Functional Selectivity Of G Protein Coupled Receptor Ligands

Author : Kim Neve
Publisher : Springer Science & Business Media
Page : 290 pages
File Size : 46,5 Mb
Release : 2009-02-27
Category : Medical
ISBN : 9781603273350

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Functional Selectivity of G Protein-Coupled Receptor Ligands by Kim Neve Pdf

Functional selectivity refers to the ability of different ligands acting at one receptor subtype to activate multiple signaling pathways in unique combinations; that is, one drug can be an agonist at pathway A and an antagonist or partial agonist at pathway B, and another drug can have the reverse profile. Functional selectivity has profound implications for drug development, for chemical biology, and for the design of experiments to characterize receptor function. In Functional Selectivity of G Protein-Coupled Receptors expert neuroscientists and pharmacologists review the work that demonstrated the existence of functional selectivity, placed it within a theoretical framework, and provided a mechanistic basis for the phenomenon. This exciting, comprehensive, and future-oriented volume includes chapters that focus on theoretical and mechanistic aspects of functional selectivity and that cut across subfamilies of GPCRs. Additional chapters focus on subfamilies of therapeutically relevant receptors where there is considerable evidence of ligand functional selectivity. Accessible and authoritative, Functional Selectivity of G Protein-Coupled Receptors is a valuable educational tool and reference source for students and scientists interested in drug development, chemical biology, and GPCR function.

Author : Tatsuya Haga,Shigeki Takeda
Publisher : CRC Press
Page : 336 pages
File Size : 45,6 Mb
Release : 2005-08-04
Category : Medical
ISBN : 9781420038279

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G Protein-Coupled Receptors by Tatsuya Haga,Shigeki Takeda Pdf

This book provides a broad base of knowledge of G-protein-coupled receptors. Useful at both the university and industrial levels, this book is of particular interest to those who are developing therapeutic approaches to diseases using drugs that influence receptor activation.

Author : Lakshmi A. Devi
Publisher : Springer Science & Business Media
Page : 414 pages
File Size : 51,5 Mb
Release : 2008-03-01
Category : Medical
ISBN : 9781592599196

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The G Protein-Coupled Receptors Handbook by Lakshmi A. Devi Pdf

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.

Author : Richard R. Neubig
Publisher : Academic Press
Page : 408 pages
File Size : 42,9 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 : Jesus Giraldo,Jean-Philippe Pin
Publisher : Royal Society of Chemistry
Page : 548 pages
File Size : 43,7 Mb
Release : 2011-08-16
Category : Science
ISBN : 9781849733441

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G Protein-Coupled Receptors by Jesus Giraldo,Jean-Philippe Pin Pdf

G protein-coupled receptors (GPCRs) are the largest family of cell-surface receptors, with more than 800 members identified thus far in the human genome. They regulate the function of most cells in the body, and represent approximately 3% of the genes in the human genome. These receptors respond to a wide variety of structurally diverse ligands, ranging from small molecules, such as biogenic amines, nucleotides and ions, to lipids, peptides, proteins, and even light. Ligands (agonists and antagonists) acting on GPCRs are important in the treatment of numerous diseases, including cardiovascular and mental disorders, retinal degeneration, cancer, and AIDS. It is estimated that these receptors represent about one third of the actual identified targets of clinically used drugs. The determination of rhodopsin crystal structure and, more recently, of opsin, 1 and 2 adrenergic and A2A adenosine receptors provides both academia and industry with extremely valuable data for a better understanding of the molecular determinants of receptor function and a more reliable rationale for drug design. GPCR structure and function constitutes a hot topic. The book, which lies between the fields of chemical biology, molecular pharmacology and medicinal chemistry, is divided into three parts. The first part considers what receptor structures tell us about the mechanism of receptor activation. Part II focuses on receptor function. It discusses what the data from biophysical and mutational studies, and the analysis of the interactions of the receptor with ligands and regulator proteins, tell us about the process of signal transduction. The final part, on modelling and simulation, details new insights on the link between structure and mechanism and their implications in drug design.

