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Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors

Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors
  • Author : Anonim
  • Publisher :Unknown
  • Release Date :2012-12-02
  • Total pages :488
  • ISBN : 9780123947918
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Summary : 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

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

From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors
  • Author : Anonim
  • Publisher :Unknown
  • Release Date :2020-05-13
  • Total pages :328
  • ISBN : 9780128201886
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Summary : 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 Receptor Modulation in Drug Targeting

Allosteric Receptor Modulation in Drug Targeting
  • Author : Norman G. Bowery
  • Publisher :Unknown
  • Release Date :2016-04-19
  • Total pages :376
  • ISBN : 1420016180
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Summary : 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 those already working in the field with specific reference information. This title provides in-depth chapters on basic principles of allosterism and its significance at GABAA, 5HT3, nicotinic, and GABAB receptors, ionotropic and metabotropic receptors for glutamate, muscarinic receptors and alpha 2 adrenoceptors to provide a firm foundation to the subject.

Protein Allostery in Drug Discovery

Protein Allostery in Drug Discovery
  • Author : Jian Zhang,Ruth Nussinov
  • Publisher :Unknown
  • Release Date :2019-11-09
  • Total pages :384
  • ISBN : 9789811387197
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Summary : 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

Allosteric Modulation of G Protein-coupled Receptors
  • Author : Joaquin Botta
  • Publisher :Unknown
  • Release Date :2018
  • Total pages :229
  • ISBN : OCLC:1108701507
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Summary :

Allosterism in Drug Discovery

Allosterism in Drug Discovery
  • Author : Dario Doller
  • Publisher :Unknown
  • Release Date :2016-11-24
  • Total pages :437
  • ISBN : 9781782624592
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Summary : 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.

The Metabotropic Glutamate Receptors

The Metabotropic Glutamate Receptors
  • Author : P. Jeffrey Conn,Jitendra Patel
  • Publisher :Unknown
  • Release Date :2013-03-09
  • Total pages :277
  • ISBN : 9781475722987
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Summary : 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.

Computational Methods for GPCR Drug Discovery

Computational Methods for GPCR Drug Discovery
  • Author : Alexander Heifetz
  • Publisher :Unknown
  • Release Date :2018-08-30
  • Total pages :436
  • ISBN : 1493984942
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Summary : 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.

GPCR Molecular Pharmacology and Drug Targeting

GPCR Molecular Pharmacology and Drug Targeting
  • Author : Annette Gilchrist
  • Publisher :Unknown
  • Release Date :2010-12-10
  • Total pages :544
  • ISBN : 1118035178
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Summary : G protein-coupled receptors (GPCRs) are a large protein family of transmembrane receptors vital in dictating cellular responses. GPCRs are involved in many diseases, but are also the target of around half of all modern medicinal drugs. Shifting Paradigms in G Protein Coupled Receptors takes a look at the way GPCRs are examined today, how they react, how their mutations lead to disease, and the many ways in which they can be screened for compounds that modulate them. Chemists, pharmacologists, and biologists will find essential information in this comprehensive reference.

Pharmacology of G Protein Coupled Receptors

Pharmacology of G Protein Coupled Receptors
  • Author : Anonim
  • Publisher :Unknown
  • Release Date :2011-09-08
  • Total pages :408
  • ISBN : 9780123859532
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Summary : 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

GPCRs

GPCRs
  • Author : Beata Jastrzebska,Paul S.-H. Park
  • Publisher :Unknown
  • Release Date :2019-09-11
  • Total pages :500
  • ISBN : 9780128167281
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Summary : 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

Receptor-Receptor Interactions

Receptor-Receptor Interactions
  • Author : Kjell Fuxe,Luigi F. Agnati
  • Publisher :Unknown
  • Release Date :2013-03-13
  • Total pages :580
  • ISBN : 9781468454154
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Summary :

Insights into Receptor Function and New Drug Development Targets

Insights into Receptor Function and New Drug Development Targets
  • Author : P. Michael Conn,Claude Kordon
  • Publisher :Unknown
  • Release Date :2006-09-28
  • Total pages :202
  • ISBN : 3540344470
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Summary : 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.

The Adenosine Receptors

The Adenosine Receptors
  • Author : Pier Andrea Borea,Katia Varani,Stefania Gessi,Stefania Merighi,Fabrizio Vincenzi
  • Publisher :Unknown
  • Release Date :2018-07-28
  • Total pages :593
  • ISBN : 9783319908083
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Summary : This book traces the history of adenosine receptor research from molecular biology to medicinal chemistry to behavior, including their implications in disease and potential strategies as therapeutic targets. It provides the reader with a comprehensive overview of the adenosine receptors that includes information on all subtypes - A1, A2A, A2B and A3. Aspects addressed include the most up to date information on their functional distribution in the nervous and peripheral systems, behavioral roles in inflammation, cancer, pain and neurological diseases such as Huntington’s disease, Epilepsy, Parkinson’s disease and Alzheimer’s disease.

Metabotropic GPCRs: TGR5 and P2Y Receptors in Health and Diseases

Metabotropic GPCRs: TGR5 and P2Y Receptors in Health and Diseases
  • Author : Senthilkumar Rajagopal,Murugavel Ponnusamy
  • Publisher :Unknown
  • Release Date :2018-11-19
  • Total pages :76
  • ISBN : 9789811315718
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Summary : 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.

