Structure and Function of GPCRs

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.

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  • Author : Guillaume Lebon
  • Publisher : Springer
  • Pages : 289 pages
  • ISBN : 3030245918
  • Rating : 4/5 from 21 reviews
CLICK HERE TO GET THIS BOOKStructure and Function of GPCRs

Structure and Function of GPCRs

Structure and Function of GPCRs
  • Author : Guillaume Lebon
  • Publisher : Springer
  • Release : 01 August 2019
GET THIS BOOKStructure and Function of GPCRs

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

Metabotropic GPCRs: TGR5 and P2Y Receptors in Health and Diseases

Metabotropic GPCRs: TGR5 and P2Y Receptors in Health and Diseases
  • Author : Senthilkumar Rajagopal,Murugavel Ponnusamy
  • Publisher : Springer
  • Release : 19 November 2018
GET THIS BOOKMetabotropic GPCRs: TGR5 and P2Y Receptors in Health and Diseases

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.

G Protein-Coupled Receptors

G Protein-Coupled Receptors
  • Author : David Poyner,Mark Wheatley
  • Publisher : John Wiley & Sons
  • Release : 11 December 2009
GET THIS BOOKG Protein-Coupled Receptors

G-Protein Coupled Receptors (GPCRs) are not only the largest protein family in the human genome but are also the single biggest target for therapeutic agents. Research into GPCRs is therefore growing at a fast pace and the range of techniques that can be applied to GPCRs is vast and continues to grow. This book provides an invaluable bench-side guide into the best and most up-to-date techniques for current and future research on GPCRs. With contributions from leading international authorities, this

G Protein-Coupled Receptors in Health and Disease

G Protein-Coupled Receptors in Health and Disease
  • Author : Anonim
  • Publisher : Academic Press
  • Release : 05 August 2009
GET THIS BOOKG Protein-Coupled Receptors in Health and Disease

G protein-coupled receptors (GPCRs) transduce signals from a diverse array of endogenous ligands, including ions, amino acids, nucleotides, lipids, peptides, and large glycoprotein hormones. They are also responsible for our sensing of exogenous stimuli, including photons and odorants. GPCRs regulate almost every aspect of our physiological functions. It is estimated that 40% to 50% of currently used therapeutic drugs target GPCRs directly or indirectly. Because the current drugs target only a small portion of the GPCRs, opportunities for targeting the remaining GPCRs

G Protein-Coupled Receptors in Drug Discovery

G Protein-Coupled Receptors in Drug Discovery
  • Author : Wayne R. Leifert
  • Publisher : Humana Press
  • Release : 23 August 2016
GET THIS BOOKG Protein-Coupled Receptors in Drug Discovery

The G protein-coupled receptors (GPCRs) and associated peripheral G proteins underpin a multitude of physiological processes. The GPCRs represent one of the largest superfamilies in the human genome and are a significant target for bioactive and drug discovery programs. It is estimated that greater than 50% of all drugs, including those in development, currently target GPCRs. Many of the characterized GPCRs have known ligands; however, approximately 20% of GPCRs are described as orphan GPCRs, apparent GPCRs that share the generic high-level structure

G Protein-Coupled Receptors - Modeling and Simulation

G Protein-Coupled Receptors - Modeling and Simulation
  • Author : Marta Filizola
  • Publisher : Springer Science & Business Media
  • Release : 25 October 2013
GET THIS BOOKG Protein-Coupled Receptors - Modeling and Simulation

G protein-coupled receptors (GPCRs) are heptahelical transmembrane receptors that convert extra-cellular stimuli into intra-cellular signaling, and ultimately into biological responses. Since GPCRs are natural targets for approximately 40% of all modern medicines, it is not surprising that they have been the subject of intense research. Notwithstanding the amount of data generated over the years, discovering ligands of these receptors with optimal therapeutic properties is not straightforward and has certainly been hampered for years by the lack of high-resolution structural information about

G Protein-Coupled Receptors

G Protein-Coupled Receptors
  • Author : Sandra Siehler,Graeme Milligan
  • Publisher : Cambridge University Press
  • Release : 30 September 2010
GET THIS BOOKG Protein-Coupled Receptors

