Download or read book G Protein Coupled Receptor Guidebook written by Amy Sojka MS and published by Lulu.com. This book was released on 2015-07-20 with total page 40 pages. Available in PDF, EPUB and Kindle. Book excerpt: G Protein-Coupled Receptors (GPCRs) represent a versatile family of plasma membrane receptors that elicit downstream intracellular signaling events. GPCRs play central roles in many physiological processes from sensory to neurological, cardiovascular, endocrine, and reproductive functions. Moreover GPCRs represent one of the largest gene families in the human genome, encoding approximately 800 unique proteins (Pawson et al., 2014). GPCRs' unique structure and cell surface location make them ideal "druggable" targets for different drug therapies, assuring interest in the pharmaceutical and clinical medicine communities (Vischer, Watts, Nijmeijer, & Leurs, 2011). It is estimated that roughly 40%% of pharmaceuticals currently marketed target GPCRs (Vischer et al., 2011). It is important for medical illustrators to know how to illustrate GPCRs and understand the scientific literature available.

Download or read book The G Protein Coupled Receptors Handbook written by Lakshmi A. Devi and published by Springer Science & Business Media. This book was released on 2008-03-01 with total page 414 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Download or read book G Protein Coupled Receptors in Drug Discovery written by Wayne R. Leifert and published by Humana Press. This book was released on 2009-06-09 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Download or read book Identification and Expression of G Protein Coupled Receptors written by Kevin R. Lynch and published by John Wiley & Sons. This book was released on 1999-05-10 with total page 246 pages. Available in PDF, EPUB and Kindle. Book excerpt: The past decade has seen tremendous advances in the study of G protein-coupled receptors (GPCRs), including the molecular cloning and identification of more than 100 hundred GPCR genes. But while GPCRs serve as targets for more than 300 medicines in the modern pharmacopoeia, the shrinking pool of known ligands and the continuing discovery of orphan GPCR genes have underscored the need for new approaches to ligand identification. Identification and Expression of G Protein-Coupled Receptors addresses this new direction in GPCR biochemistry-offering a definitive laboratory bench manual that emphasizes expression over primary cloning strategies. In a series of expert contributions by well-known researchers, this book provides detailed protocols for various expression systems-from bacteria to mammalian cells-as well as straightforward opinions on the advantages and shortcomings of each approach. Topics covered include: * Homology screening and the polymerase chain reaction in the cloning of GPCR genes * Cloning of GPCRs using mammalian cell expression * GPCR informatics and the orphan problem * The use of Xenopus laevis oocytes for the study of GPCRs * Stable expression of GPCRs in mammalian cells * Heterologous expression in primary cell cultures * Expression of GPCR in Escherichia coli * Large scale expression and purification of GPCRs in mammalian cells * High-level expression of GPCRs in the Baculovirus/Sf9 cell expression system * Expression of GPCRs in Drosophila Schneider 2 cells * Methods for genetic analysis and ligand identification using heterologous GPCRs expressed in Saccharomyces cerevisiae Supplemented with numerous photographs and illustrations, Identification and Expression of G Protein-Coupled Receptors is important reading for biochemists, pharmacologists, neuroscientists, structural biologists, and anyone involved in GPCR-based research. It delivers a wealth of useful advice, practical tips, and invaluable insight into trends at the cutting-edge of current research.

Download or read book G Protein Coupled Receptors written by David Poyner and published by John Wiley & Sons. This book was released on 2009-12-11 with total page 310 pages. Available in PDF, EPUB and Kindle. Book excerpt: G-Protein Coupled Receptors (GPCRs) are not only the largest protein family in the human genome but are also the single biggest target for therapeutic agents. Research into GPCRs is therefore growing at a fast pace and the range of techniques that can be applied to GPCRs is vast and continues to grow. This book provides an invaluable bench-side guide into the best and most up-to-date techniques for current and future research on GPCRs. With contributions from leading international authorities, this book equips readers with clear and detailed protocols for both well-known and up-and-coming techniques along with hints and tips for success. All the methods have been tried and tested by leading international research labs and are presented in easy-to-follow stages along with a useful overview of each technique. This book is an essential resource for all researchers in molecular biology, biochemistry, pharmacology and for graduate students.

Download or read book G Protein Coupled Receptors written by Gabriel Berstein and published by CRC Press. This book was released on 2019-12-18 with total page 432 pages. Available in PDF, EPUB and Kindle. Book excerpt: Covering recently developed methods in membrane-bound receptors, this book emphasizes receptor structure and function. This book provides a broad base of knowledge. Topics include the regulation of receptors; phosphorylation of G-protein-coupled receptors and ion channel receptors; desensitization studies using electrophysiological or confocal micr

Download or read book Handbook of Receptors and Channels written by Stephen J. Peroutka and published by CRC Press. This book was released on 1993-10-20 with total page 372 pages. Available in PDF, EPUB and Kindle. Book excerpt: The cloning, sequencing, and expression of a variety of membrane receptors and channels indicate the existence of at least four "superfamilies" of molecular structures that mediate signal transduction. Presently, more than 400 receptors have been cloned and sequenced. The Handbook of Receptors and Channels is the first handbook series to present the enormous amount of new molecular biological receptor data in a practical and useful format. Each volume in this remarkable series will focus on a specific molecular superfamily of receptors. Complete amino acid sequence information on all cloned receptors, as well as relevant pharmacological information, will be included. Furthermore, the format for each of the volumes will be consistent to allow for easy comparisons of different molecular subtypes for a given transmitter. G Protein-Coupled Receptors is the first volume in this new handbook series. Topics covered in future volumes include:

