Oligomerization and Allosteric Modulation in G Protein Coupled Receptors Book

Oligomerization and Allosteric Modulation in G Protein Coupled Receptors


  • Author : Anonim
  • Publisher : Academic Press
  • Release Date : 2012-12-02
  • Genre: Science
  • Pages : 488
  • ISBN 10 : 9780123947918

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Oligomerization and Allosteric Modulation in G Protein Coupled Receptors 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

Protein Allostery in Drug Discovery Book

Protein Allostery in Drug Discovery


  • Author : Jian Zhang
  • Publisher : Springer Nature
  • Release Date : 2019-11-09
  • Genre: Medical
  • Pages : 384
  • ISBN 10 : 9789811387197

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Protein Allostery in Drug Discovery 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.

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

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


  • Author : Anonim
  • Publisher : Academic Press
  • Release Date : 2020-05-22
  • Genre: Medical
  • Pages : 328
  • ISBN 10 : 9780128201879

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

Allosteric Modulation of G Protein Coupled Receptors


  • Author : Robert Laprairie
  • Publisher : Elsevier
  • Release Date : 2022-02-10
  • Genre: Business & Economics
  • Pages : 212
  • ISBN 10 : 9780128197714

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Allosteric Modulation of G Protein Coupled Receptors 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

Receptor Receptor Interactions Book

Receptor Receptor Interactions


  • Author : Kjell Fuxe
  • Publisher : Springer Science & Business Media
  • Release Date : 2013-03-13
  • Genre: Computers
  • Pages : 580
  • ISBN 10 : 9781468454154

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Receptor Receptor Interactions Excerpt :

Allosterism in Drug Discovery Book

Allosterism in Drug Discovery


  • Author : Dario Doller
  • Publisher : Royal Society of Chemistry
  • Release Date : 2016-11-24
  • Genre: Medical
  • Pages : 458
  • ISBN 10 : 9781782624592

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Allosterism in Drug Discovery Excerpt :

Although the concept of allosterism has been known for over half a century, its application in drug discovery has exploded in recent years. The emergence of novel technologies that enable molecular-level ligand-receptor interactions to be studied in studied in unprecedented detail has driven this trend. This book, written by the leaders in this young research area, describes the latest developments in allosterism for drug discovery. Bringing together research in a diverse range of scientific disciplines, Allosterism in Drug Discovery is a key reference for academics and industrialists interested in understanding allosteric interactions. The book provides an in-depth review of research using small molecules as chemical probes and drug candidates that interact allosterically with proteins of relevance to life sciences and human disease. Knowledge of these interactions can then be applied in the discovery of the novel therapeutics of the future. This book will be useful for people working in all disciplines associated with drug discovery in academia or industry, as well as postgraduate students who may be working in the design of allosteric modulators.

Oligomerization and Allosteric Modulation in G Protein Coupled Receptors Book

Oligomerization and Allosteric Modulation in G Protein Coupled Receptors


  • Author : Terry Kenakin
  • Publisher : Academic Press
  • Release Date : 2013
  • Genre: Medical
  • Pages : 471
  • ISBN 10 : 0123945879

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Oligomerization and Allosteric Modulation in G Protein Coupled Receptors 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. Key features: * Contributions from leading authorities * Informs and updates on all the latest developments in the field

Molecular Pharmacology Book

Molecular Pharmacology


  • Author : Angel Catala
  • Publisher : BoD – Books on Demand
  • Release Date : 2020-12-16
  • Genre: Medical
  • Pages : 168
  • ISBN 10 : 9781839629310

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Molecular Pharmacology Excerpt :

This book concentrates on recent developments related to the application of original structural biology, biochemistry, biophysics, physiology, genetics, and molecular biology as well as basic pharmacological problems that offer mechanistic insights that are generally significant for the field of pharmacology. Written by experts, chapters cover such topics as drug transport mechanisms and drug–receptor complexes. This volume offers up-to-date, expert reviews of the fast-moving field of molecular pharmacology.

