Structure And Function Of Gpcrs

Author : Guillaume Lebon
Publisher : Springer
Page : 289 pages
File Size : 52,5 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 : Tatsuya Haga,Shigeki Takeda
Publisher : CRC Press
Page : 336 pages
File Size : 41,5 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 : Guillaume Lebon
Publisher : Unknown
Page : 289 pages
File Size : 50,7 Mb
Release : 2019
Category : G proteins
ISBN : 303024590X

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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 : Beata Jastrzebska,Paul S.H. Park
Publisher : Academic Press
Page : 0 pages
File Size : 40,8 Mb
Release : 2019-09-12
Category : Science
ISBN : 0128162287

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GPCRs by Beata Jastrzebska,Paul S.H. Park Pdf

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.

Author : Jesus Giraldo,Jean-Philippe Pin
Publisher : Royal Society of Chemistry
Page : 548 pages
File Size : 52,5 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 : Krishna C. Persaud,Santiago Marco,Agustin Gutierrez-Galvez
Publisher : CRC Press
Page : 237 pages
File Size : 47,9 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 : Lakshmi A. Devi
Publisher : Springer Science & Business Media
Page : 414 pages
File Size : 52,9 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 : Wayne R. Leifert
Publisher : Humana Press
Page : 0 pages
File Size : 46,8 Mb
Release : 2009-06-09
Category : Medical
ISBN : 1603273166

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G Protein-Coupled Receptors in Drug Discovery by Wayne R. Leifert Pdf

The G protein-coupled receptors (GPCRs) and associated peripheral G proteins underpin a multitude of physiological processes. The GPCRs represent one of the largest superfamilies in the human genome and are a significant target for bioactive and drug discovery programs. It is estimated that greater than 50% of all drugs, including those in development, currently target GPCRs. Many of the characterized GPCRs have known ligands; however, approximately 20% of GPCRs are described as orphan GPCRs, apparent GPCRs that share the generic high-level structure charact- istic of GPCRs but whose endogenous ligand is not known. Therefore, it is expected that the field of GPCR drug discovery and development will greatly expand in the coming years with emphasis on new generations of drugs against GPCRs with unique therapeuticuseswhichmayincludedrugssuchasallostericregulators,inverseagonists, and identification of orphan GPCR ligands. AswelearnmoreaboutthemolecularsignalingcascadesfollowingGPCRactivation, we acquire a better appreciation of the complexity of cell signaling and as a result, also acquire a vast array ofnew molecularmethods toinvestigate these andother processes. Thegeneralaimofthisbookistoprovideresearcherswitharangeofprotocolsthatmay be useful in their GPCR drug discovery programs. It is also the basis for the devel- ment of future assays in this field. Therefore, the range of topics covered and the appropriate methodological approaches in GPCR drug discovery are reflected in this book. Itisinterestingtonotethatfuturedirectionsindrugdiscoverywillrequireinput and collaboration from a plethora of fields of research. As such, this book will likely be of interest to scientists involved in such fields as molecular biology, pharmacology, biochemistry, cellular signaling, and bio-nanotechnology.

Author : Jürgen Wess
Publisher : Unknown
Page : 412 pages
File Size : 43,5 Mb
Release : 1999
Category : Cell receptors
ISBN : 0471252271

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Structure-function Analysis of G Protein-coupled Receptors by Jürgen Wess Pdf

This is a study of the structure and function of G protein-coupled receptors (GPCRs) and provides an up-to-date presentation of methods, including molecular genetic, biochemical, and biophysical. It focuses on methodology, but also includes techniques that can be used by readers at the laboratory bench. Furthermore, each chapter provides background information and a discussion of key results.

Author : Anonim
Publisher : Unknown
Page : 128 pages
File Size : 47,7 Mb
Release : 1997
Category : Electronic
ISBN : OCLC:81763681

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G-protein Coupled Receptors by Anonim Pdf

Author : Antonino Belfiore,Derek LeRoith
Publisher : Springer
Page : 0 pages
File Size : 54,5 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 : Jean-Paul Renaud
Publisher : John Wiley & Sons
Page : 1367 pages
File Size : 55,6 Mb
Release : 2020-01-09
Category : Medical
ISBN : 9781118900505

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Structural Biology in Drug Discovery by Jean-Paul Renaud Pdf

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

Author : Katharine Herrick-Davis,Graeme Milligan,Giuseppe Di Giovanni
Publisher : Humana Press
Page : 501 pages
File Size : 51,5 Mb
Release : 2017-09-12
Category : Medical
ISBN : 3319601725

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G-Protein-Coupled Receptor Dimers by Katharine Herrick-Davis,Graeme Milligan,Giuseppe Di Giovanni Pdf

G-protein-coupled receptors (GPCRs) are believed to be the largest family of membrane proteins involved in signal transduction and cellular responses. They dimerize (form a pair of macromolecules) with a wide variety of other receptors. The proposed book will provide a comprehensive overview of GPCR dimers, starting with a historical perspective and including, basic information about the different dimers, how they synthesize, their signaling properties, and the many diverse physiological processes in which they are involved. In addition to presenting information about healthy GPCR dimer activity, the book will also include a section on their pathology and therapeutic potentials.

Author : Sandra Siehler,Graeme Milligan
Publisher : Cambridge University Press
Page : 447 pages
File Size : 43,8 Mb
Release : 2010-09-30
Category : Medical
ISBN : 9781139491747

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G Protein-Coupled Receptors by Sandra Siehler,Graeme Milligan Pdf

Provides a comprehensive overview of recent discoveries and current understandings of G protein-coupled receptors (GPCRs). Recent advances include the first mammalian non-rhodopsin GPCR structures and reconstitution of purified GPCRs into membrane discs for defined studies, novel signaling features including oligomerization, and advances in understanding the complex ligand pharmacology and physiology of GPCRs, in new assay technologies and drug targeting. The authors take time to detail the importance of the pathophysiological function and drug targeting of GPCRs, specifically β-adrenoceptors in cardiovascular and respiratory diseases, metabotropic glutamate receptors in CNS disorders, S1P receptors in the immune system, and Wnt/Frizzled receptors in osteoporosis. This book will be invaluable to researchers and graduate students in academia and industry who are interested in the GPCR field.

Author : Kjell Fuxe,Luigi F. Agnati
Publisher : Springer Science & Business Media
Page : 577 pages
File Size : 53,5 Mb
Release : 2013-03-13
Category : Computers
ISBN : 9781468454154

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