The G Protein-Coupled Receptors Handbook

The G Protein-Coupled Receptors Handbook
Title The G Protein-Coupled Receptors Handbook PDF eBook
Author Lakshmi A. Devi
Publisher Springer Science & Business Media
Pages 414
Release 2008-03-01
Genre Medical
ISBN 1592599192

Download The G Protein-Coupled Receptors Handbook Book in PDF, Epub and Kindle

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
Title G Protein-Coupled Receptors in Drug Discovery PDF eBook
Author Wayne R. Leifert
Publisher Humana Press
Pages 0
Release 2009-06-09
Genre Medical
ISBN 9781603273169

Download G Protein-Coupled Receptors in Drug Discovery Book in PDF, Epub and Kindle

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.

Neuromorphic Olfaction

Neuromorphic Olfaction
Title Neuromorphic Olfaction PDF eBook
Author Krishna C. Persaud
Publisher CRC Press
Pages 237
Release 2016-04-19
Genre Medical
ISBN 1439871728

Download Neuromorphic Olfaction Book in PDF, Epub and Kindle

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
Title Free Fatty Acid Receptors PDF eBook
Author Graeme Milligan
Publisher Springer
Pages 258
Release 2017-02-08
Genre Medical
ISBN 3319506935

Download Free Fatty Acid Receptors Book in PDF, Epub and Kindle

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.

The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems

The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems
Title The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems PDF eBook
Author Terrence P. Kenakin
Publisher Springer Science & Business Media
Pages 482
Release 2000
Genre Medical
ISBN 9783540661245

Download The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems Book in PDF, Epub and Kindle

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.

Computational Methods for GPCR Drug Discovery

Computational Methods for GPCR Drug Discovery
Title Computational Methods for GPCR Drug Discovery PDF eBook
Author Alexander Heifetz
Publisher Humana Press
Pages 436
Release 2017-11-30
Genre Medical
ISBN 9781493974641

Download Computational Methods for GPCR Drug Discovery Book in PDF, Epub and Kindle

This volume looks at modern computational strategies and techniques used in GPCR drug discovery including structure and ligand-based approaches and cheminformatics. The chapters in this book describe how these approaches can be applied to address key drug discovery issues, such as receptor structure modelling, function and dynamics, prediction of protein-water-ligand interactions and binding kinetics, free energy of binding, interconversion between agonists and antagonists, deorphanization of GPCRs, and the discovery of biased and allosteric modulators. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary software and tools, step-by-step, readily reproducible modelling protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and unique,Computational Methods for GPCR Drug Discovery is a valuable resource for structural and molecular biologists, computational and medicinal chemists, pharmacologists, and drug designers.

G Protein-Coupled Receptor Guidebook

G Protein-Coupled Receptor Guidebook
Title G Protein-Coupled Receptor Guidebook PDF eBook
Author Amy Sojka MS
Publisher Lulu.com
Pages 40
Release 2015-07-20
Genre Science
ISBN 1329400100

Download G Protein-Coupled Receptor Guidebook Book in PDF, Epub and Kindle

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.