Allosteric Modulation Of G Protein Coupled Receptors

Oligomerization And Allosteric Modulation In G Protein Coupled Receptors Book PDF
✏Book Title : Oligomerization and Allosteric Modulation in G Protein Coupled Receptors
✏Author :
✏Publisher : Academic Press
✏Release Date : 2012-12-02
✏Pages : 488
✏ISBN : 9780123947918
✏Available Language : English, Spanish, And French

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✏Oligomerization and Allosteric Modulation in G Protein Coupled Receptors Book Summary : 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

From Structure To Clinical Development Allosteric Modulation Of G Protein Coupled Receptors Book PDF
✏Book Title : From Structure to Clinical Development Allosteric Modulation of G Protein Coupled Receptors
✏Author : Christopher J. Langmead
✏Publisher : Academic Press
✏Release Date : 2020-06
✏Pages : 312
✏ISBN : 9780128201879
✏Available Language : English, Spanish, And French

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✏From Structure to Clinical Development Allosteric Modulation of G Protein Coupled Receptors Book Summary : From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors, Volume 88, the latest release in the Advances in Pharmacology series, presents a variety of chapters from the best authors in the field. Chapters in this updated edition include Targeting muscarinic M1 receptor in neurodegeneration, Photo‐switchable allosteric ligands, Computational approaches for the design of mGlu receptor allosteric modulators, Allosteric modulation of GLP‐1 receptor in metabolic disorders, Group II mGluR roles in the nervous system and their roles in addiction, RAMPs as allosteric modulators of Class B GPCRs, Structure‐based discovery and development of mGlu5 NAMs, and much more.

Allosteric Modulation Of G Protein Coupled Receptors Book PDF
✏Book Title : Allosteric Modulation of G Protein coupled Receptors
✏Author : Joaquin Botta
✏Publisher :
✏Release Date : 2018
✏Pages :
✏ISBN : OCLC:1108701507
✏Available Language : English, Spanish, And French

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✏Allosteric Modulation of G Protein coupled Receptors Book Summary :

Allosteric Receptor Modulation In Drug Targeting Book PDF
✏Book Title : Allosteric Receptor Modulation in Drug Targeting
✏Author : Norman G. Bowery
✏Publisher : CRC Press
✏Release Date : 2016-04-19
✏Pages : 376
✏ISBN : 1420016180
✏Available Language : English, Spanish, And French

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✏Allosteric Receptor Modulation in Drug Targeting Book Summary : Offering a wide array of illustrations and tables in every chapter, this book extensively covers the principles of allosterism in reference to drug action and progresses to a detailed examination of individual ionotropic and G-protein coupled receptor systems-helping those new to the subject understand the importance of allosterism and providing those already working in the field with specific reference information. This title provides in-depth chapters on basic principles of allosterism and its significance at GABAA, 5HT3, nicotinic, and GABAB receptors, ionotropic and metabotropic receptors for glutamate, muscarinic receptors and alpha 2 adrenoceptors to provide a firm foundation to the subject.

Pharmacology Of G Protein Coupled Receptors Book PDF
✏Book Title : Pharmacology of G Protein Coupled Receptors
✏Author :
✏Publisher : Academic Press
✏Release Date : 2011-09-08
✏Pages : 408
✏ISBN : 9780123859532
✏Available Language : English, Spanish, And French

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✏Pharmacology of G Protein Coupled Receptors Book Summary : G protein coupled receptors remain the most important class of therapeutic targets in medicine. In the last 5 years, tremendous advances have been made in our understanding of the structure and mechanism of this critical family of drug targets. The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors. It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones. In addition, emerging drug targets such as receptor families for fatty acids, carboxylic acids, lipid mediators, etc. are included. Final chapters cover novel mechanisms of signal regulation through PDZ domains and RGS proteins. This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists. The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists

Gpcr Molecular Pharmacology And Drug Targeting Book PDF
✏Book Title : GPCR Molecular Pharmacology and Drug Targeting
✏Author : Annette Gilchrist
✏Publisher : John Wiley & Sons
✏Release Date : 2010-12-10
✏Pages : 544
✏ISBN : 1118035178
✏Available Language : English, Spanish, And French

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✏GPCR Molecular Pharmacology and Drug Targeting Book Summary : 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.

Ligand Design For G Protein Coupled Receptors Book PDF
✏Book Title : Ligand Design for G Protein coupled Receptors
✏Author : Didier Rognan
✏Publisher : John Wiley & Sons
✏Release Date : 2006-03-10
✏Pages : 264
✏ISBN : 3527312846
✏Available Language : English, Spanish, And French

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✏Ligand Design for G Protein coupled Receptors Book Summary : 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.