Download or read book G Protein Coupled Receptors written by Sandra Siehler and published by Cambridge University Press. This book was released on 2010-09-30 with total page 446 pages. Available in PDF, EPUB and Kindle. Book excerpt: This text 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 first chapters of this book illustrate the history of GPCRs based on distinct species and genomic information. This is followed by discussion of the homo- and hetero-oligomerization features of GPCRs, including receptors for glutamate, GABAB, dopamine, and chemokines. Several chapters are devoted to the key signaling features of GPCRs. The authors take time to detail the importance of the pathophysiological function and drug targeting of GPCRs, specifically -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.

Download or read book G Protein Coupled Receptors in Drug Discovery written by Kenneth H. Lundstrom and published by CRC Press. This book was released on 2005-07-11 with total page 376 pages. Available in PDF, EPUB and Kindle. Book excerpt: The broad range of G protein-coupled receptors (GPCRs) encompasses all areas of modern medicine and have an enormous impact on the process of drug development. Using disease-oriented methods to cover everything from screening to expression and crystallization, G Protein-Coupled Receptors in Drug Discovery describes the physiological roles of GPCRs

Download or read book G Protein Coupled Receptors written by Tatsuya Haga and published by CRC Press. This book was released on 2005-08-04 with total page 336 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Download or read book Molecular Aspects of G Protein coupled Receptors written by Francisco Ciruela and published by Nova Publishers. This book was released on 2008 with total page 328 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Download or read book G Protein coupled Receptors written by Georges Vauquelin and published by John Wiley & Sons. This book was released on 2008-03-11 with total page 264 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Download or read book G Protein Coupled Receptor Dimers written by Katharine Herrick-Davis and published by Springer. This book was released on 2017-08-31 with total page 502 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Download or read book G Protein Coupled Receptors written by Tiina P. Iismaa and published by Springer Science & Business Media. This book was released on 2013-06-29 with total page 189 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is about the recent advances in the structural and functional characterization of receptors that influence intracellular signalling events through interaction with intracellular GTP-binding proteins (G proteins). Molecular cloning of members of the G protein-coupled receptor superfamily has complemented pharmacological investigations in providing a realization of the structural and functional diversity of these receptors. An increased understanding of the involvement of particular receptor subtypes in normal and pathophysiological processes represents exciting possibilities for the development of highly specific and effective therapeutic agents.

Download or read book G Protein Coupled Receptor Protein Interactions written by Susan R. George and published by Wiley-Liss. This book was released on 2005-03-31 with total page 362 pages. Available in PDF, EPUB and Kindle. Book excerpt: This exciting volume elucidates how GPCRs organize signal transduction and control intracellular activities. Chapters written by the recognized expert in each respective topic offer state-of-the-art updates on the principles and technology, as well as stepwise protocols for methods currently applied to the analysis of protein-receptor interactions.

Download or read book G Protein Coupled Receptor Genetics written by Craig W. Stevens and published by Humana Press. This book was released on 2014-01-24 with total page 423 pages. Available in PDF, EPUB and Kindle. Book excerpt: G Protein‐Coupled Receptor Genetics: Research and Methods in the Post‐Genomic Era features practical techniques inspired by the fast moving GPCR field. From powerful bioinformatic tools tracing the evolution of GPCRs, to methods for the cellular transfection of engineered viruses containing GPCRs, to optogenetic techniques that produce light-activated GPCRs in live mice, what was once science fiction is now science fact. This detailed volume includes sections covering genetic mechanisms, a genetic toolbox for GPCR discovery, as well as genetic aspects of G protein-coupled receptors in health and medicine. Written for the Methods in Pharmacology and Toxicology series, this book contains the kind of key implementation advice that encourages successful results in the lab. Authoritative and easy to use, G Protein‐Coupled Receptor Genetics: Research and Methods in the Post‐Genomic Era serves as an ideal guide for researchers aiming to continue our progress in this dynamic and exciting area of study.

Download or read book Methods for the Discovery and Characterization of G Protein Coupled Receptors written by Craig W. Stevens and published by Humana Press. This book was released on 2011-07-15 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: The goal of the characterization and discovery of G protein-coupled receptors, arguably the most important class of signaling molecules in humans and other vertebrates, has spawned numerous vital methodologies. In Methods for the Discovery and Characterization of G Protein-Coupled Receptors, experts in the field present the very latest on the methods and technology used to characterize and discover novel mechanisms of GPCRs which, in many cases, can be used directly to design experiments for the reader’s particular GPCR of interest and their specific avenue of investigation. Divided into four convenient sections, this detailed volume covers GPCRs in the genome, trafficking of GPCRs, GPCRs on the membrane, as well as the regulation of these key receptors. Chapters also feature an important section called “Future Directions” which gives the reader an insight into advances soon to be realized in each area. Written for the popular Neuromethods series, this book contains the kind of detailed description and implementation advice that is crucial for getting optimal results. Authoritative and cutting-edge, Methods for the Discovery and Characterization of G Protein-Coupled Receptors serves as an ideal guide for scientists determined to further our knowledge of crucially important set of receptors.