Gpcrs

Author : Beata Jastrzebska,Paul S.H. Park
Publisher : Academic Press
Page : 0 pages
File Size : 45,8 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 : Georges Vauquelin,Bengt von Mentzer
Publisher : John Wiley & Sons
Page : 264 pages
File Size : 46,6 Mb
Release : 2008-03-11
Category : Medical
ISBN : 047051664X

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G Protein-coupled Receptors by Georges Vauquelin,Bengt von Mentzer Pdf

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.

Author : Katharine Herrick-Davis,Graeme Milligan,Giuseppe Di Giovanni
Publisher : Springer
Page : 501 pages
File Size : 49,5 Mb
Release : 2017-08-31
Category : Medical
ISBN : 9783319601748

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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 : Wayne R. Leifert
Publisher : Humana Press
Page : 376 pages
File Size : 52,6 Mb
Release : 2016-08-23
Category : Medical
ISBN : 1493957066

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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 : Sofia Aires M. Martins,Duarte Miguel F. Prazeres
Publisher : Humana
Page : 327 pages
File Size : 41,6 Mb
Release : 2022-06-19
Category : Science
ISBN : 1071612239

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G Protein-Coupled Receptor Screening Assays by Sofia Aires M. Martins,Duarte Miguel F. Prazeres Pdf

This fully updated edition targets not only those assays directly involved in the discovery of GPCR-active compounds but also those involved in cell-based experiments designed to study physiological responses. Whether coming from academia or industry, or being an experienced researcher or a newcomer to the field, the reader will find accessible methods and protocols that cover the latest developments on receptor purification, molecular biology, recombinant engineering, and analytical techniques that enable the real time monitoring of the complex GPCR signaling cascade and identification of potential drug targets. 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 up-to-date, G Protein-Coupled Receptor Screening Assays: Methods and Protocols, Second Edition aims to provide the tools necessary to contribute to the advancement of GPCR research and discovery and ultimately lead to the availability of innovative and more efficient drugs.

Author : Krishna C. Persaud,Santiago Marco,Agustin Gutierrez-Galvez
Publisher : CRC Press
Page : 237 pages
File Size : 43,5 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 : Denis J. Dupré,Terence E. Hébert,Ralf Jockers
Publisher : Springer Science & Business Media
Page : 298 pages
File Size : 55,7 Mb
Release : 2012-11-19
Category : Medical
ISBN : 9789400747654

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GPCR Signalling Complexes – Synthesis, Assembly, Trafficking and Specificity by Denis J. Dupré,Terence E. Hébert,Ralf Jockers Pdf

Main Question: G protein coupled receptors are involved in highly efficient and specific activation of signalling pathways. How do GPCR signalling complexes get assembled to generate such specificity? In order to answer this question, we need to understand how receptors and their signalling partners are synthesized, folded and quality-controlled in order to generate functional proteins. Then, we need to understand how each partner of the signalling complex is selected to join a complex, and what makes this assembly possible. GPCRs are known to be able to function as oligomers, what drives the assembly into oligomers and what will be the effects of such organization on specificity and efficacy of signal transduction. Once the receptor complexes are assembled, they need to reach different locations in the cell; what drives and controls the trafficking of GPCR signalling complexes. Finally, defects in synthesis, maturation or trafficking can alter functionality of GPCRs signalling complexes; how can we manipulate the system to make it function normally again? Pharmacological chaperones may just be part of the answer to this question.

Author : Jae Young Seong,Hubert Vaudry
Publisher : Frontiers E-books
Page : 826 pages
File Size : 43,7 Mb
Release : 2014-11-07
Category : Diseases of the endocrine glands. Clinical endocrinology
ISBN : 9782889192670

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Neuropeptide GPCRs in neuroendocrinology by Jae Young Seong,Hubert Vaudry Pdf

The human genome encompasses ˜ 860 G protein-coupled receptors (GPCRs) including 374 non-chemosensory GPCRs. Half of these latter GPCRs recognize (neuro)peptides as natural ligands. GPCRs thus play a pivotal role in neuroendocrine communication. In particular, GPCRs are involved in the neuroendocrine control of feeding behavior, reproduction, growth, hydromineral homeostasis and stress response. GPCRs are also major drug targets and hence possess a strong potential for the development of innovative pharmaceuticals. The aim of this Research Topic was to assemble a series of review articles and original research papers on neuropeptide GPCRs and their ligands that would illustrate the different facets of the studies currently conducted in this domain.

