On the Nature of Allosteric Interactions at the M2 Muscarinic Receptor

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ISBN 13 :
Total Pages : pages
Book Rating : 4.:/5 (13 download)

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Book Synopsis On the Nature of Allosteric Interactions at the M2 Muscarinic Receptor by : Rabindra Vishwadev Shivnaraine

Download or read book On the Nature of Allosteric Interactions at the M2 Muscarinic Receptor written by Rabindra Vishwadev Shivnaraine and published by . This book was released on 2015 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:

Allosteric Modulation of G Protein-Coupled Receptors

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Publisher : Academic Press
ISBN 13 : 0128197722
Total Pages : 214 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Allosteric Modulation of G Protein-Coupled Receptors by : Robert Laprairie

Download or read book Allosteric Modulation of G Protein-Coupled Receptors written by Robert Laprairie and published by Academic Press. This book was released on 2022-02-05 with total page 214 pages. Available in PDF, EPUB and Kindle. Book excerpt: Allosteric Modulation of G Protein-Coupled Receptors reviews fundamental information on G protein-coupled receptors (GPCRs) and allosteric modulation, presenting original research in the area and collectively providing a comprehensive description of key issues in GPCR allosteric modulation. The book provides background on core concepts of molecular pharmacology while also introducing the most important advances and studies in the area. It also discusses key methodologies. This is an essential book for researchers and advanced students engaged in pharmacology, toxicology and pharmaceutical sciences training and research. Many of the GPCR-targeted drugs released in the past decade have specifically worked via allosteric mechanisms. Unlike direct orthosteric-acting compounds that occupy a similar receptor site to that of endogenous ligands, allosteric modulators alter GPCR-dependent signaling at a site apart from the endogenous ligand. Recent methodological and analytical advances have greatly improved our ability to understand the signaling mechanisms of GPCRs. We now know that allostery is a common regulatory mechanism for all GPCRs and not – as we once believed – unique to a few receptor subfamilies. - Introduces background on core concepts of molecular pharmacology, including statistical analyses, non-linear regression, complex models and GPCR-dependent signal transduction as they relate to allosteric modulation - Discusses critical advances and landmark studies, including discoveries in the area of GPCR allosteric modulation, which are reviewed for their importance in positive and negative regulation, protein-protein interactions, and small molecule drug discovery - Includes key methodologies used to study allosteric modulation at the in silico, in vitro, and in vivo levels of drug discovery and characterization

Receptor-Receptor Interactions

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Publisher : Springer Science & Business Media
ISBN 13 : 1468454153
Total Pages : 577 pages
Book Rating : 4.4/5 (684 download)

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Book Synopsis Receptor-Receptor Interactions by : Kjell Fuxe

Download or read book Receptor-Receptor Interactions written by Kjell Fuxe and published by Springer Science & Business Media. This book was released on 2013-03-13 with total page 577 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Muscarinic Receptor

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ISBN 13 : 9781493928583
Total Pages : 287 pages
Book Rating : 4.9/5 (285 download)

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Book Synopsis Muscarinic Receptor by : Jaromir Myslivecek

Download or read book Muscarinic Receptor written by Jaromir Myslivecek and published by . This book was released on 2016 with total page 287 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Muscarinic Receptor

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Publisher : Springer Nature
ISBN 13 : 1071640151
Total Pages : 361 pages
Book Rating : 4.0/5 (716 download)

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Book Synopsis Muscarinic Receptor by : Jaromir Myslivecek

Download or read book Muscarinic Receptor written by Jaromir Myslivecek and published by Springer Nature. This book was released on with total page 361 pages. Available in PDF, EPUB and Kindle. Book excerpt:

GPCRs

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Publisher : Academic Press
ISBN 13 : 0128167289
Total Pages : 502 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis GPCRs by : Beata Jastrzebska

Download or read book GPCRs written by Beata Jastrzebska and published by Academic Press. This book was released on 2019-09-11 with total page 502 pages. Available in PDF, EPUB and Kindle. Book excerpt: GPCRS: Structure, Function, and Drug Discovery provides a comprehensive overview of recent discoveries and our current understanding of GPCR structure, signaling, physiology, pharmacology and methods of study. In addition to the fundamental aspects of GPCR function and dynamics, international experts discuss crystal structures, GPCR complexes with partner proteins, GPCR allosteric modulation, biased signaling through protein partners, deorphanization of GPCRs, and novel GPCR-targeting ligands that could lead to the development of new therapeutics against human diseases. GPCR association with, and possible therapeutic pathways for, retinal degenerative diseases, Alzheimer's disease, Parkinson's disease, cancer and diabetic nephropathy, among other illnesses, are examined in-depth. - Addresses our current understanding and novel advances in the GPCR field, directing readers towards recent finding of key significance for translational medicine - Combines a thorough discussion of structure and function of GPCRs with disease association and drug discovery - Features chapter contributions from international experts in GPCR structure, signaling, physiology and pharmacology

