G Protein Coupled Receptor Screening Assays

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G Protein-Coupled Receptor Screening Assays

Duarte Miguel F. Prazeres,Sofia Aires M. Martins
G Protein Coupled Receptor Screening Assays Book PDF

Author : Duarte Miguel F. Prazeres,Sofia Aires M. Martins
Publisher : Humana
Page : 0 pages
File Size : 55,6 Mb
Release : 2016-09-24
Category : Medical
ISBN : 1493955802

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

This volume explores the considerable efforts that have been directed towards the development of G Protein-Coupled Receptors (GPCR) screening assays in order to disclose GPCR acting compounds, elucidate signaling mechanisms or evaluate compound’s efficacy. New discoveries in the field, along with the widely recognized need for better and safer pharmaceutical drugs constitute the main motivation for this book. Readers, both beginners and experienced researchers, will receive an updated overview of not only the established, but also the innovative technologies that promise to advance GPCR drug research. This book is organized into two major parts: the introductory part discusses the necessary foundations for the understanding of GPCR action and the rationale behind the design of the available screening assays; and part two provides detailed protocols for different screening approaches. Written in the highly successful Methods in Molecular Biology series format, the chapters include the kind of detailed description and implementation advice that is crucial for getting optimal results in the laboratory. Practical and innovative, G Protein-Coupled Receptor Screening Assays: Methods and Protocols reaches out to everyone involved in the discovery of GPCR-active drugs, and provides a transversal overview of the different levels of GPCR signaling addressable in the different screening strategies and presents practical examples of how current assay technologies are contributing to new paradigms in GPCR drug research.

G Protein-Coupled Receptors in Drug Discovery

Kenneth H. Lundstrom,Mark L. Chiu
G Protein Coupled Receptors in Drug Discovery Book PDF

Author : Kenneth H. Lundstrom,Mark L. Chiu
Publisher : CRC Press
Page : 376 pages
File Size : 42,7 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

G Protein Coupled Receptors

Anonim
G Protein Coupled Receptors Book PDF

Author : Anonim
Publisher : Academic Press
Page : 489 pages
File Size : 40,8 Mb
Release : 2013-01-24
Category : Science
ISBN : 9780123918734

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G Protein Coupled Receptors by Anonim Pdf

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 G protein-coupled receptor trafficking motifs, structure-based virtual screening, and automation-friendly high throughput assays for identification of pharmacoperone drugs. 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 G protein-coupled receptor trafficking motifs, structure-based virtual screening, and automation-friendly high-throughput assays for identifying pharmacoperone drugs

G Protein-Coupled Receptors in Drug Discovery

Wayne R. Leifert
G Protein Coupled Receptors in Drug Discovery Book PDF

Author : Wayne R. Leifert
Publisher : Humana Press
Page : 0 pages
File Size : 52,6 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.

G Protein Coupled Receptors

Anonim
G Protein Coupled Receptors Book PDF

Author : Anonim
Publisher : Academic Press
Page : 541 pages
File Size : 54,7 Mb
Release : 2013-01-28
Category : Science
ISBN : 9780124079441

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G Protein Coupled Receptors by Anonim Pdf

This new volume of Methods in Enzymology continues the legacy of this premier serial with quality chapters authored by leaders in the field. This volume covers G protein coupled receptors, and includes chapters on such topics as GPCR modelling, interactions with other molecules, virtual screening and GPCR activation. 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 GPCR modelling, interactions with other molecules, virtual screening and GPCR activation

Ligand Design for G Protein-coupled Receptors, Volume 30

Didier Rognan
Ligand Design for G Protein coupled Receptors Volume 30 Book PDF

Author : Didier Rognan
Publisher : John Wiley & Sons
Page : 300 pages
File Size : 47,6 Mb
Release : 2006-03-10
Category : Medical
ISBN : 3527312846

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Ligand Design for G Protein-coupled Receptors, Volume 30 by Didier Rognan Pdf

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

Tatsuya Haga,Shigeki Takeda
G Protein Coupled Receptors Book PDF

Author : Tatsuya Haga,Shigeki Takeda
Publisher : CRC Press
Page : 336 pages
File Size : 45,6 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.