Protein Allostery In Drug Discovery Book PDF
✏Book Title : Protein Allostery in Drug Discovery
✏Author : Jian Zhang
✏Publisher : Springer Nature
✏Release Date : 2019-11-09
✏Pages : 384
✏ISBN : 9789811387197
✏Available Language : English, Spanish, And French

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✏Protein Allostery in Drug Discovery Book Summary : 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 Receptors In Drug Discovery Book PDF
✏Book Title : G Protein Coupled Receptors in Drug Discovery
✏Author : Marta Filizola
✏Publisher : Humana Press
✏Release Date : 2018-02-21
✏Pages : 327
✏ISBN : 1493949675
✏Available Language : English, Spanish, And French

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✏G Protein Coupled Receptors in Drug Discovery Book Summary : This detailed volume provides an overview of recent techniques employed in the field of G protein-coupled receptors (GPCRs) to screen for new drugs and to derive information about their receptor structure, dynamics, and function for the purpose of developing improved therapeutics. Owing to remarkable recent advances in the structural, biophysical and biochemical analyses of these receptors, as well as a growing body of evidence hinting at the possible relevance of allosteric modulators, biased agonists and oligomer-selective ligands as improved therapeutic agents, drug discovery for GPCRs has recently taken a completely new direction. For this book, expert contributors have shared their protocols and views on the impact of these methodologies on modern drug discovery. 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. Practical and fully updated, G Protein-Coupled Receptors in Drug Discovery: Methods and Protocols, Second Edition serves as an ideal guide for a diverse audience from structural and molecular biologists to pharmacologists and drug designers who wish to explore this extensive class of key drug targets.

📒G Protein Coupled Receptors ✍ Sandra Siehler

G Protein Coupled Receptors Book PDF
✏Book Title : G Protein Coupled Receptors
✏Author : Sandra Siehler
✏Publisher : Cambridge University Press
✏Release Date : 2010-09-30
✏Pages :
✏ISBN : 9781139491747
✏Available Language : English, Spanish, And French

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✏G Protein Coupled Receptors Book Summary : Provides a comprehensive overview of recent discoveries and current understandings of G protein-coupled receptors (GPCRs). Recent advances include the first mammalian non-rhodopsin GPCR structures and reconstitution of purified GPCRs into membrane discs for defined studies, novel signaling features including oligomerization, and advances in understanding the complex ligand pharmacology and physiology of GPCRs, in new assay technologies and drug targeting. The authors take time to detail the importance of the pathophysiological function and drug targeting of GPCRs, specifically β-adrenoceptors in cardiovascular and respiratory diseases, metabotropic glutamate receptors in CNS disorders, S1P receptors in the immune system, and Wnt/Frizzled receptors in osteoporosis. This book will be invaluable to researchers and graduate students in academia and industry who are interested in the GPCR field.

Structure And Function Of Gpcrs Book PDF
✏Book Title : Structure and Function of GPCRs
✏Author : Guillaume Lebon
✏Publisher : Springer
✏Release Date : 2019-08-01
✏Pages : 289
✏ISBN : 9783030245917
✏Available Language : English, Spanish, And French

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✏Structure and Function of GPCRs Book Summary : This book introduces readers to the latest advances in G protein-coupled receptor (GPCR) biology. It reviews our current understanding of the structural basis of ligand binding and allosteric mechanisms, following a decade of technological breakthroughs. Several examples of structure-based drug discovery are presented, together with the future challenges involved in designing better drugs that target GPCRs. In turn, the book illustrates the important concept of GPCR biased signaling in physiological contexts, and presents fluorescent- and light-based methodologies frequently used to measure GPCR signaling or to trace their dynamics in cells upon ligand activation. Taken together, the chapters provide an essential overview and toolkit for new scientific investigators who plan to develop GPCR projects. All chapters were written by experts in their respective fields, and share valuable insights and powerful methodologies for the GPCR field.