Author : Didier Rognan
Publisher : John Wiley & Sons
Page : 300 pages
File Size : 51,5 Mb
Release : 2006-03-10
Category : Medical
ISBN : 3527312846

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Ligand Design for G Protein-coupled Receptors, Volume 30 by Didier Rognan Pdf

1. G protein-coupled receptors in the human genome -- 2. Why G protein-coupled receptors databases are needed -- 3. A novel drug screening assay for G protein-coupled receptors -- 4. Importance of GPCR dimerization for function : the case of the class C GPCRs -- 5. Molecular mechanisms of GPCR activation -- 6. Allosteric properties and regulation of G protein-coupled receptors -- 7. Chemogenomics approaches to ligand design -- 8. Strategies for the design of pGPCR-targeted libraries -- 9. Ligand-based rational design : virtual screening -- 10. 3-D structure of G protein-coupled receptors --11. 7TM models in structure-based drug design -- 12. Receptor-based rational design : virtual screening.

Author : Guillaume Lebon
Publisher : Springer
Page : 289 pages
File Size : 50,9 Mb
Release : 2019-08-01
Category : Science
ISBN : 9783030245917

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Structure and Function of GPCRs by Guillaume Lebon Pdf

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.

Author : Xinfeng Zhao,Qian Li,Jing Wang,Qi Liang,Jia Quan
Publisher : Springer Nature
Page : 100 pages
File Size : 42,8 Mb
Release : 2023-02-20
Category : Science
ISBN : 9789819900787

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G Protein-Coupled Receptors by Xinfeng Zhao,Qian Li,Jing Wang,Qi Liang,Jia Quan Pdf

This book summarizes the progress made to functional immobilize G protein-coupled receptors (GPCRs) through site-specific or orientated recognition in both non-covalent and covalent manners. The last decade is the dawn of the “post-structural biology” era for G protein-coupled receptor research. As an emerging approach for state-of-the-art immobilization, this book discusses efforts to explore the elegance of naturally-occurring biochemical reactions by using their high specificity and robust reactivity in the complex system, such as site-specific conjugation by covalent recognition between enzymes and their substrates. With the perspective of protein-drug interactions, this book also reviews the applications of protein immobilization, with an emphasis on G protein-coupled receptors, in drug discovery and protein-ligand interaction analysis. In addition, the merits, opportunities and disadvantages are analyzed for different immobilization methods, and a perspective for future directions is presented. Given its scope, this book appeals to a broad readership, particularly researchers engaged in the field of analytical chemistry, bioconjugate chemistry, and chemical biology, and other related field, as well as teachers of relevant majors in colleges and universities.

Author : Antonino Belfiore,Derek LeRoith
Publisher : Springer
Page : 0 pages
File Size : 51,6 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 : Amitabha Chattopadhyay
Publisher : CRC Press
Page : 230 pages
File Size : 47,6 Mb
Release : 2007-05-17
Category : Medical
ISBN : 9781420005752

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Serotonin Receptors in Neurobiology by Amitabha Chattopadhyay Pdf

A number of developments spanning a multitude of techniques makes this an exciting time for research in serotonin receptors. A comprehensive review of the subject from a multidisciplinary perspective, Serotonin Receptors in Neurobiology is among the first books to include information on serotonin receptor knockout studies. With contributions from l

Author : Brian J Arey
Publisher : Elsevier
Page : 316 pages
File Size : 47,9 Mb
Release : 2014-06-05
Category : Medical
ISBN : 9780124115071

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Biased Signaling in Physiology, Pharmacology and Therapeutics by Brian J Arey Pdf