Muscarinic Receptors

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Publisher : Springer Science & Business Media
ISBN 13 : 3642232744
Total Pages : 501 pages
Book Rating : 4.6/5 (422 download)

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Book Synopsis Muscarinic Receptors by : Allison D. Fryer

Download or read book Muscarinic Receptors written by Allison D. Fryer and published by Springer Science & Business Media. This book was released on 2012-01-06 with total page 501 pages. Available in PDF, EPUB and Kindle. Book excerpt: Muscarinic acetylcholine receptors have played a key role in the advancement of knowledge of pharmacology and neurotransmission since the inception of studies in these fields, and the effects of naturally occurring drugs acting on muscarinic receptors were known and exploited for both therapeutic and non-therapeutic purposes for hundreds of years before the existence of the receptors themselves was recognized. This volume presents a broad yet detailed review of current knowledge of muscarinic receptors that will be valuable both to long-time muscarinic investigators and to those new to the field. It describes the detailed insights that have been obtained on the structure, function, and cell biology of muscarinic receptors. This volume also describes physiological analyses of muscarinic receptors and their roles in regulating the function of the brain and of a variety of peripheral tissues. This volume shows how the study of muscarinic receptors continues to provide new and surprising insights not just to the cholinergic system but to the broad areas of neurobiology, cell biology, pharmacology, and therapeutics.

Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors

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Publisher : Academic Press
ISBN 13 : 012394791X
Total Pages : 495 pages
Book Rating : 4.1/5 (239 download)

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Book Synopsis Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors by :

Download or read book Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors written by and published by Academic Press. This book was released on 2012-12-02 with total page 495 pages. Available in PDF, EPUB and Kindle. Book excerpt: In this thematic volume of Progress in Molecular Biology and Translational Science, researchers reflect on recent developments and research surrounding G protein-coupled receptors. The chapters cover a large breadth of research, including GPCR role in stem cell function and pharmacology. Authors explore in-depth research techniques and applications of GPCR usage, covering theory, laboratory approaches, and unique qualities that make GPCRs a crucial tool in microbiological and cancer research. - Contributions from leading authorities - Informs and updates on all the latest developments in the field

Drug-Acceptor Interactions

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Publisher : CRC Press
ISBN 13 : 1351660578
Total Pages : 847 pages
Book Rating : 4.3/5 (516 download)

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Book Synopsis Drug-Acceptor Interactions by : Niels Bindslev

Download or read book Drug-Acceptor Interactions written by Niels Bindslev and published by CRC Press. This book was released on 2017-02-10 with total page 847 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug-Acceptor Interactions: Modeling theoretical tools to test and evaluate experimental equilibrium effects suggests novel theoretical tools to test and evaluate drug interactions seen with combinatorial drug therapy. The book provides an in-depth, yet controversial, exploration of existing tools for analysis of dose-response studies at equilibrium or steady state. The book is recommended reading for post-graduate students and researchers engaged in the study of systems biology, networks, and the pharmacodynamics of natural or industrial drugs, as well as for medical clinicians interested in drug application and combinatorial drug therapy. Even people without mathematical skills will be able to follow the pros and cons of reaction schemes and their related distribution equations. Chapter 9 is a hands-on guide for software to plot, fit and analyze one’s own data.

Affinity And Efficacy: The Components Of Drug-receptor Interactions

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Publisher : World Scientific
ISBN 13 : 9814632163
Total Pages : 750 pages
Book Rating : 4.8/5 (146 download)

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Book Synopsis Affinity And Efficacy: The Components Of Drug-receptor Interactions by : Frederick J Ehlert

Download or read book Affinity And Efficacy: The Components Of Drug-receptor Interactions written by Frederick J Ehlert and published by World Scientific. This book was released on 2014-11-13 with total page 750 pages. Available in PDF, EPUB and Kindle. Book excerpt: The interaction of a drug with a receptor generates a code of information having components of affinity and efficacy. How this information is translated into a response depends on the unique cells, tissue, organ or system in which the receptor resides. This book describes how to analyze various responses to estimate the affinity and efficacy components of the initial drug-receptor interaction. More specifically, it describes how to measure the affinity and efficacy of drugs through the analysis of single receptor activity, the activation state of a population of receptors, and responses downstream from receptor activation. More light is thrown on ligand-gated ion channels and G protein-coupled receptors in this book.The topics discussed include radioligand binding, estimation of agonist affinity and efficacy, competitive antagonism, inverse agonism, allosteric agonists and modulators, agonist bias, modulation of pathway selectivity, and the estimation of ligand affinity for active and inactive receptor states. The natural history and structure of ligand-gated ion channels, G proteins, and G protein-coupled receptors are also discussed.