GPCRs Book

GPCRs


  • Author : Beata Jastrzebska
  • Publisher : Academic Press
  • Release Date : 2019-09-11
  • Genre: Science
  • Pages : 500
  • ISBN 10 : 9780128167281

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GPCRs Excerpt :

GPCRS: Structure, Function, and Drug Discovery provides a comprehensive overview of recent discoveries and our current understanding of GPCR structure, signaling, physiology, pharmacology and methods of study. In addition to the fundamental aspects of GPCR function and dynamics, international experts discuss crystal structures, GPCR complexes with partner proteins, GPCR allosteric modulation, biased signaling through protein partners, deorphanization of GPCRs, and novel GPCR-targeting ligands that could lead to the development of new therapeutics against human diseases. GPCR association with, and possible therapeutic pathways for, retinal degenerative diseases, Alzheimer’s disease, Parkinson’s disease, cancer and diabetic nephropathy, among other illnesses, are examined in-depth. Addresses our current understanding and novel advances in the GPCR field, directing readers towards recent finding of key significance for translational medicine Combines a thorough discussion of structure and function of GPCRs with disease association and drug discovery Features chapter contributions from international experts in GPCR structure, signaling, physiology and pharmacology

G Protein Coupled Receptors as Drug Targets Book

G Protein Coupled Receptors as Drug Targets


  • Author : Roland Seifert
  • Publisher : John Wiley & Sons
  • Release Date : 2006-05-12
  • Genre: Science
  • Pages : 304
  • ISBN 10 : 9783527606955

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G Protein Coupled Receptors as Drug Targets Excerpt :

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.

Computational Methods for GPCR Drug Discovery Book

Computational Methods for GPCR Drug Discovery


  • Author : Alexander Heifetz
  • Publisher : Humana Press
  • Release Date : 2018-08-30
  • Genre: Medical
  • Pages : 436
  • ISBN 10 : 1493984942

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Computational Methods for GPCR Drug Discovery 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.

Metabotropic GPCRs  TGR5 and P2Y Receptors in Health and Diseases Book

Metabotropic GPCRs TGR5 and P2Y Receptors in Health and Diseases


  • Author : Senthilkumar Rajagopal
  • Publisher : Springer
  • Release Date : 2018-11-19
  • Genre: Medical
  • Pages : 76
  • ISBN 10 : 9789811315718

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Metabotropic GPCRs TGR5 and P2Y Receptors in Health and Diseases Excerpt :

This book will provide current understandings about two ubiquitously expressed metabotropic GPCRs, G-coupled purinoreceptor type 2 (P2Y) and Takeda G-protein-coupled bile acid receptor 5 (TGR5). G protein coupled receptors (GPCRs) are the largest family of proteins implicated in majority of cellular responses. The two receptor sub-families play a central role in many physiological functions as well as in many pathological conditions. This book offers up-to-date information on the physiological functions, signaling pathways and regulatory mechanisms of P2Y and TGR5 receptors. In addition, this book provides a comprehensive overview about the abnormalities of P2Y/TGR5 receptors and their contribution in the development and progression of pathological conditions. It also covers the currently available natural, chemical and pharmacological agents targeting these two receptor families and their therapeutic implications in P2Y and TGR5 associated disorders. This book is a valuable source for beginners and researchers to follow the rapidly progressing field of these two GPCR subfamily members.

G Protein Coupled Receptor Signaling Book

G Protein Coupled Receptor Signaling


  • Author : Mario Tiberi
  • Publisher : Humana Press
  • Release Date : 2019-03-01
  • Genre: Science
  • Pages : 406
  • ISBN 10 : 1493991205

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G Protein Coupled Receptor Signaling 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.

Allosteric Modulation of G Protein Coupled Receptors Book

Allosteric Modulation of G Protein Coupled Receptors


  • Author : Robert Laprairie
  • Publisher : Academic Press
  • Release Date : 2022-02-18
  • Genre: Business & Economics
  • Pages : 212
  • ISBN 10 : 9780128197721

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Allosteric Modulation of G Protein Coupled Receptors 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

Structure and Function of GPCRs Book

Structure and Function of GPCRs


  • Author : Guillaume Lebon
  • Publisher : Springer
  • Release Date : 2019-08-01
  • Genre: Science
  • Pages : 289
  • ISBN 10 : 9783030245917

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Structure and Function of GPCRs Excerpt :

This book introduces readers to the latest advances in G protein-coupled receptor (GPCR) biology. It reviews our current understanding of the structural basis of ligand binding and allosteric mechanisms, following a decade of technological breakthroughs. Several examples of structure-based drug discovery are presented, together with the future challenges involved in designing better drugs that target GPCRs. In turn, the book illustrates the important concept of GPCR biased signaling in physiological contexts, and presents fluorescent- and light-based methodologies frequently used to measure GPCR signaling or to trace their dynamics in cells upon ligand activation. Taken together, the chapters provide an essential overview and toolkit for new scientific investigators who plan to develop GPCR projects. All chapters were written by experts in their respective fields, and share valuable insights and powerful methodologies for the GPCR field.