G Protein-Coupled Receptors - Part B

Anonim
G Protein Coupled Receptors Part B Book PDF

Author : Anonim
Publisher : Elsevier
Page : 194 pages
File Size : 50,9 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

G Protein-Coupled Receptors

Anonim
G Protein Coupled Receptors Book PDF

Author : Anonim
Publisher : Academic Press
Page : 502 pages
File Size : 45,9 Mb
Release : 2016-02-26
Category : Science
ISBN : 9780128036129

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G Protein-Coupled Receptors by Anonim Pdf

G-Protein-Coupled Receptors: Signaling, Trafficking, and Regulation, a new volume 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 research methods in G-Protein-Coupled Receptors, and includes sections on such topics signaling, trafficking and regulation. Covers the increasingly appreciated cell biology field of G-protein-coupled receptors Includes both established and new technologies Contributed by experts in the field Covers topics such as signaling, trafficking, and regulation

GPCRs as Therapeutic Targets

Annette Gilchrist
GPCRs as Therapeutic Targets Book PDF

Author : Annette Gilchrist
Publisher : John Wiley & Sons
Page : 1610 pages
File Size : 45,7 Mb
Release : 2022-09-19
Category : Medical
ISBN : 9781119564720

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GPCRs as Therapeutic Targets by Annette Gilchrist Pdf

Eine umfassende Betrachtung der Struktur, Pharmakologie, Funktion und Rolle von G-Protein-gekoppelten Rezeptoren Mit GPCRs as Therapeutic Targets legt die renommierte Forscherin Dr. Annette Gilchrist einen maßgeblichen, umfassenden Leitfaden für einen dynamischen, aktiven Bereich der akademischen und industriellen Arzneimittelforschung vor. Das Werk, in dem die molekulare Pharmakologie dieser wichtigen Zielklasse behandelt wird, ist ein wichtiges Referenzwerk für neue und erfahrene Forscher, die sich mit G-Protein-gekoppelten Rezeptoren beschäftigen. Es enthält außerdem aktuelle Daten zu GPCR-Strukturen und dem strukturbasierten Wirkstoffdesign. In diesem Werk wird die Rolle von GPCR bei der Behandlung von Krankheiten und für neue Ansätze in deren Erforschung analysiert. Dabei werden nicht nur Informationen über die Struktur, Pharmakologie und Funktion von GPCR dargestellt, sondern es wird auch deren Rolle bei Krankheitszuständen erörtert. Neue Methoden zur Messung der GPCR-Aktivität werden auf verständliche und ansprechende Weise präsentiert. Das Werk bietet: * Eine gründliche Einführung in die molekulare Pharmakologie G-Protein-gekoppelter Rezeptoren mit aktuellen Angaben zu GPCR-Strukturen und dem strukturbasierten Wirkstoffdesign * Ausführliche Erörterungen der entstehenden Pharmakologie von GPCR, des intrazellulären Transports und der subzellulären GPCR-Signalübertragung * Umfassende Betrachtung der allosterischen Modulation, Rezeptordimerisierung, Deorphanisierung und Ubiquitinierung * Ausführliche Besprechung der Rolle von GPCR bei der Behandlung von Krebs, Substanzmissbrauch, zerebrovaskulären Erkrankungen und Stoffwechselkrankheiten Als ideales Referenzwerk für Forscher in den Bereichen Biochemie, Zellbiologie und Pharmakologie sollte GPCRs as Therapeutic Targets auch in den Bibliotheken von Fachleuten der Medizinischen Chemie, Strukturbiologie und klinischen Pharmakologie einen Platz finden.

