Allosteric Modulation Of G Protein Coupled Receptors

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From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors

Author :
Publisher : Academic Press
ISBN 13 : 0128201886
Total Pages : 328 pages
Book Rating : 4.1/5 (282 download)

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Book Synopsis From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors by :

Download or read book From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors written by and published by Academic Press. This book was released on 2020-05-13 with total page 328 pages. Available in PDF, EPUB and Kindle. Book excerpt: From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors, Volume 88, the latest release in the Advances in Pharmacology series, presents a variety of chapters from the best authors in the field. Chapters in this updated edition include Targeting muscarinic M1 receptor in neurodegeneration, Photo-switchable allosteric ligands, Computational approaches for the design of mGlu receptor allosteric modulators, Allosteric modulation of GLP-1 receptor in metabolic disorders, Group II mGluR roles in the nervous system and their roles in addiction, RAMPs as allosteric modulators of Class B GPCRs, Structure-based discovery and development of mGlu5 NAMs, and much more. Includes the authority and expertise of leading contributors in pharmacology Presents the latest release in the Advances in Pharmacology series

Allosteric Modulation of G Protein-Coupled Receptors

Author : Robert Laprairie
Publisher : Academic Press
ISBN 13 : 0128197722
Total Pages : 214 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Allosteric Modulation of G Protein-Coupled Receptors by : Robert Laprairie

Download or read book Allosteric Modulation of G Protein-Coupled Receptors written by Robert Laprairie and published by Academic Press. This book was released on 2022-02-05 with total page 214 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors

Author :
Publisher : Academic Press
ISBN 13 : 012394791X
Total Pages : 495 pages
Book Rating : 4.1/5 (239 download)

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Book Synopsis Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors by :

Download or read book Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors written by and published by Academic Press. This book was released on 2012-12-02 with total page 495 pages. Available in PDF, EPUB and Kindle. Book excerpt: In this thematic volume of Progress in Molecular Biology and Translational Science, researchers reflect on recent developments and research surrounding G protein-coupled receptors. The chapters cover a large breadth of research, including GPCR role in stem cell function and pharmacology. Authors explore in-depth research techniques and applications of GPCR usage, covering theory, laboratory approaches, and unique qualities that make GPCRs a crucial tool in microbiological and cancer research. - Contributions from leading authorities - Informs and updates on all the latest developments in the field

Allosteric Modulation of G Protein-coupled Receptors

Author : Zhan-Guo Gao
Publisher :
ISBN 13 : 9789090140230
Total Pages : 188 pages
Book Rating : 4.1/5 (42 download)

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Book Synopsis Allosteric Modulation of G Protein-coupled Receptors by : Zhan-Guo Gao

Download or read book Allosteric Modulation of G Protein-coupled Receptors written by Zhan-Guo Gao and published by . This book was released on 2000 with total page 188 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Allosteric Modulation of G Protein-coupled Receptors

Author : Lauren Therese May
Publisher :
ISBN 13 :
Total Pages : 430 pages
Book Rating : 4.:/5 (271 download)

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Book Synopsis Allosteric Modulation of G Protein-coupled Receptors by : Lauren Therese May

Download or read book Allosteric Modulation of G Protein-coupled Receptors written by Lauren Therese May and published by . This book was released on 2007 with total page 430 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Protein Allostery in Drug Discovery

Author : Jian Zhang
Publisher : Springer Nature
ISBN 13 : 9811387192
Total Pages : 384 pages
Book Rating : 4.8/5 (113 download)

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Book Synopsis Protein Allostery in Drug Discovery by : Jian Zhang

Download or read book Protein Allostery in Drug Discovery written by Jian Zhang and published by Springer Nature. This book was released on 2019-11-09 with total page 384 pages. Available in PDF, EPUB and Kindle. Book excerpt: The book focuses on protein allostery in drug discovery. Allosteric regulation, ʹthe second secret of lifeʹ, fine-tunes virtually most biological processes and controls physiological activities. Allostery can both cause human diseases and contribute to development of new therapeutics. Allosteric drugs exhibit unparalleled advantages compared to conventional orthosteric drugs, rendering the development of allosteric modulators as an appealing strategy to improve selectivity and pharmacodynamic properties in drug leads. The Series delineates the immense significance of protein allostery—as demonstrated by recent advances in the repertoires of the concept, its mechanistic mechanisms, and networks, characteristics of allosteric proteins, modulators, and sites, development of computational and experimental methods to predict allosteric sites, small-molecule allosteric modulators of protein kinases and G-protein coupled receptors, engineering allostery, and the underlying role of allostery in precise medicine. Comprehensive understanding of protein allostery is expected to guide the rational design of allosteric drugs for the treatment of human diseases. The book would be useful for scientists and students in the field of protein science and Pharmacology etc.

