Gpcrs As Therapeutic Targets

Author : Annette Gilchrist
Publisher : John Wiley & Sons
Page : 1610 pages
File Size : 41,8 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.

Author : Roland Seifert,Thomas Wieland
Publisher : John Wiley & Sons
Page : 304 pages
File Size : 53,5 Mb
Release : 2006-05-12
Category : Science
ISBN : 9783527606955

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G Protein-Coupled Receptors as Drug Targets by Roland Seifert,Thomas Wieland Pdf

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 methods of investigating constitutive GPCR activity. The text is well illustrated by selected experimental data and schemes._The chaptes are all cross-referenced with each other and cover general mechnisms, methodological approaches and cover selected important GPCR sysstems, the consequences for drug action, including, side effects, and rational drug design for GPCR targets. A highly recommended reference for researchers in academia and industry. authors addresses in detail current models and concepts, so as to introduce pharmaceutical chemists, physiologists and medical researchers to the advances in the understanding of GPCR activation and constitutive activity, and provides an overview of the methods of investigating GPCR activity. The text is backed by abundant case studies and methodological advice for analyzing GPCRs, covering selected pharmacologically relevant GPCR systems, the consequences for drug action, including unwanted side effects, and rational drug design for GPCR targets. A highly practical reference for researchers in academia and industry.

Author : Kenneth H. Lundstrom,Mark L. Chiu
Publisher : CRC Press
Page : 376 pages
File Size : 43,9 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 : Bruce G. Allen,Terence E. Hébert
Publisher : Humana
Page : 0 pages
File Size : 45,6 Mb
Release : 2016-08-23
Category : Science
ISBN : 1493955462

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Nuclear G-Protein Coupled Receptors by Bruce G. Allen,Terence E. Hébert Pdf

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.

Author : Krishna C. Persaud,Santiago Marco,Agustin Gutierrez-Galvez
Publisher : CRC Press
Page : 237 pages
File Size : 42,5 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 : Denis J. Dupré,Terence E. Hébert,Ralf Jockers
Publisher : Springer Science & Business Media
Page : 298 pages
File Size : 44,6 Mb
Release : 2012-11-19
Category : Medical
ISBN : 9789400747654

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GPCR Signalling Complexes – Synthesis, Assembly, Trafficking and Specificity by Denis J. Dupré,Terence E. Hébert,Ralf Jockers Pdf

Main Question: G protein coupled receptors are involved in highly efficient and specific activation of signalling pathways. How do GPCR signalling complexes get assembled to generate such specificity? In order to answer this question, we need to understand how receptors and their signalling partners are synthesized, folded and quality-controlled in order to generate functional proteins. Then, we need to understand how each partner of the signalling complex is selected to join a complex, and what makes this assembly possible. GPCRs are known to be able to function as oligomers, what drives the assembly into oligomers and what will be the effects of such organization on specificity and efficacy of signal transduction. Once the receptor complexes are assembled, they need to reach different locations in the cell; what drives and controls the trafficking of GPCR signalling complexes. Finally, defects in synthesis, maturation or trafficking can alter functionality of GPCRs signalling complexes; how can we manipulate the system to make it function normally again? Pharmacological chaperones may just be part of the answer to this question.

Author : Richard R. Neubig
Publisher : Academic Press
Page : 408 pages
File Size : 48,7 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

Author : P. Michael Conn,Claude Kordon
Publisher : Springer Science & Business Media
Page : 211 pages
File Size : 42,6 Mb
Release : 2006-09-28
Category : Medical
ISBN : 9783540344476

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Insights into Receptor Function and New Drug Development Targets by P. Michael Conn,Claude Kordon Pdf

This book describes the current state of knowledge in receptor function in the development of new drugs. Science is on the verge of viewing effector molecules and other regulatory sites as therapeutic targets for the amelioration of human and animal disease. The book reviews the availability of state-of-the-art tools that allow measurement of interactions and afford unprecedented insight into the biomolecular interactions that present novel approaches to drug design.

Author : Marta Filizola
Publisher : Unknown
Page : 327 pages
File Size : 49,5 Mb
Release : 2015
Category : Medical
ISBN : 1493929143

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G Protein-coupled Receptors in Drug Discovery by Marta Filizola Pdf

This detailed volume provides an overview of recent techniques employed in the field of G protein-coupled receptors (GPCRs) to screen for new drugs and to derive information about their receptor structure, dynamics, and function for the purpose of developing improved therapeutics. Owing to remarkable recent advances in the structural, biophysical, and biochemical analyses of these receptors, as well as a growing body of evidence hinting at the possible relevance of allosteric modulators, biased agonists, and oligomer-selective ligands as improved therapeutic agents, drug discovery for GPCRs has recently taken a completely new direction. For this book, expert contributors have shared their protocols and views on the impact of these methodologies on modern drug discovery. 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. Practical and fully updated, G Protein-Coupled Receptors in Drug Discovery: Methods and Protocols, Second Edition serves as an ideal guide for a diverse audience from structural and molecular biologists to pharmacologists and drug designers who wish to explore this extensive class of key drug targets.--

