss not only the well-known aspects of GPCR signaling in immunology, but also presents many emerging paradigms that have not yet been reported in classical textbooks. Each chapter presents a forward-looking discussion, providing a glimpse of the tremendous potential associated with the specific receptor systems discussed. Brings together contributions from leading experts in the area of GPCR biology Discusses current paradigms and the future potential of understanding GPCR signaling in immune response and regulation Presents the first of its kind book to focus on specific GPCR systems in various aspects of immunology, all brought together in one volume

Cell Biology Physiology and Molecular Pharmacology of G protein Coupled Receptors

Cell Biology  Physiology and Molecular Pharmacology of G protein Coupled Receptors Book
Author : Sameer Mohammad,Muheeb Beg,Manveen Kaur Gupta
Publisher : Frontiers Media SA
Release : 2022-01-28
ISBN : 288974213X
Language : En, Es, Fr & De

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Book Description :

Download Cell Biology Physiology and Molecular Pharmacology of G protein Coupled Receptors book written by Sameer Mohammad,Muheeb Beg,Manveen Kaur Gupta, available in PDF, EPUB, and Kindle, or read full book online anywhere and anytime. Compatible with any devices.

Identification and Expression of G Protein Coupled Receptors

Identification and Expression of G Protein Coupled Receptors Book
Author : Kevin R. Lynch
Publisher : John Wiley & Sons
Release : 1999-05-10
ISBN : 9780471194934
Language : En, Es, Fr & De

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Book Description :

The past decade has seen tremendous advances in the study of G protein-coupled receptors (GPCRs), including the molecular cloning and identification of more than 100 hundred GPCR genes. But while GPCRs serve as targets for more than 300 medicines in the modern pharmacopoeia, the shrinking pool of known ligands and the continuing discovery of orphan GPCR genes have underscored the need for new approaches to ligand identification. Identification and Expression of G Protein-Coupled Receptors addresses this new direction in GPCR biochemistry-offering a definitive laboratory bench manual that emphasizes expression over primary cloning strategies. In a series of expert contributions by well-known researchers, this book provides detailed protocols for various expression systems-from bacteria to mammalian cells-as well as straightforward opinions on the advantages and shortcomings of each approach. Topics covered include: * Homology screening and the polymerase chain reaction in the cloning of GPCR genes * Cloning of GPCRs using mammalian cell expression * GPCR informatics and the orphan problem * The use of Xenopus laevis oocytes for the study of GPCRs * Stable expression of GPCRs in mammalian cells * Heterologous expression in primary cell cultures * Expression of GPCR in Escherichia coli * Large scale expression and purification of GPCRs in mammalian cells * High-level expression of GPCRs in the Baculovirus/Sf9 cell expression system * Expression of GPCRs in Drosophila Schneider 2 cells * Methods for genetic analysis and ligand identification using heterologous GPCRs expressed in Saccharomyces cerevisiae Supplemented with numerous photographs and illustrations, Identification and Expression of G Protein-Coupled Receptors is important reading for biochemists, pharmacologists, neuroscientists, structural biologists, and anyone involved in GPCR-based research. It delivers a wealth of useful advice, practical tips, and invaluable insight into trends at the cutting-edge of current research.

G Protein Coupled Receptors

G Protein Coupled Receptors Book
Author : Gabriel Berstein
Publisher : CRC Press
Release : 2019-04-24
ISBN : 9781420048513
Language : En, Es, Fr & De

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Book Description :

Covering recently developed methods in membrane-bound receptors, this book emphasizes receptor structure and function, knowledge of which is essential to the study of signal transduction. G Protein-Coupled Receptors has culled contributors from domestic and international sources, providing a broad base of knowledge. Some topics covered are the r

G Protein Coupled Receptors

G Protein Coupled Receptors Book
Author : Anonim
Publisher : Academic Press
Release : 2013-01-17
ISBN : 0123918723
Language : En, Es, Fr & De

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Book Description :

This new volume of Methods in Enzymology continues the legacy of this premier serial by containing quality chapters authored by leaders in the field. This volume covers G protein coupled receptors and includes chapters on such topics as post-translation modification of GPCR in relationship to biased agonism, structure-based virtual screening, and GPCR oligomerization in the brain. Continues the legacy of this premier serial with quality chapters authored by leaders in the field Covers G protein coupled receptors Contains chapters on such topics as post-translation modification of GPCR in relationship to biased agonism, structure-based virtual screening, and GPCR oligomerization in the brain

Structure Function Analysis of G Protein Coupled Receptors

Structure Function Analysis of G Protein Coupled Receptors Book
Author : Jürgen Wess,Wess
Publisher : Wiley-Liss
Release : 1999-06-15
ISBN : 0987650XXX
Language : En, Es, Fr & De

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Book Description :

Structure-Function Analysis of G Protein-Coupled Receptors edited by Jürgen Wess. G protein-coupled receptors (GPCRs) are the largest single class of receptors in biology, playing key roles in a remarkably large number of physiological and pathophysiological conditions. GPCRs or GPCR-dependent signalling pathways are the targets of a very large number of therapeutically useful drugs. Detailed knowledge about the molecular structure of GPCRs should therefore pave the way for the design of novel drugs with increased efficacy and specificity. This volume provides a concise, up-to-date presentation of methods (including molecular genetic, biochemical, and biophysical) which have been used successfully in studying the structure and function of GPCRs. With contributions from international leaders in the field, the editor provides overviews of various techniques, followed by in-depth descriptions of basic procedures and discussions of critical experimental parameters. Divided into specific, accessible sections, Structure-Function Analysis of G Protein-Coupled Receptors includes: * An overview of mutagenesis techniques. * Examples of molecular modeling techniques. * Using peptides as tools for the study of GPCR interactions. * Site-Directed Spin Labeling (SDSL) studies of the GPCR rhodopsin. * A complete description of the electron-crystallographic analysis of two-dimensional rhodopsin crystals. * The use of nuclear magnetic resonance techniques to study GPCR structure. Structure-Function Analysis of G Protein-Coupled Receptors is an invaluable reference for receptor biochemists and biological chemists, pharmacologists, and neuroscientists as well as molecular biologists, cell biologists, and structural biologists worldwide. Also in this series: Receptor Localization: * Laboratory Methods and Procedures edited by Marjorie A. Ariano. * Identification and Expression of G Protein-Coupled Receptors edited by Kevin R. Lynch.

G Protein Coupled Receptor Dimers

G Protein Coupled Receptor Dimers Book
Author : Katharine Herrick-Davis,Graeme Milligan,Giuseppe Di Giovanni
Publisher : Springer
Release : 2017-08-31
ISBN : 3319601741
Language : En, Es, Fr & De

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Book Description :

G-protein-coupled receptors (GPCRs) are believed to be the largest family of membrane proteins involved in signal transduction and cellular responses. They dimerize (form a pair of macromolecules) with a wide variety of other receptors. The proposed book will provide a comprehensive overview of GPCR dimers, starting with a historical perspective and including, basic information about the different dimers, how they synthesize, their signaling properties, and the many diverse physiological processes in which they are involved. In addition to presenting information about healthy GPCR dimer activity, the book will also include a section on their pathology and therapeutic potentials.