Nuclear G-Protein Coupled Receptors

Nuclear G-Protein Coupled Receptors PDF

Author: Bruce G. Allen

Publisher: Humana

Published: 2016-08-23

Total Pages: 0

ISBN-13: 9781493955466

DOWNLOAD EBOOK →

Nuclear G-Protein Coupled Receptors: Methods and Protocols is a compilation of a number of conceptual and methodological aspects important for the validation and characterization of intacrine signaling systems. To date, the best-characterized intracrine signaling system is that of angiotensin II (Ang II), covered in depth in various chapters. Methodology to study the subcellular localization and function of GPCRs and other signaling systems is provided, as well as numerous chapters focusing on methods designed to understand signaling mediated by nuclear and other internal GPCRs. Methods are also described to study the formation of second messengers such as cAMP and to study the trafficking of receptors from the cell surface. Written in the successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and notes on troubleshooting and avoiding known pitfalls. Authoritative and easily accessible, Nuclear G-Protein Coupled Receptors: Methods and Protocols seeks to serve both professionals and novices with state-of-the-art approaches to characterize what is becoming a common theme in cellular signaling.

G Protein-Coupled Receptors in Drug Discovery

G Protein-Coupled Receptors in Drug Discovery PDF

Author: Kenneth H. Lundstrom

Publisher: CRC Press

Published: 2005-07-11

Total Pages: 376

ISBN-13: 1420028219

DOWNLOAD EBOOK →

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

GPCRs as Therapeutic Targets

GPCRs as Therapeutic Targets PDF

Author: Annette Gilchrist

Publisher: John Wiley & Sons

Published: 2022-09-19

Total Pages: 1610

ISBN-13: 1119564727

DOWNLOAD EBOOK →

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.

Structure-Function Analysis of G Protein-Coupled Receptors

Structure-Function Analysis of G Protein-Coupled Receptors PDF

Author: Jürgen Wess

Publisher: Wiley-Liss

Published: 1999-06-15

Total Pages: 448

ISBN-13:

DOWNLOAD EBOOK →

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.

The G Protein-Coupled Receptors Handbook

The G Protein-Coupled Receptors Handbook PDF

Author: Lakshmi A. Devi

Publisher: Springer Science & Business Media

Published: 2008-03-01

Total Pages: 414

ISBN-13: 1592599192

DOWNLOAD EBOOK →

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.

Signal Transduction: Pathways, Mechanisms and Diseases

Signal Transduction: Pathways, Mechanisms and Diseases PDF

Author: Ari Sitaramayya

Publisher: Springer Science & Business Media

Published: 2009-12-02

Total Pages: 429

ISBN-13: 3642021123

DOWNLOAD EBOOK →

Providing an overview of recent developments in the field of signal transduction, this volume emphasizes direct clinical significance. As such, topics like nuclear receptors, apoptosis, growth factors, cell cycles and cancer are examined.

Receptor Binding Techniques

Receptor Binding Techniques PDF

Author: Anthony P. Davenport

Publisher: Springer Science & Business Media

Published: 2008-02-02

Total Pages: 246

ISBN-13: 1592599273

DOWNLOAD EBOOK →

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.

Pharmacology of G Protein Coupled Receptors

Pharmacology of G Protein Coupled Receptors PDF

Author: Richard R. Neubig

Publisher: Academic Press

Published: 2011-09-19

Total Pages: 408

ISBN-13: 0123859522

DOWNLOAD EBOOK →

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

Lanterna Rally - Theme by Grace Themes