Author : Luis M. Botana,Mabel Loza
Publisher : John Wiley & Sons
Page : 503 pages
File Size : 52,7 Mb
Release : 2012-04-20
Category : Medical
ISBN : 9781118185520

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Therapeutic Targets by Luis M. Botana,Mabel Loza Pdf

The Latest Applications For Cellmechanism Research in Drug Discovery Designed to connect research on cell mechanisms with the drug discovery process, Therapeutic Targets: Modulation, Inhibition, and Activation introduces readers to a range of new concepts and novel approaches to drug screening and therapeutic drug targeting to help inform future avenues of drug research. Highly topical, this accessible edited volume features chapters contributed by respected experts from around the globe. The book helps postgraduate students and professional scientists working in academia and industry understand the molecular mechanisms of pharmacology, current pharmacological knowledge, and future perspectives in drug discovery, focusing on important biochemical protein targets and drug targeting strategies for specific diseases. Examining the pharmacology of therapeutically undefined targets and their potential applications, it includes chapters on traditional therapeutic targets, including enzymes (phosphodiesterases and proteases), ion channels, and G protein-coupled receptors, as well as more recently identified avenues of exploration, such as lipids, nuclear receptors, gene promoters, and more. Since different diseases require different targeting techniques, the book also includes dedicated chapters on strategies for investigating Alzheimer's, diabetes, pain, and inflammation treatments. Concluding with a cross-sectional look at new approaches in drug screening, Therapeutic Targets is an invaluable resource for understanding where the next generation of drugs are likely to emerge.

Author : Antonino Belfiore,Derek LeRoith
Publisher : Springer
Page : 0 pages
File Size : 41,6 Mb
Release : 2018-02-08
Category : Medical
ISBN : 3319446746

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Principles of Endocrinology and Hormone Action by Antonino Belfiore,Derek LeRoith Pdf

This volume provides comprehensive coverage of the current knowledge of the physiology of the endocrine system and hormone synthesis and release, transport, and action at the molecular and cellular levels. It presents essential as well as in-depth information of value to both medical students and specialists in Endocrinology, Gynecology, Pediatrics, and Internal Medicine. Although it is well established that the endocrine system regulates essential functions involved in growth, reproduction, and homeostasis, it is increasingly being recognized that this complex regulatory system comprises not only hormones secreted by the classic endocrine glands but also hormones and regulatory factors produced by many organs, and involves extensive crosstalk with the neural and immune system. At the same time, our knowledge of the molecular basis of hormone action has greatly improved. Understanding this complexity of endocrine physiology is crucial to prevent endocrine disorders, to improve the sensitivity of our diagnostic tools, and to provide the rationale for pharmacological, immunological, or genetic interventions. It is such understanding that this book is designed to foster.

Author : Sameer Mohammad,Muheeb Beg,Manveen Kaur Gupta
Publisher : Frontiers Media SA
Page : 146 pages
File Size : 51,9 Mb
Release : 2022-01-28
Category : Science
ISBN : 9782889742134

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Cell Biology, Physiology and Molecular Pharmacology of G protein Coupled Receptors by Sameer Mohammad,Muheeb Beg,Manveen Kaur Gupta Pdf

Author : P.Michael Conn,Claude Kordon
Publisher : Springer
Page : 202 pages
File Size : 52,8 Mb
Release : 2009-09-02
Category : Medical
ISBN : 3540824464

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Insights into Receptor Function and New Drug Development Targets by P.Michael Conn,Claude Kordon Pdf

This book describes the current state of knowledge in receptor function in the development of new drugs. Science is on the verge of viewing effector molecules and other regulatory sites as therapeutic targets for the amelioration of human and animal disease. The book reviews the availability of state-of-the-art tools that allow measurement of interactions and afford unprecedented insight into the biomolecular interactions that present novel approaches to drug design.

Author : Kjell Fuxe,Luigi F. Agnati
Publisher : Springer Science & Business Media
Page : 577 pages
File Size : 48,8 Mb
Release : 2013-03-13
Category : Computers
ISBN : 9781468454154

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Receptor-Receptor Interactions by Kjell Fuxe,Luigi F. Agnati Pdf

Author : Mario Tiberi
Publisher : Humana Press
Page : 406 pages
File Size : 52,7 Mb
Release : 2019-03-01
Category : Science
ISBN : 1493991205

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G Protein-Coupled Receptor Signaling by Mario Tiberi Pdf

This detailed volume assembles comprehensive protocols to assist with the study of structural, molecular, cell biological, and in vivo facets of GPCRs, and to enable the development of experimental tools for screening novel GPCR drugs. Sections explore the tweaking of ligands, bioluminescence and FRET approaches, specific GPCR signaling properties, as well as visualization of subcellular compartmentalization. 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 practical, G Protein-Coupled Receptor Signaling: Methods and Protocols serves as an ideal reference for life scientists working in a variety of research fields including molecular pharmacology, cell and developmental biology, brain behavior and physiology, drug development and screening. Chapter 4 is available open access under a CC BY 4.0 license via link.springer.com.