G Protein Coupled Receptors in Drug Discovery

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.

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Author: Wayne R. Leifert

Publisher: Humana Press

ISBN: 1493957066

Category: Medical

Page: 376

View: 641

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.

The G Protein Coupled Receptors Handbook

Authoritative and cutting-edge, The G Protein-Coupled Receptors Handbook offers pharmacologists, biochemists, and neuroscientists an exhaustive review of the progress made in understanding how GPCRs are activated and regulated, key factors ...

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Author: Lakshmi A. Devi

Publisher: Springer Science & Business Media

ISBN: 9781592599196

Category: Medical

Page: 412

View: 999

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.

G Protein Coupled Receptors

Covering recently developed methods in membrane-bound receptors, this book emphasizes receptor structure and function, knowledge of which is essential to the study of signal transduction.

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Author: Gabriel Berstein

Publisher: CRC Press

ISBN: 1420048511

Category: Medical

Page: 424

View: 780

Covering recently developed methods in membrane-bound receptors, this book emphasizes receptor structure and function, knowledge of which is essential to the study of signal transduction. G Protein-Coupled Receptors has culled contributors from domestic and international sources, providing a broad base of knowledge. Some topics covered are the r

G Protein Coupled Receptors

This book provides a broad base of knowledge of G-protein-coupled receptors.

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Author: Tatsuya Haga

Publisher: CRC Press

ISBN: 9781420038279

Category: Medical

Page: 336

View: 502

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.

Molecular Biology of G Protein Coupled Receptors

LESLIE L. IVERSEN The present series of volumes is well timed, as the impact of molecular genetics on pharmacology has been profound, and a comprehensive review of the rapid advances of the past decade is much needed.

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Author: M. Brann

Publisher: Birkhäuser

ISBN: 1468467743

Category: Science

Page: 326

View: 830

LESLIE L. IVERSEN The present series of volumes is well timed, as the impact of molecular genetics on pharmacology has been profound, and a comprehensive review of the rapid advances of the past decade is much needed. Since the pioneering work of Dale, Ariens, and others in the early years of this century, much of pharmacology has been founded on the concept of receptors. To begin with, the receptor was conceived of as a "black box," which recognized and transduced the biological effects of neurotransmit ters, hormones, or other biological messengers-and which could also represent a target for man-made drugs. It is only in the last two decades that "molecular pharmacology" has blossomed, first with the advent of radioligand binding techniques and second messenger studies which greatly facilitated the biochemical study of drug-receptor interactions, and latterly with increasing knowledge of the molecular architecture of the receptor proteins themselves. This started with the traditional biochemical approach of isolating and purifying the receptor molecules. This proved to be a task of immense technical difficulty because of the low density of receptors in most biological source tissues, although there were some notable successes, e. g. , the purification of the nicotinic acetylcholine receptor from the electric organ of Torpedo. It was the ap plication of molecular genetics technology during the 1980s, however, which really accelerated progress in this field.

G Protein Coupled Receptor Dimers

In addition to presenting information about healthy GPCR dimer activity, the book will also include a section on their pathology and therapeutic potentials.

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Author: Katharine Herrick-Davis

Publisher: Springer

ISBN: 9783319601748

Category: Medical

Page: 501

View: 706

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.

Methods for the Discovery and Characterization of G Protein Coupled Receptors

Written for the popular Neuromethods series, this book contains the kind of detailed description and implementation advice that is crucial for getting optimal results.

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Author: Craig W. Stevens

Publisher: Humana Press

ISBN: 1493958518

Category: Medical

Page: 428

View: 516

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.

G Protein Coupled Receptors Modeling and Simulation

This book, which provides, for the first time, state-of-the-art views on modeling and simulation of GPCRs, is divided into 4 parts.

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Author: Marta Filizola

Publisher: Springer Science & Business Media

ISBN: 9789400774230

Category: Science

Page: 228

View: 111

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.

Ligand Design for G Protein coupled Receptors Volume 30

This is the first work to describe in detail the structure-based rational approach to GPCR drug design.

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Author: Didier Rognan

Publisher: John Wiley & Sons

ISBN: 3527312846

Category: Science

Page: 264

View: 372

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.

G Protein Coupled Receptors

This book considers the relationship between structure and function in G protein-coupled receptors (GPCRs) and the implications for drug design.

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Author: Jesus Giraldo

Publisher: Royal Society of Chemistry

ISBN: 9781849731836

Category: Science

Page: 511

View: 403

This book considers the relationship between structure and function in G protein-coupled receptors (GPCRs) and the implications for drug design.