Allosteric Modulation of G Protein-coupled Receptors

Author : Joaquin Botta
Publisher :
ISBN 13 :
Total Pages : pages
Book Rating : 4.:/5 (11 download)

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Book Synopsis Allosteric Modulation of G Protein-coupled Receptors by : Joaquin Botta

Download or read book Allosteric Modulation of G Protein-coupled Receptors written by Joaquin Botta and published by . This book was released on 2018 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:

Receptor-Receptor Interactions

Author : Kjell Fuxe
Publisher : Springer Science & Business Media
ISBN 13 : 1468454153
Total Pages : 577 pages
Book Rating : 4.4/5 (684 download)

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Book Synopsis Receptor-Receptor Interactions by : Kjell Fuxe

Download or read book Receptor-Receptor Interactions written by Kjell Fuxe and published by Springer Science & Business Media. This book was released on 2013-03-13 with total page 577 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Allosteric Receptor Modulation in Drug Targeting

Author : Norman G. Bowery
Publisher : CRC Press
ISBN 13 : 1420016180
Total Pages : 378 pages
Book Rating : 4.4/5 (2 download)

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Book Synopsis Allosteric Receptor Modulation in Drug Targeting by : Norman G. Bowery

Download or read book Allosteric Receptor Modulation in Drug Targeting written by Norman G. Bowery and published by CRC Press. This book was released on 2016-04-19 with total page 378 pages. Available in PDF, EPUB and Kindle. Book excerpt: Offering a wide array of illustrations and tables in every chapter, this book extensively covers the principles of allosterism in reference to drug action and progresses to a detailed examination of individual ionotropic and G-protein coupled receptor systems-helping those new to the subject understand the importance of allosterism and providing th

Computational Methods for GPCR Drug Discovery

Author : Alexander Heifetz
Publisher : Humana Press
ISBN 13 : 9781493974641
Total Pages : 436 pages
Book Rating : 4.9/5 (746 download)

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Book Synopsis Computational Methods for GPCR Drug Discovery by : Alexander Heifetz

Download or read book Computational Methods for GPCR Drug Discovery written by Alexander Heifetz and published by Humana Press. This book was released on 2017-11-30 with total page 436 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume looks at modern computational strategies and techniques used in GPCR drug discovery including structure and ligand-based approaches and cheminformatics. The chapters in this book describe how these approaches can be applied to address key drug discovery issues, such as receptor structure modelling, function and dynamics, prediction of protein-water-ligand interactions and binding kinetics, free energy of binding, interconversion between agonists and antagonists, deorphanization of GPCRs, and the discovery of biased and allosteric modulators. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary software and tools, step-by-step, readily reproducible modelling protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and unique,Computational Methods for GPCR Drug Discovery is a valuable resource for structural and molecular biologists, computational and medicinal chemists, pharmacologists, and drug designers.

Pharmacology of G Protein Coupled Receptors

Author : Richard R. Neubig
Publisher : Academic Press
ISBN 13 : 0123859522
Total Pages : 408 pages
Book Rating : 4.1/5 (238 download)

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Book Synopsis Pharmacology of G Protein Coupled Receptors by : Richard R. Neubig

Download or read book Pharmacology of G Protein Coupled Receptors written by Richard R. Neubig and published by Academic Press. This book was released on 2011-09-19 with total page 408 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

The Metabotropic Glutamate Receptors

Author : P. Jeffrey Conn
Publisher : Springer Science & Business Media
ISBN 13 : 1475722982
Total Pages : 284 pages
Book Rating : 4.4/5 (757 download)

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Book Synopsis The Metabotropic Glutamate Receptors by : P. Jeffrey Conn

Download or read book The Metabotropic Glutamate Receptors written by P. Jeffrey Conn and published by Springer Science & Business Media. This book was released on 2013-03-09 with total page 284 pages. Available in PDF, EPUB and Kindle. Book excerpt: The Metabotropic Glutamate Receptors offers state-of-the-art summaries and reviews of virtually everything known today about metabotropic glutamate receptors (mGluRs), including their molecular biology, pharmacology, anatomical distribution, and physiological and pathological roles. Illuminating the overall role played by this crucial class of receptors in brain function, the book also pinpoints those areas in which there is the greatest continuing need for focused research. Because mGluRs have the potential for participating in virtually all known functions of the central nervous system (CNS), the opportunity now exists to develop pharmacological agents that can potentially alter many brain disease processes by selective interaction with precise CNS functions. With its critical and insightful reviews, The Metabotropic Glutamate Receptors will immediately become your essential key to the development of novel treatment strategies for the widest variety of neurological disorders.