Universality Of The Sodium Ion Binding Mechanism In Class A G Protein Coupled Receptors Book PDF
✏Book Title : Universality of the Sodium Ion Binding Mechanism in Class A G Protein Coupled Receptors
✏Author :
✏Publisher :
✏Release Date : 2018
✏Pages :
✏ISBN : OCLC:1051343236
✏Available Language : English, Spanish, And French

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✏Universality of the Sodium Ion Binding Mechanism in Class A G Protein Coupled Receptors Book Summary : Abstract: The allosteric modulation of G‐protein‐coupled receptors (GPCRs) by sodium ions has received significant attention as crystal structures of several receptors show Na + ions bound to the inactive conformations at the conserved Asp 2.50 . To date, structures from 24 families of GPCRs have been determined, though mechanistic insights into Na + binding to the allosteric site are limited. We performed hundreds‐of‐microsecond long simulations of 18 GPCRs and elucidated their Na + binding mechanism. In class A GPCRs, the Na + ion binds to the conserved residue 2.50 whereas in class B receptors, it binds at 3.43b, 6.53b, and 7.49b. Using Markov state models, we obtained the free energy profiles and kinetics of Na + binding to the allosteric site, which reveal a conserved mechanism of Na + binding for GPCRs and show the residues that act as major barriers for ion diffusion. Furthermore, we also show that the Na + ion can bind to GPCRs from the intracellular side when the allosteric site is inaccessible from the extracellular side. Abstract : The free energy barriers for Na + ion binding to the allosteric site of 18 G‐protein‐coupled receptors were calculated using Markov state models. Receptors from different classes and families follow a conserved Na + ion binding mechanism but they exhibit large differences in the kinetics of the ion binding process. For PAR1 and P2 Y12, ion binding occurs from the intracellular side.

Multifaceted Roles Of Crystallography In Modern Drug Discovery Book PDF
✏Book Title : Multifaceted Roles of Crystallography in Modern Drug Discovery
✏Author : Giovanna Scapin
✏Publisher : Springer
✏Release Date : 2015-02-27
✏Pages : 240
✏ISBN : 9789401797191
✏Available Language : English, Spanish, And French

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✏Multifaceted Roles of Crystallography in Modern Drug Discovery Book Summary : The present work offers a snapshot of the state-of-the-art of crystallographic, analytical, and computational methods used in modern drug design and development. Topics discussed include: drug design against complex systems (membrane proteins, cell surface receptors, epigenetic targets, and ribosomes); modulation of protein-protein interactions; the impact of small molecule structures in drug discovery and the application of concepts such as molecular geometry, conformation, and flexibility to drug design; methodologies for understanding and characterizing protein states and protein-ligand interactions during the drug design process; and monoclonal antibody therapies. These methods are illustrated through their application to problems of medical and biological significance, such as viral and bacterial infections, diabetes, autoimmune disease, and CNS diseases. As approaches to drug discovery have changed over time, so have the methodologies used to solve the varied, new, and difficult problems encountered in drug discovery. In recent years we have seen great progress in the fields of genetics, biology, chemistry, and medicine, but there are still many unmet medical needs, from bacterial infections to cancer to chronic maladies, that require novel, different, or better therapies. This work will be of interest to researchers and policy makers interested in the latest developments in drug design.

G Protein Coupled Receptors In Health And Disease Book PDF
✏Book Title : G Protein Coupled Receptors in Health and Disease
✏Author :
✏Publisher : Academic Press
✏Release Date : 2009-09-19
✏Pages : 192
✏ISBN : 0080911943
✏Available Language : English, Spanish, And French

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✏G Protein Coupled Receptors in Health and Disease Book Summary : G protein-coupled receptors (GPCRs) transduce signals from a diverse array of endogenous ligands, including ions, amino acids, nucleotides, lipids, peptides, and large glycoprotein hormones. They are also responsible for our sensing of exogenous stimuli, including photons and odorants. GPCRs regulate almost every aspect of our physiological functions. It is estimated that 40% to 50% of currently used therapeutic drugs target GPCRs directly or indirectly. Because the current drugs target only a small portion of the GPCRs, opportunities for targeting the remaining GPCRs is enormous. This volume reviews the latest developments in this rapidly advancing field. * This series provides a forum for discussion of new discoveries, approaches, and ideas * Contributions from leading scholars and industry experts * Reference guide for researchers involved in molecular biology and related fields

Receptor Receptor Interactions Book PDF
✏Book Title : Receptor Receptor Interactions
✏Author : P. Michael Conn
✏Publisher : Academic Press
✏Release Date : 2013-10-18
✏Pages : 538
✏ISBN : 9780124104709
✏Available Language : English, Spanish, And French

