The G Protein-Coupled Receptors Handbook

The G Protein-Coupled Receptors Handbook

Author: Lakshmi A. Devi

Publisher: Springer Science & Business Media

Published: 2008-03-01

Total Pages: 414

ISBN-13: 1592599192

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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.


G Protein-Coupled Receptors in Drug Discovery

G Protein-Coupled Receptors in Drug Discovery

Author: Wayne R. Leifert

Publisher: Humana Press

Published: 2009-06-09

Total Pages: 0

ISBN-13: 9781603273169

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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.


G Protein-Coupled Receptor--Protein Interactions

G Protein-Coupled Receptor--Protein Interactions

Author: Susan R. George

Publisher: Wiley-Liss

Published: 2005-03-31

Total Pages: 362

ISBN-13:

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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.


The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems

The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems

Author: Terrence P. Kenakin

Publisher: Springer Science & Business Media

Published: 2000

Total Pages: 482

ISBN-13: 9783540661245

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The technology of drug testing is rapidly advancing. This book brings together world renowned experts in the fields of pharmacology and physiology united with the common theme of describing methods, theoretical concepts and in vitro systems used to study drug receptor mechanisms and the action of drugs on receptors. The first section deals with the physiology and pharmacology of integrated natural systems, the second with the new theoretical ideas used to model receptor systems (i.e. the nature of efficacy, receptor activation) and the third with the new in vitro systems available for the study of receptors and drugs. The latest ideas regarding receptor theory are critically evaluated and presented to the reader.


GPCR Molecular Pharmacology and Drug Targeting

GPCR Molecular Pharmacology and Drug Targeting

Author: Annette Gilchrist

Publisher: John Wiley & Sons

Published: 2010-12-10

Total Pages: 675

ISBN-13: 1118035178

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G protein-coupled receptors (GPCRs) are a large protein family of transmembrane receptors vital in dictating cellular responses. GPCRs are involved in many diseases, but are also the target of around half of all modern medicinal drugs. Shifting Paradigms in G Protein Coupled Receptors takes a look at the way GPCRs are examined today, how they react, how their mutations lead to disease, and the many ways in which they can be screened for compounds that modulate them. Chemists, pharmacologists, and biologists will find essential information in this comprehensive reference.


Neuromorphic Olfaction

Neuromorphic Olfaction

Author: Krishna C. Persaud

Publisher: CRC Press

Published: 2016-04-19

Total Pages: 237

ISBN-13: 1439871728

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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


Free Fatty Acid Receptors

Free Fatty Acid Receptors

Author: Graeme Milligan

Publisher: Springer

Published: 2017-02-08

Total Pages: 258

ISBN-13: 3319506935

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This book highlights the important role free fatty acids (FFA) play as potential drug targets. While FFA have long been considered byproducts of cell metabolism, they are now recognized as ligands that regulate cell and tissue function via G-protein-coupled receptors. At least three receptors have been identified for which FFA appear to be the endogenous ligands.