G Protein-Coupled Receptor Signaling

Author : Mario Tiberi
Publisher : Humana Press
ISBN 13 : 9781493991204
Total Pages : 406 pages
Book Rating : 4.9/5 (912 download)

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Book Synopsis G Protein-Coupled Receptor Signaling by : Mario Tiberi

Download or read book G Protein-Coupled Receptor Signaling written by Mario Tiberi and published by Humana Press. This book was released on 2019-03-01 with total page 406 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Structural Biology in Drug Discovery

Author : Jean-Paul Renaud
Publisher : John Wiley & Sons
ISBN 13 : 1118900502
Total Pages : 1367 pages
Book Rating : 4.1/5 (189 download)

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Book Synopsis Structural Biology in Drug Discovery by : Jean-Paul Renaud

Download or read book Structural Biology in Drug Discovery written by Jean-Paul Renaud and published by John Wiley & Sons. This book was released on 2020-01-09 with total page 1367 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins

Novel Antipsychotic Drugs

Author : Herbert Y. Meltzer
Publisher : Raven Press (ID)
ISBN 13 :
Total Pages : 296 pages
Book Rating : 4.3/5 (91 download)

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Book Synopsis Novel Antipsychotic Drugs by : Herbert Y. Meltzer

Download or read book Novel Antipsychotic Drugs written by Herbert Y. Meltzer and published by Raven Press (ID). This book was released on 1992 with total page 296 pages. Available in PDF, EPUB and Kindle. Book excerpt: Contains highlights of an American College of Neuropsychopharmacology conference on new directions in the development of atypical and other novel antipsychotic drugs. Presents new theories and preclinical and clinical data on various drugs and classes of drugs including amperozide and other drugs.

G Protein-Coupled Receptors - Part B

Author :
Publisher : Elsevier
ISBN 13 : 0323994350
Total Pages : 194 pages
Book Rating : 4.3/5 (239 download)

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Book Synopsis G Protein-Coupled Receptors - Part B by :

Download or read book G Protein-Coupled Receptors - Part B written by and published by Elsevier. This book was released on 2023-01-25 with total page 194 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Author : Georges Vauquelin
Publisher : John Wiley & Sons
ISBN 13 : 9780470516645
Total Pages : 264 pages
Book Rating : 4.5/5 (166 download)

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Book Synopsis G Protein-coupled Receptors by : Georges Vauquelin

Download or read book G Protein-coupled Receptors written by Georges Vauquelin and published by John Wiley & Sons. This book was released on 2008-03-11 with total page 264 pages. Available in PDF, EPUB and Kindle. Book excerpt: G protein-coupled receptors (GPCRs) are membrane proteins that transduce a vast array of extracellular signals into intracellular reactions ranging from cell-cell communication processes to physiological responses. They play an important role in a variety of diseases from cancer and diabetes, to neurodegenerative, inflammatory and respiratory disorders. GPCRs are therefore of utmost interest in drug development: over half of all prescription drugs currently on the market act by targeting these receptors directly or indirectly. G Protein-coupled Receptors: Molecular Pharmacology provides a clear summary of the current knowledge in this fast-evolving field. The book sets out with an introduction to signalling molecules and their receptors, and an overview of the technical approaches used to investigate these interactions. Structural, functional and especially pharmacological aspects of GPCRs are then discussed in more detail and much attention is devoted to the analysis and interpretation of experimental data. The now widespread use of recombinant cell lies, receptor mutants and related artifices in drug research is critically evaluated. Special attention is also devoted to topical but often poorly understood concepts, such as insurmountable antagonism, inverse agonism and allosteric interactions. By combining general information with the major state-of-the-art concepts in GPCR-research, this outstanding book equips the reader with the necessary background for understanding and critically evaluating the current literature. Written by two experts from academia and industry, G Protein-coupled Receptors: Molecular Pharmacology offers a unique view of academic and applied approaches aiming to reveal new ideas in pharmaceutical research. The book is of interest to anyone involved in drug development and preclinical research and those who need to function within multi-disciplinary teams in the pharmaceutical industry: from investigators to product managers or clinicians who seek to have a broad mechanistic understanding of drug-receptor interactions. It is also an invaluable resource for final year undergraduate and postgraduate students in pharmacology and cell and molecular biology.