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✏Receptor Receptor Interactions Book Summary : This new volume of Methods in Cell Biology looks at receptor-receptor interactions, with sections on allosteric and effector interactions, crystallization and modeling, measuring receptor-receptor interactions and oligomerization in individual classes. With cutting-edge material, this comprehensive collection is intended to guide researchers of receptor-receptor interactions for years to come. Covers sections on allosteric and effector interactions, crystallization and modeling, measuring receptor-receptor interactions and oligomerization in individual classes Chapters are written by experts in the field Cutting-edge material

📒Gpcrs ✍ Beata Jastrzebska

Gpcrs Book PDF
✏Book Title : GPCRs
✏Author : Beata Jastrzebska
✏Publisher : Academic Press
✏Release Date : 2019-09-11
✏Pages : 500
✏ISBN : 9780128167281
✏Available Language : English, Spanish, And French

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✏GPCRs Book Summary : 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

📒Gpcrs ✍ Beata Jastrzebska

Gpcrs Book PDF
✏Book Title : GPCRs
✏Author : Beata Jastrzebska
✏Publisher : Academic Press
✏Release Date : 2019-10
✏Pages : 552
✏ISBN : 0128162287
✏Available Language : English, Spanish, And French

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✏GPCRs Book Summary : 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

G Protein Coupled Receptors Book PDF
✏Book Title : G Protein Coupled Receptors
✏Author : David Poyner
✏Publisher : John Wiley & Sons
✏Release Date : 2009-12-11
✏Pages : 310
✏ISBN : 9780470749227
✏Available Language : English, Spanish, And French

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✏G Protein Coupled Receptors Book Summary : G-Protein Coupled Receptors (GPCRs) are not only the largest protein family in the human genome but are also the single biggest target for therapeutic agents. Research into GPCRs is therefore growing at a fast pace and the range of techniques that can be applied to GPCRs is vast and continues to grow. This book provides an invaluable bench-side guide into the best and most up-to-date techniques for current and future research on GPCRs. With contributions from leading international authorities, this book equips readers with clear and detailed protocols for both well-known and up-and-coming techniques along with hints and tips for success. All the methods have been tried and tested by leading international research labs and are presented in easy-to-follow stages along with a useful overview of each technique. This book is an essential resource for all researchers in molecular biology, biochemistry, pharmacology and for graduate students.

📒G Protein Coupled Receptors ✍ Georges Vauquelin

G Protein Coupled Receptors Book PDF
✏Book Title : G Protein coupled Receptors
✏Author : Georges Vauquelin
✏Publisher : John Wiley & Sons
✏Release Date : 2008-03-11
✏Pages : 264
✏ISBN : 047051664X
✏Available Language : English, Spanish, And French

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✏G Protein coupled Receptors Book Summary : G protein-coupled receptors (GPCRs) are membrane proteins that transduce a vast array of extracellular signals into intracellular reactions ranging from cell-cell communication processes to physiological responses. They play an important role in a variety of diseases from cancer and diabetes, to neurodegenerative, inflammatory and respiratory disorders. GPCRs are therefore of utmost interest in drug development: over half of all prescription drugs currently on the market act by targeting these receptors directly or indirectly. G Protein-coupled Receptors: Molecular Pharmacology provides a clear summary of the current knowledge in this fast-evolving field. The book sets out with an introduction to signalling molecules and their receptors, and an overview of the technical approaches used to investigate these interactions. Structural, functional and especially pharmacological aspects of GPCRs are then discussed in more detail and much attention is devoted to the analysis and interpretation of experimental data. The now widespread use of recombinant cell lies, receptor mutants and related artifices in drug research is critically evaluated. Special attention is also devoted to topical but often poorly understood concepts, such as insurmountable antagonism, inverse agonism and allosteric interactions. By combining general information with the major state-of-the-art concepts in GPCR-research, this outstanding book equips the reader with the necessary background for understanding and critically evaluating the current literature. Written by two experts from academia and industry, G Protein-coupled Receptors: Molecular Pharmacology offers a unique view of academic and applied approaches aiming to reveal new ideas in pharmaceutical research. The book is of interest to anyone involved in drug development and preclinical research and those who need to function within multi-disciplinary teams in the pharmaceutical industry: from investigators to product managers or clinicians who seek to have a broad mechanistic understanding of drug-receptor interactions. It is also an invaluable resource for final year undergraduate and postgraduate students in pharmacology and cell and molecular biology.