Protein Allostery in Drug Discovery

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Publisher : Springer Nature
ISBN 13 : 9811387192
Total Pages : 384 pages
Book Rating : 4.8/5 (113 download)

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Book Synopsis Protein Allostery in Drug Discovery by : Jian Zhang

Download or read book Protein Allostery in Drug Discovery written by Jian Zhang and published by Springer Nature. This book was released on 2019-11-09 with total page 384 pages. Available in PDF, EPUB and Kindle. Book excerpt: The book focuses on protein allostery in drug discovery. Allosteric regulation, ʹthe second secret of lifeʹ, fine-tunes virtually most biological processes and controls physiological activities. Allostery can both cause human diseases and contribute to development of new therapeutics. Allosteric drugs exhibit unparalleled advantages compared to conventional orthosteric drugs, rendering the development of allosteric modulators as an appealing strategy to improve selectivity and pharmacodynamic properties in drug leads. The Series delineates the immense significance of protein allostery—as demonstrated by recent advances in the repertoires of the concept, its mechanistic mechanisms, and networks, characteristics of allosteric proteins, modulators, and sites, development of computational and experimental methods to predict allosteric sites, small-molecule allosteric modulators of protein kinases and G-protein coupled receptors, engineering allostery, and the underlying role of allostery in precise medicine. Comprehensive understanding of protein allostery is expected to guide the rational design of allosteric drugs for the treatment of human diseases. The book would be useful for scientists and students in the field of protein science and Pharmacology etc.

G Protein-Coupled Receptor Signaling

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Publisher : Humana Press
ISBN 13 : 9781493991204
Total Pages : 406 pages
Book Rating : 4.9/5 (912 download)

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Book Synopsis G Protein-Coupled Receptor Signaling by : Mario Tiberi

Download or read book G Protein-Coupled Receptor Signaling written by Mario Tiberi and published by Humana Press. This book was released on 2019-03-01 with total page 406 pages. Available in PDF, EPUB and Kindle. Book excerpt: This detailed volume assembles comprehensive protocols to assist with the study of structural, molecular, cell biological, and in vivo facets of GPCRs, and to enable the development of experimental tools for screening novel GPCR drugs. Sections explore the tweaking of ligands, bioluminescence and FRET approaches, specific GPCR signaling properties, as well as visualization of subcellular compartmentalization. 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 practical, G Protein-Coupled Receptor Signaling: Methods and Protocols serves as an ideal reference for life scientists working in a variety of research fields including molecular pharmacology, cell and developmental biology, brain behavior and physiology, drug development and screening. Chapter 4 is available open access under a CC BY 4.0 license via link.springer.com.

Structural Biology in Drug Discovery

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Publisher : John Wiley & Sons
ISBN 13 : 1118900502
Total Pages : 1367 pages
Book Rating : 4.1/5 (189 download)

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Book Synopsis Structural Biology in Drug Discovery by : Jean-Paul Renaud

Download or read book Structural Biology in Drug Discovery written by Jean-Paul Renaud and published by John Wiley & Sons. This book was released on 2020-01-09 with total page 1367 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins

Magnesium in the Central Nervous System

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Publisher : University of Adelaide Press
ISBN 13 : 0987073052
Total Pages : 354 pages
Book Rating : 4.9/5 (87 download)

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Book Synopsis Magnesium in the Central Nervous System by : Robert Vink

Download or read book Magnesium in the Central Nervous System written by Robert Vink and published by University of Adelaide Press. This book was released on 2011 with total page 354 pages. Available in PDF, EPUB and Kindle. Book excerpt: The brain is the most complex organ in our body. Indeed, it is perhaps the most complex structure we have ever encountered in nature. Both structurally and functionally, there are many peculiarities that differentiate the brain from all other organs. The brain is our connection to the world around us and by governing nervous system and higher function, any disturbance induces severe neurological and psychiatric disorders that can have a devastating effect on quality of life. Our understanding of the physiology and biochemistry of the brain has improved dramatically in the last two decades. In particular, the critical role of cations, including magnesium, has become evident, even if incompletely understood at a mechanistic level. The exact role and regulation of magnesium, in particular, remains elusive, largely because intracellular levels are so difficult to routinely quantify. Nonetheless, the importance of magnesium to normal central nervous system activity is self-evident given the complicated homeostatic mechanisms that maintain the concentration of this cation within strict limits essential for normal physiology and metabolism. There is also considerable accumulating evidence to suggest alterations to some brain functions in both normal and pathological conditions may be linked to alterations in local magnesium concentration. This book, containing chapters written by some of the foremost experts in the field of magnesium research, brings together the latest in experimental and clinical magnesium research as it relates to the central nervous system. It offers a complete and updated view of magnesiums involvement in central nervous system function and in so doing, brings together two main pillars of contemporary neuroscience research, namely providing an explanation for the molecular mechanisms involved in brain function, and emphasizing the connections between the molecular changes and behavior. It is the untiring efforts of those magnesium researchers who have dedicated their lives to unraveling the mysteries of magnesiums role in biological systems that has inspired the collation of this volume of work.

