GPCRs

GPCRs
Author: Beata Jastrzebska,Paul S.-H. Park
Publsiher: Academic Press
Total Pages: 500
Release: 2019-09-11
Genre: Science
ISBN: 9780128167281

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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

GPCR Signaling in Cancer

GPCR Signaling in Cancer
Author: Arun K. Shukla
Publsiher: Academic Press
Total Pages: 312
Release: 2020-02
Genre: Electronic Book
ISBN: 9780128202302

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GPCR Signaling in Cancer, Volume 145, the latest release in the Advances in Cancer Research series, highlights recent developments in the area of GPCRs and cancer biology. Chapters included in this volume cover several GPCRs and their downstream effectors as case examples to highlight their fundamental understanding and therapeutic potential. Specific chapters address the Role of GRKs and beta-arrestins in cancer, Atypical GPCRs in cancer, the Role of a chemokine receptor (CCR) 5 in cancer, Targeting G protein-coupled receptors for therapeutics in cancer, Emerging GPCR signaling pathways in cancer, and more. G protein-coupled receptors (GPCRs) constitute a large family of cell surface receptors which are involved in nearly every cellular and physiological event. These receptors can recognize a broad array of ligands and they are targeted by nearly one third of the currently prescribed drugs including anti-cancer therapeutics.

G Protein Coupled Receptor Dimers

G Protein Coupled Receptor Dimers
Author: Katharine Herrick-Davis,Graeme Milligan,Giuseppe Di Giovanni
Publsiher: Humana Press
Total Pages: 501
Release: 2017-09-12
Genre: Medical
ISBN: 3319601725

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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.

GPCR Signalling Complexes Synthesis Assembly Trafficking and Specificity

GPCR Signalling Complexes     Synthesis  Assembly  Trafficking and Specificity
Author: Denis J. Dupré,Terence E. Hébert,Ralf Jockers
Publsiher: Springer Science & Business Media
Total Pages: 300
Release: 2012-11-19
Genre: Medical
ISBN: 9789400747654

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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.

G Protein Coupled Receptors

G Protein Coupled Receptors
Author: Anonim
Publsiher: Academic Press
Total Pages: 332
Release: 2019-01-05
Genre: Science
ISBN: 9780128151082

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G-Protein-Coupled Receptors, Part B, 2nd Edition, Volume 149, the latest release in the Methods in Cell Biology series, continues the legacy of this premier serial with quality chapters authored by leaders in the field. This volume covers Optical Approaches for Visualization of Arrestin Binding to Muscarinic Receptors, Luciferase Reporter Assay for Unlocking Ligand-mediated Signaling of GPCRs, Assays to Measure GPCR Dependent Cellular Migration, Characterization of the Frizzled GPCRs, Binding Assays for Bradykinin and Angiotensin Receptors, Detection of Misfolded Rhodopsin Aggregates in Cells, Measuring GPCR Ubiquitination and Trafficking, Culture of Primary Neurons and its Use in Studying GPCR Trafficking, and much more. Covers the increasingly appreciated cell biology field of G-protein-coupled receptors Includes both established and new technologies Contributed by experts in the field

GPCRs From Deorphanization to Lead Structure Identification

GPCRs  From Deorphanization to Lead Structure Identification
Author: H. Bourne,Richard Horuk,J. Kuhnke,H. Michel
Publsiher: Springer Science & Business Media
Total Pages: 269
Release: 2007-05-23
Genre: Medical
ISBN: 9783540489825

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This book offers an insight into the approaches taken by industry and academia to address GPCRs and depict how mature this target class-oriented research has become in the last decade. Coverage also reflects the actual trends in the fast-emerging field of GPCR research in academia and industry. It is based on the international workshop GPCRs: From Deorphanisation to Lead Structure Identification, held in Berlin in May 2006.

Modelling of GPCRs

Modelling of GPCRs
Author: Andrea Strasser,Hans-Joachim Wittmann
Publsiher: Springer Science & Business Media
Total Pages: 218
Release: 2012-08-13
Genre: Medical
ISBN: 9789400745964

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G protein coupled receptors (GPCRs) comprise an important protein family, which is involved in signal transduction in the cell. Besides that a large number of drugs, available on market, address GPCRs. For an efficient and improved development of appropriate drugs, molecular modelling of GPCRs is – in order to understand the ligand-receptor interactions and functionality of GPCRs on molecular level - an important tool. The book “Modelling of GPCRs – a practical handbook” is focussed onto a practical introduction into molecular modelling of GPCRs. This book is very useful for beginners in GPCR modelling, but also addresses the advanced GPCR modeller: On the one hand, the book introduces principles of GPCR modelling, including extensive examples. On the other hand, detailed outlooks onto advanced GPCR modelling techniques are presented. Furthermore, the book includes important data, like information about crystal structures in a summarized manner or amino acid sequences, which are essential for GPCR modelling in general. Due to an increase in efficacy and data handling most modellers use LINUX as operating system. To address this, a summary of most important LINUX commands with examples is presented within the book.

Neuropeptide GPCRs in neuroendocrinology

Neuropeptide GPCRs in neuroendocrinology
Author: Jae Young Seong,Hubert Vaudry
Publsiher: Frontiers E-books
Total Pages: 135
Release: 2014-11-07
Genre: Electronic Book
ISBN: 9782889192670

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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.

Adhesion GPCRs

Adhesion   GPCRs
Author: Simon Yona,Martin Stacey
Publsiher: Springer Science & Business Media
Total Pages: 199
Release: 2011-06-26
Genre: Medical
ISBN: 9781441979131

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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.

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
Publsiher: Springer
Total Pages: 76
Release: 2018-11-19
Genre: Medical
ISBN: 9789811315718

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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.

Trafficking of GPCRs

Trafficking of GPCRs
Author: Guangyu Wu
Publsiher: Academic Press
Total Pages: 328
Release: 2015-06-05
Genre: Science
ISBN: 9780128029558

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G protein-coupled receptors (GPCRs) constitute the largest superfamily of cell surface receptors that regulate a variety of cell functions. Over the past few decades great progress has been made in defining the roles of intracellular trafficking in controlling the functionality of the receptors as well as in the development of various human diseases. This volume of Progress in Molecular Biology and Translational Science reviews the recent understanding of GPCR trafficking regulators and molecular mechanisms. Written by future leaders in the pain field Covers a wide range of targets Contains provocative ideas about GPCR trafficking

The Physiology and Pharmacology of Leucine rich Repeat GPCRs

The Physiology and Pharmacology of Leucine rich Repeat GPCRs
Author: Brian J. Arey,James A. Dias
Publsiher: Frontiers Media SA
Total Pages: 135
Release: 2016-08-05
Genre: Electronic Book
ISBN: 9782889199587

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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.

Ligand Design for G Protein coupled Receptors Volume 30

Ligand Design for G Protein coupled Receptors  Volume 30
Author: Didier Rognan,Raimund Mannhold,Hugo Kubinyi,Gerd Folkers
Publsiher: John Wiley & Sons
Total Pages: 264
Release: 2006-03-10
Genre: Science
ISBN: 3527312846

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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.

The G Protein Coupled Receptors Handbook

The G Protein Coupled Receptors Handbook
Author: Lakshmi A. Devi
Publsiher: Springer Science & Business Media
Total Pages: 412
Release: 2008-03-01
Genre: Medical
ISBN: 9781592599196

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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.

Pharmacology of G Protein Coupled Receptors

Pharmacology of G Protein Coupled Receptors
Author: S. J. Enna
Publsiher: Academic Press
Total Pages: 391
Release: 2011
Genre: Medical
ISBN: 9780123859525

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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