Lipid Peroxidation

Lipid Peroxidation
  • Author : Angel Catalá
  • Publisher :Unknown
  • Release Date :2017
  • Total pages :376
  • ISBN : 1536105309
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Summary : This book presents an overview of lipid peroxidation: inhibition, effects and mechanisms. The topics analyzed, cover a broad spectrum of functions played by lipid peroxidation and presents new information in this area of research. The topics analyzed include: progress in the knowledge of lipid peroxidation, from the first evidences issued by Nicolas Theodore de Saussure in Paris 1804; fighting against lipid peroxidation: the unique story of docosahexaenoic acid in the brain; protective effects of melatonin and structurally-related molecules in reducing membrane rigidity due to lipid peroxidation; synergistic effects of antioxidant compositions during inhibited lipid autoxidation; lipid peroxidation and animal longevity; free radicals in health and disease; lipid peroxidation in autoimmune diseases; aldehydes derived from lipid peroxidation in cancer and autoimmunity; the role of reactive oxygen species and lipid peroxidation in the neurodegenerative process after spinal cord injury; kinetics and mechanisms of inhibited lipid autoxidation in presence of 4-substituted-coumarins; hypoxia and oxidative stress: cell signaling mechanisms and protective role of vitamin C and cilnidipine; characterization of oxidative stress and antioxidant potency; paying attention to time and location; lipid peroxidation in aquatic organisms: ontogenetic, phylogenetic and ecological aspects; chemistry of lipid oxidation in edible oils; and menopause progression and oxidative stress: associated mechanisms and the importance of physical exercise.

Structure and Function of GPCRs

Structure and Function of GPCRs
  • Author : Guillaume Lebon
  • Publisher :Unknown
  • Release Date :2019-08-01
  • Total pages :289
  • ISBN : 9783030245917
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Summary : 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.

Drug Discovery Strategies and Methods

Drug Discovery Strategies and Methods
  • Author : Alexandros Makriyannis,Diane Biegel
  • Publisher :Unknown
  • Release Date :2003-11-04
  • Total pages :348
  • ISBN : 9780824757670
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Summary : Navigate the complex and multidisciplinary path of drug discovery procedures with Drug Discovery Strategies and Methods-a well-organized and timely reference that analyzes methods in target identification and validation, lead detection, compound optimization, and biological testing. This volume addresses challenges encountered during the discovery of new pharmaceutical candidates including the use of cutting-edge techniques utilized in drug design and development. It considers key elements in the drug design cycle ranging from appropriateness of targets and disease models to compound characterization, safety, and efficacy and the role of protein crystallography in structure-based drug design.

A Pharmacology Primer

A Pharmacology Primer
  • Author : Terry Kenakin
  • Publisher :Unknown
  • Release Date :2018-10-26
  • Total pages :488
  • ISBN : 9780128139585
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Summary : A Pharmacology Primer: Techniques for More Effective and Strategic Drug Discovery, Fifth Edition features the latest ideas and research regarding the application of pharmacology to the process of drug discovery. Written by well-respected pharmacologist, Terry P. Kenakin, this primer is an indispensable resource for all those involved in drug discovery. This updated edition has been thoroughly revised to include material on quantifying drug efficacy through bias and cluster analysis, the impact of molecular dynamics and protein structural analysis, the real time kinetic analysis of drug effect, virtual screening for new drug chemical scaffolds, and much more. With full color illustrations and new examples throughout, this book remains a top reference for all industry and academic scientists that is also ideal for students directly involved in drug discovery or pharmacologic research. Highlights changes surrounding strategies for drug discovery, providing a comprehensive reference and featuring advances in the methods involved Includes multiple new sections, such as development and utilization of models in pharmacology, de-orphanization of new drug targets, predicting impact of disease on drug pharmacokinetics, and the impact of enzyme kinetics on drug-drug interactions Illustrates the application of rapid inexpensive assays to predict activity in the therapeutic setting, showing data outcomes and the limitations inherent in interpreting this data

Muscarinic Receptor: From Structure to Animal Models

Muscarinic Receptor: From Structure to Animal Models
  • Author : Jaromir Myslivecek,Jan Jakubik
  • Publisher :Unknown
  • Release Date :2015-08-05
  • Total pages :287
  • ISBN : 1493928570
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Summary : This volume provides methods for characterization of muscarinic receptor in crystallography studies that advanced our understanding of structural properties and activation mechanism of muscarinic receptors and are cornerstone in molecular modeling and computer‐based approaches to study muscarinic receptors. Muscarinic Receptor: From Structure to Animal Models guides readers through binding techniques, protocols to investigate molecular properties of muscarinic receptors, protocols to study muscarinic receptors in the central nervous system using autoradiography and PET studies and protocols on animals with knock-out and knock-in muscarinic genes to study role of muscarinic receptors in physiology and behavior. Written in the popular Neuromethods series style, chapters include the kind of detail and key advice from the specialists needed to get successful results in your own laboratory. Concise and easy-to-use, Muscarinic Receptor: From Structure to Animal Models aims to ensure successful results in the further study of this vital field.

GABAB Receptor

GABAB Receptor
  • Author : Giancarlo Colombo
  • Publisher :Unknown
  • Release Date :2016-12-19
  • Total pages :385
  • ISBN : 9783319460444
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Summary : An up-to-date comprehensive overview of the GABA B receptor system with a particular focus on the most recent therapeutic applications and potential. This receptor system has recently been implicated in several diseases and disorders including gastroesophageal reflux disease, epilepsy, mood disorders, depression, and alcohol and substance use disorder. The authors, leading researchers in the field, explore a number of approaches, including medicinal chemistry, molecular biology, physiology, and preclinical and clinical pharmacology. This overview provides a translational perspective on the potential of the GABA B receptor pharmacology.