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Author : Steve P. Watson
Publisher : Academic Press
Page : 452 pages
File Size : 25,72 MB
Release : 1994-02-28
Category : Medical
ISBN :
Catalogues major facts about receptors, G-proteins and effector molecules. Each entry has a common format, using a minimum amount of text, and contains information on the sequence, gene structure, distribution, agonists/antagonists and physiochemical properties of these proteins.
Author : Katharine Herrick-Davis
Publisher : Humana Press
Page : 501 pages
File Size : 34,23 MB
Release : 2017-09-12
Category : Medical
ISBN : 9783319601724
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.
Author : Bruce Alberts
Publisher :
Page : 0 pages
File Size : 18,19 MB
Release : 2002
Category : Cytology
ISBN : 9780815332183
Author : Tiina P. Iismaa
Publisher : Springer Science & Business Media
Page : 189 pages
File Size : 21,42 MB
Release : 2013-06-29
Category : Science
ISBN : 3662219301
This book is about the recent advances in the structural and functional characterization of receptors that influence intracellular signalling events through interaction with intracellular GTP-binding proteins (G proteins). Molecular cloning of members of the G protein-coupled receptor superfamily has complemented pharmacological investigations in providing a realization of the structural and functional diversity of these receptors. An increased understanding of the involvement of particular receptor subtypes in normal and pathophysiological processes represents exciting possibilities for the development of highly specific and effective therapeutic agents.
Author : Lakshmi A. Devi
Publisher : Springer Science & Business Media
Page : 414 pages
File Size : 16,56 MB
Release : 2008-03-01
Category : Medical
ISBN : 1592599192
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.
Author : Sofia Aires M. Martins
Publisher : Humana
Page : 327 pages
File Size : 29,26 MB
Release : 2022-06-19
Category : Science
ISBN : 9781071612231
This fully updated edition targets not only those assays directly involved in the discovery of GPCR-active compounds but also those involved in cell-based experiments designed to study physiological responses. Whether coming from academia or industry, or being an experienced researcher or a newcomer to the field, the reader will find accessible methods and protocols that cover the latest developments on receptor purification, molecular biology, recombinant engineering, and analytical techniques that enable the real time monitoring of the complex GPCR signaling cascade and identification of potential drug targets. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and up-to-date, G Protein-Coupled Receptor Screening Assays: Methods and Protocols, Second Edition aims to provide the tools necessary to contribute to the advancement of GPCR research and discovery and ultimately lead to the availability of innovative and more efficient drugs.
Author : Wayne R. Leifert
Publisher : Humana Press
Page : 0 pages
File Size : 35,90 MB
Release : 2009-06-09
Category : Medical
ISBN : 9781603273169
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 charact- istic of GPCRs but whose endogenous ligand is not known. Therefore, it is expected that the field of GPCR drug discovery and development will greatly expand in the coming years with emphasis on new generations of drugs against GPCRs with unique therapeuticuseswhichmayincludedrugssuchasallostericregulators,inverseagonists, and identification of orphan GPCR ligands. AswelearnmoreaboutthemolecularsignalingcascadesfollowingGPCRactivation, we acquire a better appreciation of the complexity of cell signaling and as a result, also acquire a vast array ofnew molecularmethods toinvestigate these andother processes. Thegeneralaimofthisbookistoprovideresearcherswitharangeofprotocolsthatmay be useful in their GPCR drug discovery programs. It is also the basis for the devel- ment of future assays in this field. Therefore, the range of topics covered and the appropriate methodological approaches in GPCR drug discovery are reflected in this book. Itisinterestingtonotethatfuturedirectionsindrugdiscoverywillrequireinput and collaboration from a plethora of fields of research. As such, this book will likely be of interest to scientists involved in such fields as molecular biology, pharmacology, biochemistry, cellular signaling, and bio-nanotechnology.
Author : Francisco Ciruela
Publisher : Nova Publishers
Page : 328 pages
File Size : 23,99 MB
Release : 2008
Category : Science
ISBN : 9781600219153
In the recent years, studies based on two-hybrid screens, proteomic, biochemical and cell biology approaches, have shown that intracellular domains of G protein-coupled receptors (GPCR) or heptaspanning membrane receptors (HSMRs) interact with intracellular proteins. These interactions are the basis of a protein network associated to these receptors which includes scaffolding proteins containing one or several PDZ (post-synaptic density-95, discs large, zona occludens-1) domains, signalling proteins and proteins of the cytoskeleton. The present book is focused on the emerging evidence for interactions of G protein-coupled receptors with scaffolding, cytoskeletal and signalling proteins that will play a role in the targeting, anchoring and functioning of these receptors in the plasma membrane, thus contributing to cell development and plasticity.
Author :
Publisher : ScholarlyEditions
Page : 113 pages
File Size : 28,67 MB
Release : 2012-01-09
Category : Science
ISBN : 1464930090
G-Protein-Coupled Receptors: Advances in Research and Application: 2011 Edition is a ScholarlyEditions™ eBook that delivers timely, authoritative, and comprehensive information about G-Protein-Coupled Receptors. The editors have built G-Protein-Coupled Receptors: Advances in Research and Application: 2011 Edition on the vast information databases of ScholarlyNews.™ You can expect the information about G-Protein-Coupled Receptors in this eBook to be deeper than what you can access anywhere else, as well as consistently reliable, authoritative, informed, and relevant. The content of G-Protein-Coupled Receptors: Advances in Research and Application: 2011 Edition has been produced by the world’s leading scientists, engineers, analysts, research institutions, and companies. All of the content is from peer-reviewed sources, and all of it is written, assembled, and edited by the editors at ScholarlyEditions™ and available exclusively from us. You now have a source you can cite with authority, confidence, and credibility. More information is available at http://www.ScholarlyEditions.com/.
Author : Kevin R. Lynch
Publisher : John Wiley & Sons
Page : 246 pages
File Size : 42,1 MB
Release : 1999-05-10
Category : Science
ISBN : 9780471194934
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.