📒Endocrinology E Book ✍ J. Larry Jameson

Endocrinology E Book Book PDF
✏Book Title : Endocrinology E Book
✏Author : J. Larry Jameson
✏Publisher : Elsevier Health Sciences
✏Release Date : 2010-05-18
✏Pages : 3064
✏ISBN : 9781455711260
✏Available Language : English, Spanish, And French

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✏Endocrinology E Book Book Summary : ENDOCRINOLOGY, edited by J. Larry Jameson, MD, PhD and Leslie J. De Groot, MD, has been considered the definitive source in its field for decades. Now this landmark reference has been exhaustively updated to bring you the latest clinical guidance on all aspects of diagnosis and treatment for the full range of endocrine and metabolism disorders, including new information on diabetes, obesity, MEN I and II, disorders of sex determination, and pituitary tumors. Entirely new chapters on Lipodystrophy Syndromes, Lipoprotein Metabolism, and Genetic Disorders of Phosphate Homeostasis keep you well informed on today’s hot topics. You’ll benefit from unique, global perspectives on adult and pediatric endocrinology prepared by an international team of renowned authorities. This reference is optimally designed to help you succeed in your demanding practice and ensure the best possible outcomes for every patient. Overcome virtually any clinical challenge with detailed, expert coverage of every area of endocrinology, authored by hundreds of leading luminaries in the field. Provide state-of-the-art care with comprehensive updates on diabetes, obesity, MEN I and II, disorders of sex determination, and pituitary tumors ... brand-new chapters on Lipodystrophy Syndromes, Lipoprotein Metabolism, and Genetic Disorders of Phosphate Homeostasis ... expanded coverage of sports performance, including testosterone, androgen research, and bone growth and deterioration ... and the newest discoveries in genetics and how they affect patient care. Make the best clinical decisions with an enhanced emphasis on evidence-based practice in conjunction with expert opinion. Rapidly consult with trusted authorities thanks to new expert-opinion treatment strategies and recommendations. Zero in on the most relevant and useful references with the aid of a more focused, concise bibliography. Locate information more quickly, while still getting the complete coverage you expect.

📒Drug Discovery Strategies And Methods ✍ Alexandros Makriyannis

Drug Discovery Strategies And Methods Book PDF
✏Book Title : Drug Discovery Strategies and Methods
✏Author : Alexandros Makriyannis
✏Publisher : CRC Press
✏Release Date : 2003-11-04
✏Pages : 348
✏ISBN : 9780824757670
✏Available Language : English, Spanish, And French

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✏Drug Discovery Strategies and Methods Book Summary : Navigate the complex and multidisciplinary path of drug discovery procedures with Drug Discovery Strategies and Methods-a well-organized and timely reference that analyzes methods in target identification and validation, lead detection, compound optimization, and biological testing. This volume addresses challenges encountered during the discovery of new pharmaceutical candidates including the use of cutting-edge techniques utilized in drug design and development. It considers key elements in the drug design cycle ranging from appropriateness of targets and disease models to compound characterization, safety, and efficacy and the role of protein crystallography in structure-based drug design.

Olgomerization In Health And Disease Book PDF
✏Book Title : Olgomerization in Health and Disease
✏Author : Francisco Ciruela
✏Publisher : Academic Press
✏Release Date : 2020-01-15
✏Pages : 300
✏ISBN : 9780128179291
✏Available Language : English, Spanish, And French

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✏Olgomerization in Health and Disease Book Summary : Oligomerization in Health and Disease: From Enzymes to G Protein-Coupled Receptors, Volume 169 in the Progress in Molecular Biology and Translational Science series, provides in-depth reviews on topics of exceptional scientific importance. Topics of note in this new release include Computational prediction and re-design of aberrant oligomerization, Oligomerization of G protein-coupled receptors: an historical overview, Prediction and targeting of GPCR oligomer interfaces, GPCR Oligomerization dynamics: Functional consequences, GPCR heteromerization in neuropsychiatric disorders, Structural basis of regulation and oligomerization of human cystathionine ß-synthase, and Oligomerization of Porphobilinogen Synthase. Includes comprehensive coverage of molecular biology Presents ample use of tables, diagrams, schemata and color figures to enhance the reader's ability to rapidly grasp the information provided Contains contributions from renowned experts in the field of molecular biology

Medical Pharmacology And Therapeutics E Book Book PDF
✏Book Title : Medical Pharmacology and Therapeutics E Book
✏Author : Derek G. Waller
✏Publisher : Elsevier Health Sciences
✏Release Date : 2013-08-07
✏Pages : 744
✏ISBN : 9780702055034
✏Available Language : English, Spanish, And French