Evolution of Nervous Systems

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Publisher : Academic Press
ISBN 13 : 0128040963
Total Pages : 2064 pages
Book Rating : 4.1/5 (28 download)

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Book Synopsis Evolution of Nervous Systems by : Georg F. Striedter

Download or read book Evolution of Nervous Systems written by Georg F. Striedter and published by Academic Press. This book was released on 2016-11-23 with total page 2064 pages. Available in PDF, EPUB and Kindle. Book excerpt: Evolution of Nervous Systems, Second Edition, Four Volume Set is a unique, major reference which offers the gold standard for those interested both in evolution and nervous systems. All biology only makes sense when seen in the light of evolution, and this is especially true for the nervous system. All animals have nervous systems that mediate their behaviors, many of them species specific, yet these nervous systems all evolved from the simple nervous system of a common ancestor. To understand these nervous systems, we need to know how they vary and how this variation emerged in evolution. In the first edition of this important reference work, over 100 distinguished neuroscientists assembled the current state-of-the-art knowledge on how nervous systems have evolved throughout the animal kingdom. This second edition remains rich in detail and broad in scope, outlining the changes in brain and nervous system organization that occurred from the first invertebrates and vertebrates, to present day fishes, reptiles, birds, mammals, and especially primates, including humans. The book also includes wholly new content, fully updating the chapters in the previous edition and offering brand new content on current developments in the field. Each of the volumes has been carefully restructured to offer expanded coverage of non-mammalian taxa, mammals, primates, and the human nervous system. The basic principles of brain evolution are discussed, as are mechanisms of change. The reader can select from chapters on highly specific topics or those that provide an overview of current thinking and approaches, making this an indispensable work for students and researchers alike. Presents a broad range of topics, ranging from genetic control of development in invertebrates, to human cognition, offering a one-stop resource for the evolution of nervous systems throughout the animal kingdom Incorporates the expertise of over 100 outstanding investigators who provide their conclusions in the context of the latest experimental results Presents areas of disagreement and consensus views that provide a holistic view of the subjects under discussion

The G-Protein Linked Receptor Facts Book

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Publisher : Academic Press
ISBN 13 :
Total Pages : 452 pages
Book Rating : 4.3/5 (91 download)

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Book Synopsis The G-Protein Linked Receptor Facts Book by : Steve P. Watson

Download or read book The G-Protein Linked Receptor Facts Book written by Steve P. Watson and published by Academic Press. This book was released on 1994-02-28 with total page 452 pages. Available in PDF, EPUB and Kindle. Book excerpt: Catalogues major facts about receptors, G-proteins and effector molecules. Each entry has a common format, using a minimum amount of text, and contains information on the sequence, gene structure, distribution, agonists/antagonists and physiochemical properties of these proteins.

Cholinergic Mechanisms

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Publisher : CRC Press
ISBN 13 : 9781841840758
Total Pages : 854 pages
Book Rating : 4.8/5 (47 download)

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Book Synopsis Cholinergic Mechanisms by : Israel Silman

Download or read book Cholinergic Mechanisms written by Israel Silman and published by CRC Press. This book was released on 2004-09-20 with total page 854 pages. Available in PDF, EPUB and Kindle. Book excerpt: Providing a cutting-edge profile of research progress in this important field of study, Cholinergic Mechanisms: Function and Dysfunction contains a compilation of the proceedings of the Eleventh ISCM, held in St. Moritz, May 2002. Bringing together 250 contributors from 30 countries, the book presents a comprehensive picture of the cholinergic field. It provides a survey of current understanding of molecular, pharmacological, toxicological, behavioral, and clinical aspects of the cholinergic system. This volume offers a state-of-the-art account of progress in the field from the molecule in the test tube through the cell and the synapse, to the organism and the patient.