Biased Signaling in Physiology, Pharmacology and Therapeutics is a unique and essential reference for the scientific community concerning how conformational-dependent activation is a common phenomenon across many classes of receptors or signaling molecules. It discusses the role of conformational dynamics in leading to signaling bias across different classes of receptors and signaling molecules. By providing a broader view of signaling bias, this resource helps to explain common mechanisms shared across receptor classes and how this can be utilized to elucidate their cellular activity and better understand their therapeutic potential. Written for both new and established scientists in pharmacology, cell biology, biochemistry, and signal transduction, as well as physicians, this book clearly illustrates how biased receptor signaling can be utilized to develop and understand complex pharmacology. Chapters are each focused on a specific class of receptor or other important topic and make use of real-world examples illustrating how the latest research in signal transduction has led to a better understanding of pharmacology and cell biology. This structure creates a basis for understanding that physiological signalling bias has been selected by nature in order to provide complex and tissue- specific biological responses in the face of limited receptors and signaling pathways. This book provides a framework to reveal that these physiological mechanisms are not restricted to one receptor type or family and thus presents receptor signaling from a newer, more global perspective. Offers a unique and valuable resource on biased receptor signaling that provides a global view for better understanding pharmacology across many receptor families Integrates biased receptor signaling, physiology, and pharmacology to place this emerging science within the context of treating disease Includes important chapters on both the pharmaceutical and therapeutic implications of biased signaling

Author : Francisco Ciruela,Rafael Luján
Publisher : Nova Publishers
Page : 328 pages
File Size : 54,8 Mb
Release : 2008
Category : Science
ISBN : 1600219152

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Molecular Aspects of G Protein-coupled Receptors by Francisco Ciruela,Rafael Luján Pdf

In the recent years, studies based on two-hybrid screens, proteomic, biochemical and cell biology approaches, have shown that intracellular domains of G protein-coupled receptors (GPCR) or heptaspanning membrane receptors (HSMRs) interact with intracellular proteins. These interactions are the basis of a protein network associated to these receptors which includes scaffolding proteins containing one or several PDZ (post-synaptic density-95, discs large, zona occludens-1) domains, signalling proteins and proteins of the cytoskeleton. The present book is focused on the emerging evidence for interactions of G protein-coupled receptors with scaffolding, cytoskeletal and signalling proteins that will play a role in the targeting, anchoring and functioning of these receptors in the plasma membrane, thus contributing to cell development and plasticity.

Author : Todd A. Riccobene
Publisher : Unknown
Page : 322 pages
File Size : 43,6 Mb
Release : 1999
Category : Electronic
ISBN : UOM:39015043227878

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Analysis of G-protein Coupled Receptor Signaling by Todd A. Riccobene Pdf

Author : Marta Filizola
Publisher : Springer Science & Business Media
Page : 228 pages
File Size : 54,6 Mb
Release : 2013-10-25
Category : Science
ISBN : 9789400774230

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G Protein-Coupled Receptors - Modeling and Simulation by Marta Filizola Pdf

G protein-coupled receptors (GPCRs) are heptahelical transmembrane receptors that convert extra-cellular stimuli into intra-cellular signaling, and ultimately into biological responses. Since GPCRs are natural targets for approximately 40% of all modern medicines, it is not surprising that they have been the subject of intense research. Notwithstanding the amount of data generated over the years, discovering ligands of these receptors with optimal therapeutic properties is not straightforward and has certainly been hampered for years by the lack of high-resolution structural information about these receptors. Luckily, there has been a steady increase of high-resolution crystal structures of these receptors since 2007, and this information, integrated with dynamic inferences from computational and experimental methods, holds great potential for the discovery of new, improved drugs. This book, which provides, for the first time, state-of-the-art views on modeling and simulation of GPCRs, is divided into 4 parts. In the first part, the impact of currently available GPCR crystal structures on structural modeling is discussed extensively as are critical insights from simulations in the second part of the book. The third part reports recent progress in rational ligand discovery and mathematical modeling, whereas the fourth part provides an overview of bioinformatics tools and resources that are available for GPCRs.

Author : Anonim
Publisher : Academic Press
Page : 495 pages
File Size : 47,9 Mb
Release : 2012-12-02
Category : Science
ISBN : 9780123947918

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Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors by Anonim Pdf

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