Provides a comprehensive overview of recent discoveries and current understandings of G protein-coupled receptors (GPCRs). Recent advances include the first mammalian non-rhodopsin GPCR structures and reconstitution of purified GPCRs into membrane discs for defined studies, novel signaling features including oligomerization, and advances in understanding the complex ligand pharmacology and physiology of GPCRs, in new assay technologies and drug targeting. The authors take time to detail the importance of the pathophysiological function and drug targeting of GPCRs, specifically β-adrenoceptors in cardiovascular

Modelling of GPCRs

Modelling of GPCRs
  • Author : Andrea Strasser,Hans-Joachim Wittmann
  • Publisher : Springer Science & Business Media
  • Release : 13 August 2012
GET THIS BOOKModelling of GPCRs

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

G Protein-Coupled Receptors as Drug Targets

G Protein-Coupled Receptors as Drug Targets
  • Author : Roland Seifert,Thomas Wieland
  • Publisher : John Wiley & Sons
  • Release : 12 May 2006
GET THIS BOOKG Protein-Coupled Receptors as Drug Targets

With its particular emphasis on the constitutive activity of G-protein-coupled receptors (GPCRs)s, this book comprehensively discusses an important biological process that has not yet been covered in such depth in any other existing books on GPCRs. The international team of highly distinguished authors addresses in detail current models and concepts, to introduce medicinal chemists, physiologists, pharmacologists, and medical researchers into the advances in the understanding of GPCR activation and constitutive activity. In addition, the book provides an overview on

GPCR Molecular Pharmacology and Drug Targeting

GPCR Molecular Pharmacology and Drug Targeting
  • Author : Annette Gilchrist
  • Publisher : John Wiley & Sons
  • Release : 10 December 2010
GET THIS BOOKGPCR Molecular Pharmacology and Drug Targeting

G protein-coupled receptors (GPCRs) are a large protein family of transmembrane receptors vital in dictating cellular responses. GPCRs are involved in many diseases, but are also the target of around half of all modern medicinal drugs. Shifting Paradigms in G Protein Coupled Receptors takes a look at the way GPCRs are examined today, how they react, how their mutations lead to disease, and the many ways in which they can be screened for compounds that modulate them. Chemists, pharmacologists, and

Identification and Expression of G Protein-Coupled Receptors

Identification and Expression of G Protein-Coupled Receptors
  • Author : Kevin R. Lynch
  • Publisher : John Wiley & Sons
  • Release : 10 May 1999
GET THIS BOOKIdentification and Expression of G Protein-Coupled Receptors

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

Orphan G Protein-Coupled Receptors and Novel Neuropeptides

Orphan G Protein-Coupled Receptors and Novel Neuropeptides
  • Author : Olivier Civelli,Qun-Yong Zhou
  • Publisher : Springer Science & Business Media
  • Release : 15 May 2008
GET THIS BOOKOrphan G Protein-Coupled Receptors and Novel Neuropeptides

Over the last decade it has been shown that orphan G protein-coupled receptors (GPCRs) can be used as targets to discover novel neuropeptides. A dozen neuropeptides have been identified through this approach. Each of these neuropeptides has opened new doors for our understanding of fundamental physiological or behavioral responses. For example the orexins, MCH and ghrelin carry fundamental roles in regulating food intake while neuropeptide S, neuromedin S, the prokineticins and the orexins are major players in modulating sleep and

The G Protein-Coupled Receptors Handbook

The G Protein-Coupled Receptors Handbook
  • Author : Lakshmi A. Devi
  • Publisher : Springer Science & Business Media
  • Release : 01 March 2008
GET THIS BOOKThe G Protein-Coupled Receptors Handbook

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

G Protein-Coupled Receptors in Immune Response and Regulation

G Protein-Coupled Receptors in Immune Response and Regulation
  • Author : Anonim
  • Publisher : Academic Press
  • Release : 23 September 2017
GET THIS BOOKG Protein-Coupled Receptors in Immune Response and Regulation

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

The Physiology and Pharmacology of Leucine-rich Repeat GPCRs

The Physiology and Pharmacology of Leucine-rich Repeat GPCRs
  • Author : Brian J. Arey,James A. Dias
  • Publisher : Frontiers Media SA
  • Release : 05 August 2016
GET THIS BOOKThe Physiology and Pharmacology of Leucine-rich Repeat GPCRs

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