Author : Simon Yona,Martin Stacey
Publisher : Springer Science & Business Media
Page : 216 pages
File Size : 54,6 Mb
Release : 2011-06-26
Category : Medical
ISBN : 9781441979131

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Adhesion‐GPCRs by Simon Yona,Martin Stacey Pdf

Upon completion of the human genome project over 800 G protein-coupled receptor 1 (GPCR) genes, subdivided into five categories, were identified. These receptors sense a diverse array of stimuli, including peptides, ions, lipid analogues, light and odour, in a discriminating fashion. Subsequently, they transduce a signal from the ligand–receptor complex into numerous cellular responses. The importance of GPCRs is further reflected in the fact that they constitute the most common target for therapeutic drugs across a 2 wide range of human disorders. Phylogenetic analysis of GPCRs produced the GRAFS classification system, which subdivides GPCRs into five discrete families: glutamate, rhodopsin, adhesion, frizzled/taste2 and secretin receptors. The adhesion-GPCR family 2 can be further subdivided into eight groups. The field of adhesion-GPCR biology has indeed become large enough to require a volume dedicated solely to this field. The contributors to this book have made a courageous effort to address the key concepts of adhesion-GPCR biology, including the evolution and biochemistry of adhesion-GPCRs; there are extensive discussions on the functional nature of these receptors during development, the immune response and tumourgenesis. Finally, there are chapters dedicated to adhesion-GPCR signalling, an area of intense investigation.

Author : Brian J. Arey,James A. Dias
Publisher : Frontiers Media SA
Page : 117 pages
File Size : 47,9 Mb
Release : 2016-08-05
Category : Diseases of the endocrine glands. Clinical endocrinology
ISBN : 9782889199587

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The Physiology and Pharmacology of Leucine-rich Repeat GPCRs by Brian J. Arey,James A. Dias Pdf

G protein-coupled receptors (GPCRs) represent a large and physiologically important class of cell surface receptors. There are approximately 750 known GPCRs present in the human genome that can be subdivided into general classes based upon sequence homology within their transmembrane domains. Therapeutically, GPCRs represent a fertile source for the development of therapies as they are a significant percentage of our current pharmacopeia. Among the three subclasses of GPCRs, the Class A (rhodopsin-like) receptors are by far the most prevalent and extensively studied. However, within the Class A receptors, sub-families of receptors can be distinguished based upon common sequence motifs within the transmembrane domains as well as extracellular and intracellular domains. One such family of Class A receptors is characterized by multiple leucine- rich repeats within their amino- terminal domains (the Leucine-rich Repeat family (LRR)). This family of GPCRs are best represented by the glycoprotein hormone receptors (LHR, FSHR and TSHR) which have been studied extensively but also includes receptors for the peptide hormone relaxin (RXFP1 and RXFP2 (RXFP2 also binds insulin-like peptide 3)) and three other receptors (LGR4, LGR5 and LGR6). LGR4-6 were, until recently, considered orphan receptors. However, emerging data have revealed that these proteins are the receptors for a family of growth factors called R-spondins. Over the last 20 years much has been learned about LRR receptors, including the development of synthetic agonists and antagonists, new insights into signaling (including signaling bias) and the physiological role these receptors play in regulating the function of many tissues. This topic will focus on what is known concerning the regulation of these receptors, their signaling pathways, functional consequences of activation and pharmacology.

Author : Didier Rognan
Publisher : John Wiley & Sons
Page : 300 pages
File Size : 49,7 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 : Sameer Mohammad,Muheeb Beg,Manveen Kaur Gupta
Publisher : Frontiers Media SA
Page : 146 pages
File Size : 49,9 Mb
Release : 2022-01-28
Category : Science
ISBN : 9782889742134

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Cell Biology, Physiology and Molecular Pharmacology of G protein Coupled Receptors by Sameer Mohammad,Muheeb Beg,Manveen Kaur Gupta Pdf

Author : Lakshmi A. Devi
Publisher : Springer Science & Business Media
Page : 412 pages
File Size : 51,9 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 : Tatsuya Haga,Shigeki Takeda
Publisher : CRC Press
Page : 336 pages
File Size : 49,8 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 : Sandra Siehler,Graeme Milligan
Publisher : Cambridge University Press
Page : 447 pages
File Size : 43,6 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.