G Protein Coupled Receptors

Author : Wayne R. Leifert
Publisher : Humana Press
Page : 0 pages
File Size : 53,8 Mb
Release : 2009-06-09
Category : Medical
ISBN : 1603273166

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G Protein-Coupled Receptors in Drug Discovery by Wayne R. Leifert Pdf

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 : Katharine Herrick-Davis,Graeme Milligan,Giuseppe Di Giovanni
Publisher : Springer
Page : 501 pages
File Size : 41,5 Mb
Release : 2017-08-31
Category : Medical
ISBN : 9783319601748

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G-Protein-Coupled Receptor Dimers by Katharine Herrick-Davis,Graeme Milligan,Giuseppe Di Giovanni Pdf

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 : Sofia Aires M. Martins,Duarte Miguel F. Prazeres
Publisher : Humana
Page : 327 pages
File Size : 44,9 Mb
Release : 2022-06-19
Category : Science
ISBN : 1071612239

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G Protein-Coupled Receptor Screening Assays by Sofia Aires M. Martins,Duarte Miguel F. Prazeres Pdf

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 : Krishna C. Persaud,Santiago Marco,Agustin Gutierrez-Galvez
Publisher : CRC Press
Page : 237 pages
File Size : 46,6 Mb
Release : 2016-04-19
Category : Medical
ISBN : 9781439871720

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Neuromorphic Olfaction by Krishna C. Persaud,Santiago Marco,Agustin Gutierrez-Galvez Pdf

Many advances have been made in the last decade in the understanding of the computational principles underlying olfactory system functioning. Neuromorphic Olfaction is a collaboration among European researchers who, through NEUROCHEM (Fp7-Grant Agreement Number 216916)-a challenging and innovative European-funded project-introduce novel computing p

Author : Lakshmi A. Devi
Publisher : Springer Science & Business Media
Page : 412 pages
File Size : 54,7 Mb
Release : 2008-03-01
Category : Medical
ISBN : 9781592599196

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The G Protein-Coupled Receptors Handbook by Lakshmi A. Devi Pdf

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 : Gabriel Berstein
Publisher : CRC Press
Page : 424 pages
File Size : 54,5 Mb
Release : 2019-04-24
Category : Medical
ISBN : 9781420048513

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G Protein-Coupled Receptors by Gabriel Berstein Pdf

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

Author : Tatsuya Haga,Shigeki Takeda
Publisher : CRC Press
Page : 336 pages
File Size : 49,5 Mb
Release : 2005-08-04
Category : Medical
ISBN : 9781420038279

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G Protein-Coupled Receptors by Tatsuya Haga,Shigeki Takeda Pdf

This book provides a broad base of knowledge of G-protein-coupled receptors. Useful at both the university and industrial levels, this book is of particular interest to those who are developing therapeutic approaches to diseases using drugs that influence receptor activation.

Author : Kenneth H. Lundstrom,Mark L. Chiu
Publisher : CRC Press
Page : 376 pages
File Size : 53,7 Mb
Release : 2005-07-11
Category : Medical
ISBN : 9781420028218

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G Protein-Coupled Receptors in Drug Discovery by Kenneth H. Lundstrom,Mark L. Chiu Pdf

The broad range of G protein-coupled receptors (GPCRs) encompasses all areas of modern medicine and have an enormous impact on the process of drug development. Using disease-oriented methods to cover everything from screening to expression and crystallization, G Protein-Coupled Receptors in Drug Discovery describes the physiological roles of GPCRs

Author : Anonim
Publisher : Academic Press
Page : 398 pages
File Size : 52,8 Mb
Release : 2017-09-23
Category : Medical
ISBN : 9780128124048

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G Protein-Coupled Receptors in Immune Response and Regulation by Anonim Pdf

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

Author : Anonim
Publisher : Elsevier
Page : 194 pages
File Size : 51,7 Mb
Release : 2023-01-25
Category : Science
ISBN : 9780323994354

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G Protein-Coupled Receptors - Part B by Anonim Pdf

G Protein-Coupled Receptors, Part B, Volume 195 represents the largest class of cell H103 surface proteins that have intricate involvement in nearly every physiological process in our body. Approximately one third of the clinically prescribed medicines target GPCRs and the quest to improve the exiting GPCR-targeting therapeutics continues. Sections in this volume include Adhesion G protein-coupled receptors: Structure and functions, Molecular and cellular mechanisms underlying brain region-specific cannabinoid receptor modulation by estradiol across the rodent estrus cycle, Probing the orphan receptors: Tools and directions, Asymmetric activation of Class C GPCRs, Common and selective signal transduction mechanisms of GPCRs, and much more. Covers a broad range of topics related to GPCR activation and signaling Provides several receptor systems, with an emphasis on emerging paradigms Includes different processes and model systems, with a focus on GPCRs

