G Protein-Coupled Receptors in Drug Discovery

G Protein-Coupled Receptors in Drug Discovery PDF Author: Wayne R. Leifert
Publisher: Humana Press
ISBN: 9781603273169
Category : Medical
Languages : en
Pages : 0

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Book Description
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 Receptors in Drug Discovery

G Protein-Coupled Receptors in Drug Discovery PDF Author: Wayne R. Leifert
Publisher: Humana Press
ISBN: 9781603273169
Category : Medical
Languages : en
Pages : 0

Get Book Here

Book Description
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 Screening Assays

G Protein-Coupled Receptor Screening Assays PDF Author: Sofia Aires M. Martins
Publisher: Humana
ISBN: 9781071612231
Category : Science
Languages : en
Pages : 327

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Book Description
This fully updated edition targets not only those assays directly involved in the discovery of GPCR-active compounds but also those involved in cell-based experiments designed to study physiological responses. Whether coming from academia or industry, or being an experienced researcher or a newcomer to the field, the reader will find accessible methods and protocols that cover the latest developments on receptor purification, molecular biology, recombinant engineering, and analytical techniques that enable the real time monitoring of the complex GPCR signaling cascade and identification of potential drug targets. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and up-to-date, G Protein-Coupled Receptor Screening Assays: Methods and Protocols, Second Edition aims to provide the tools necessary to contribute to the advancement of GPCR research and discovery and ultimately lead to the availability of innovative and more efficient drugs.

G Protein-Coupled Receptors in Energy Homeostasis and Obesity Pathogenesis

G Protein-Coupled Receptors in Energy Homeostasis and Obesity Pathogenesis PDF Author:
Publisher: Academic Press
ISBN: 0123869528
Category : Science
Languages : en
Pages : 403

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Book Description
Obesity is an epidemic with enormous health, economic and social burdens. Current drugs for obesity treatment are far from ideal in terms of efficacy and side effects. Reviews in this volume of Progress in Molecular Biology and Translational Science summarize current status in studies of a number of G protein-coupled receptors that were shown to be promising targets for obesity treatments. Some of these receptors also cause monogenic obesity in humans. - Subject matter: obesity is an epidemic and G protein-coupled receptors are promising drug targets, with significant potential as new anti-obesity drugs - Chapters are written by leading experts

The Fragment Molecular Orbital Method

The Fragment Molecular Orbital Method PDF Author: Dmitri Fedorov
Publisher: CRC Press
ISBN: 1420078496
Category : Science
Languages : en
Pages : 304

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Book Description
Answering the need to facilitate quantum-chemical calculations of systems with thousands of atoms, Kazuo Kitaura and his coworkers developed the Fragment Molecular Orbital (FMO) method in 1999. Today, the FMO method can be applied to the study of whole proteins and protein-ligand interactions, and is extremely effective in calculating the propertie

Molecular Biology of RGS Proteins

Molecular Biology of RGS Proteins PDF Author:
Publisher: Academic Press
ISBN: 0080911978
Category : Science
Languages : en
Pages : 389

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Book Description
Molecular Biology of RGS Proteins, a volume of Progress in Molecular Biology and Translational Science, will include historical discussion of RGS proteins, the role of RGS proteins in addiction, depression and Parkinson's disease and the biology and functional regulation of RGS9 isoforms. This publication further discusses RGS proteins in cellular signaling, protein control in lymphocyte function, and alternative splicing of RGS transcripts and nuclear RGS proteins, offering the latest in research of RGS proteins.

Cells: Molecules and Mechanisms

Cells: Molecules and Mechanisms PDF Author: Eric Wong
Publisher: Axolotl Academic Publishing
ISBN: 0985226110
Category : Biology
Languages : en
Pages : 283

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Book Description
"Yet another cell and molecular biology book? At the very least, you would think that if I was going to write a textbook, I should write one in an area that really needs one instead of a subject that already has multiple excellent and definitive books. So, why write this book, then? First, it's a course that I have enjoyed teaching for many years, so I am very familiar with what a student really needs to take away from this class within the time constraints of a semester. Second, because it is a course that many students take, there is a greater opportunity to make an impact on more students' pocketbooks than if I were to start off writing a book for a highly specialized upper- level course. And finally, it was fun to research and write, and can be revised easily for inclusion as part of our next textbook, High School Biology."--Open Textbook Library.

G Protein Signaling Mechanisms in the Retina

G Protein Signaling Mechanisms in the Retina PDF Author: Kirill A. Martemyanov
Publisher: Springer
ISBN: 1493912186
Category : Medical
Languages : en
Pages : 197

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Book Description
The main purpose of this volume is to provide a focused analysis of the function of the G protein-coupled signaling pathways that operate in the interconnected network of retinal neurons as they detect and encode the information carried by light. The organization of this volume will generally follow the path of signal flow in the retina. First we will describe recent advances in understanding the phototransduction cascade of rod and cone photoreceptors, which use signaling cascade based on the GPCR rhodopsin to transduce incident light into neural activity. Chapters will be devoted to unique specializations of the two major types of photosensitive cells that comprise the predominant input for our spatial and color vision. Subsequently, the mechanisms of synaptic information encoding by retinal ON bipolar cells will be described, where the GPCR mGluR6 plays a fundamental role. Chapters in this section will examine macromolecular organization of the mGluR6 signaling pathway as well as current understanding of its function. The functional characteristics of this signaling mechanism will be explored in detail. Additionally, this section will cover the role of dopamine receptors in modulating signal transmission between photoreceptors and ON-bipolar cells. Finally, chapters will be focused on the output neurons of the inner retina, ganglion cells, where the components of the emerging GPCR melanopsin cascade in intrinsically photosensitive ganglion cells will be detailed. Collectively these mechanisms allow the retina to represent visual space over a wide range of light intensities.

Cannabinoids and the Brain

Cannabinoids and the Brain PDF Author: Attila Köfalvi
Publisher: Springer Science & Business Media
ISBN: 0387743499
Category : Medical
Languages : en
Pages : 587

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Book Description
Endocannabinoids have tremendous therapeutic potential. This book introduces readers to our current understanding of the neurobiology of endocannabinoids and related systems, detailing their pathophysiological role and therapeutic potential. Authors, experienced clinical investigators, present and analyze results of recent clinical trials as well as the development of new therapeutic strategies and medicines.

G-Protein-Coupled Receptor Dimers

G-Protein-Coupled Receptor Dimers PDF Author: Katharine Herrick-Davis
Publisher: Humana
ISBN: 9783319867953
Category : Medical
Languages : en
Pages : 0

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Book Description
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.

G Protein Signaling Pathways in Health and Disease

G Protein Signaling Pathways in Health and Disease PDF Author:
Publisher: Academic Press
ISBN: 0128167246
Category : Science
Languages : en
Pages : 230

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Book Description
G Protein Signaling Pathways in Health and Disease, Volume 161 in the Progress in Molecular Biology and Translational Science series, provides informative and exciting monographs on a wide variety of research topics related to G Protein Signaling Pathways in Health and Disease. The series gives in-depth knowledge on the important molecular biological aspects of organismal physiology and function, along with insights on how this knowledge can be applied to understand and ameliorate human disease. This updated release covers Diseases associated with mutations in CNGA3, Mutations in arrestins, Diseases caused by mutations in GPR101, Diseases caused by mutations in lutropin receptor, and much more.