G Protein Coupled Receptors

Anonim
G Protein Coupled Receptors Book PDF

Author : Anonim
Publisher : Academic Press
Page : 451 pages
File Size : 51,8 Mb
Release : 2013-01-17
Category : Science
ISBN : 9780123918727

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G Protein Coupled Receptors by Anonim Pdf

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

Identification and Expression of G Protein-Coupled Receptors

Kevin R. Lynch
Identification and Expression of G Protein Coupled Receptors Book PDF

Author : Kevin R. Lynch
Publisher : John Wiley & Sons
Page : 246 pages
File Size : 52,7 Mb
Release : 1999-05-10
Category : Science
ISBN : 047119493X

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Identification and Expression of G Protein-Coupled Receptors by Kevin R. Lynch Pdf

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.

Serotonin Receptors in Neurobiology

Amitabha Chattopadhyay
Serotonin Receptors in Neurobiology Book PDF

Author : Amitabha Chattopadhyay
Publisher : CRC Press
Page : 224 pages
File Size : 42,8 Mb
Release : 2007-05-17
Category : Science
ISBN : 1420005758

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Serotonin Receptors in Neurobiology by Amitabha Chattopadhyay Pdf

A number of developments spanning a multitude of techniques makes this an exciting time for research in serotonin receptors. A comprehensive review of the subject from a multidisciplinary perspective, Serotonin Receptors in Neurobiology is among the first books to include information on serotonin receptor knockout studies. With contributions from leading experts in their fields, the book explores serotonin receptors from a broad-based, multidisciplinary approach. The approaches described vary from molecular biological techniques to fluorescence microscopy and imaging, to genetic manipulation in animal models, providing a wide range of tools to study serotonergic phenomena. While each of these approaches has its own advantages and limitations, the synthesis of information and knowledge achieved from studies using multiple approaches will result in a comprehensive understanding of the underlying complex phenomena involved in serotonergic signaling and its implications in health and disease. The book provides an overall understanding of these receptors based on currently used methodologies and techniques. It describes specific experimental procedures that will be of use to researchers interested in addressing similar problems involving other G-protein-coupled receptor signaling systems.

Pharmacology of G Protein Coupled Receptors

Richard R. Neubig
Pharmacology of G Protein Coupled Receptors Book PDF

Author : Richard R. Neubig
Publisher : Academic Press
Page : 408 pages
File Size : 45,5 Mb
Release : 2011-09-19
Category : Medical
ISBN : 9780123859525

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Pharmacology of G Protein Coupled Receptors by Richard R. Neubig Pdf

G protein coupled receptors remain the most important class of therapeutic targets in medicine. In the last 5 years, tremendous advances have been made in our understanding of the structure and mechanism of this critical family of drug targets. The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors. It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones. In addition, emerging drug targets such as receptor families for fatty acids, carboxylic acids, lipid mediators, etc. are included. Final chapters cover novel mechanisms of signal regulation through PDZ domains and RGS proteins. This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists. The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists

Receptor Binding Techniques

Anthony P. Davenport
Receptor Binding Techniques Book PDF

Author : Anthony P. Davenport
Publisher : Springer Science & Business Media
Page : 246 pages
File Size : 44,9 Mb
Release : 2008-02-02
Category : Medical
ISBN : 9781592599271

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Receptor Binding Techniques by Anthony P. Davenport Pdf

A comprehensive collection of readily reproducible methods for studying receptors in silico, in vitro, and in vivo. These cutting-edge techniques cover mining from curated databases, identifying novel receptors by high throughput screening, molecular methods to identify mRNA encoding receptors, radioligand binding assays and their analysis, quantitative autoradiography, and imaging receptors by positron emission tomography (PET). Highlights include phenotypic characterization of receptors in knockout mice, imaging receptors using green fluorescent protein and fluorescent resonance energy transfer, and quantitative analysis of receptor mRNA by TaqMan PCR. These book equips the researcher with techniques for exploring the unprecedented number of new receptor systems now emerging and the so-called "orphan" receptors whose activating ligand has not been identified.