Author : Jesus Giraldo,Jean-Philippe Pin
Publisher : Royal Society of Chemistry
Page : 548 pages
File Size : 55,6 Mb
Release : 2011-08-16
Category : Science
ISBN : 9781849733441

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G Protein-Coupled Receptors by Jesus Giraldo,Jean-Philippe Pin Pdf

G protein-coupled receptors (GPCRs) are the largest family of cell-surface receptors, with more than 800 members identified thus far in the human genome. They regulate the function of most cells in the body, and represent approximately 3% of the genes in the human genome. These receptors respond to a wide variety of structurally diverse ligands, ranging from small molecules, such as biogenic amines, nucleotides and ions, to lipids, peptides, proteins, and even light. Ligands (agonists and antagonists) acting on GPCRs are important in the treatment of numerous diseases, including cardiovascular and mental disorders, retinal degeneration, cancer, and AIDS. It is estimated that these receptors represent about one third of the actual identified targets of clinically used drugs. The determination of rhodopsin crystal structure and, more recently, of opsin, 1 and 2 adrenergic and A2A adenosine receptors provides both academia and industry with extremely valuable data for a better understanding of the molecular determinants of receptor function and a more reliable rationale for drug design. GPCR structure and function constitutes a hot topic. The book, which lies between the fields of chemical biology, molecular pharmacology and medicinal chemistry, is divided into three parts. The first part considers what receptor structures tell us about the mechanism of receptor activation. Part II focuses on receptor function. It discusses what the data from biophysical and mutational studies, and the analysis of the interactions of the receptor with ligands and regulator proteins, tell us about the process of signal transduction. The final part, on modelling and simulation, details new insights on the link between structure and mechanism and their implications in drug design.

Author : Francisco Ciruela,Rafael Luján
Publisher : Nova Publishers
Page : 328 pages
File Size : 43,5 Mb
Release : 2008
Category : Science
ISBN : 1600219152

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Molecular Aspects of G Protein-coupled Receptors by Francisco Ciruela,Rafael Luján Pdf

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 : Tiina P. Iismaa,Trevor J. Biden,John Shine
Publisher : Springer Science & Business Media
Page : 189 pages
File Size : 51,6 Mb
Release : 2013-06-29
Category : Science
ISBN : 9783662219300

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G Protein-Coupled Receptors by Tiina P. Iismaa,Trevor J. Biden,John Shine Pdf

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 : Robert Laprairie
Publisher : Academic Press
Page : 214 pages
File Size : 43,6 Mb
Release : 2022-02-05
Category : Business & Economics
ISBN : 9780128197721

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Allosteric Modulation of G Protein-Coupled Receptors by Robert Laprairie Pdf

Allosteric Modulation of G Protein-Coupled Receptors reviews fundamental information on G protein-coupled receptors (GPCRs) and allosteric modulation, presenting original research in the area and collectively providing a comprehensive description of key issues in GPCR allosteric modulation. The book provides background on core concepts of molecular pharmacology while also introducing the most important advances and studies in the area. It also discusses key methodologies. This is an essential book for researchers and advanced students engaged in pharmacology, toxicology and pharmaceutical sciences training and research. Many of the GPCR-targeted drugs released in the past decade have specifically worked via allosteric mechanisms. Unlike direct orthosteric-acting compounds that occupy a similar receptor site to that of endogenous ligands, allosteric modulators alter GPCR-dependent signaling at a site apart from the endogenous ligand. Recent methodological and analytical advances have greatly improved our ability to understand the signaling mechanisms of GPCRs. We now know that allostery is a common regulatory mechanism for all GPCRs and not – as we once believed – unique to a few receptor subfamilies. Introduces background on core concepts of molecular pharmacology, including statistical analyses, non-linear regression, complex models and GPCR-dependent signal transduction as they relate to allosteric modulation Discusses critical advances and landmark studies, including discoveries in the area of GPCR allosteric modulation, which are reviewed for their importance in positive and negative regulation, protein-protein interactions, and small molecule drug discovery Includes key methodologies used to study allosteric modulation at the in silico, in vitro, and in vivo levels of drug discovery and characterization

Author : Bruce Alberts
Publisher : Unknown
Page : 0 pages
File Size : 48,9 Mb
Release : 2002
Category : Cytology
ISBN : 0815332181

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Molecular Biology of The Cell by Bruce Alberts Pdf