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✏Medical Pharmacology and Therapeutics E Book Book Summary : This book covers all the pharmacology you need, from basic science pharmacology and pathophysiology, through to clinical pharmacology to therapeutics, in line with the integrated approach of new medical curricula. The first section covers the basic principles, and the rest is organised by body systems. The book ends with sections on toxicity and prescribing practice. Integrates basic science pharmacology, clinical pharmacology and therapeutics Brief review of pathophysiology of major diseases Case histories and multiple choice questions (and answers) Tabular presentation of all common drugs within each class Section on further reading Kinetics chapter simplified with more practical examples Includes more on genetic issues Drug tables made more concise to make information more accessible Fully updated to reflect current clinical practice

G Protein Pathways Part A Receptors Book PDF
✏Book Title : G Protein Pathways Part A Receptors
✏Author : Ravi Iyengar
✏Publisher : Gulf Professional Publishing
✏Release Date : 2002
✏Pages : 680
✏ISBN : 0121822443
✏Available Language : English, Spanish, And French

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✏G Protein Pathways Part A Receptors Book Summary : G Protein Pathways is the first of three volumes examining the nature of heterotrimeric G proteins. The text takes an integrated approach to studying common experimental questions at many different levels related to G proteins. Methods related to G proteins using molecular modeling, systems biology, protein engineering, protein biochemistry, cell biology, and physiology are all accessible in the same volume. The critically acclaimed laboratory standard for more than forty years, Methods in Enzymology is one of the most highly respected publications in the field of biochemistry. Since 1955, each volume has been eagerly awaited, frequently consulted, and praised by researchers and reviewers alike. Now with more than 300 volumes (all of them still in print), the series contains much material still relevant today—truly an essential publication for researchers in all fields of life sciences.

📒Affinity And Efficacy ✍ Frederick J Ehlert

Affinity And Efficacy Book PDF
✏Book Title : Affinity and Efficacy
✏Author : Frederick J Ehlert
✏Publisher : World Scientific
✏Release Date : 2014-11-13
✏Pages : 752
✏ISBN : 9789814632164
✏Available Language : English, Spanish, And French

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✏Affinity and Efficacy Book Summary : 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. Contents:Ligand-Gated Ion Channels:Ligand-Gated Ion ChannelsAffinity and Efficacy of Orthosteric Ligands at Ligand-Gated Ion ChannelsCompetitive Interactions Between Orthostheric Ligands at Ligand-Gated Ion ChannelsAnalysis of Allosteric Interactions at Ligand-Gated Ion ChannelsG Protein-Coupled Receptors:G Protein-Coupled Receptors and G Protein and Arrestin SignalingAffinity and Efficacy of the Agonist-Receptor-G-Protein InteractionEstimating Affinity and Efficacy by Reverse-Engineering the Response-Clamp AnalysisAnalysis of Agonism and Inverse Agonism in Signaling Pathways that Exhibit Constitutive ActivityAnalysis of Ligand Bias in Receptor Signaling through Different G Protein PathwaysCompetitive Interactions Between Orthosteric Ligands in Functional Assays on G Protein-Coupled ReceptorsAnalysis of Allosterism in Functional Assays on G Protein-coupled ReceptorsRadioligand Binding:Analysis of Drug-receptor Interactions Using Radioligand Binding Assays on G Protein-coupled Receptors Readership: Postgraduates and researchers in pharmacology and physiology, professionals in the pharmaceutical industry, neuroscience researchers. Key Features:The concepts of receptor theory and hierarchical levels of pharmacological analysis are integrated and emphasised throughout the bookStep-by-step instructions are given for the different types of pharmacological analysesKeywords:Affinity;Efficacy;Drug-Receptor Interactions;Agonism;Antagonism;Allosterism;Binding;Ligand Directed Signaling;Pathway Selectivity;Inverse Agonism;G Protein-Coupled Receptors;Ligand-Gated Ion Channels;Cell Signaling

Pharmacology Of Purine And Pyrimidine Receptors Book PDF
✏Book Title : Pharmacology of Purine and Pyrimidine Receptors
✏Author :
✏Publisher : Academic Press
✏Release Date : 2011-07-13
✏Pages : 558
✏ISBN : 9780123855336
✏Available Language : English, Spanish, And French

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✏Pharmacology of Purine and Pyrimidine Receptors Book Summary : This is an overview of the fast-moving field of purinergic signalling through adenosine and ATP receptors. Authors are the leading authorities in their fields Subject matter is important for understanding tissue protection Subject matter is of intense interest for new drug development

Frontiers In Cns Drug Discovery Book PDF
✏Book Title : Frontiers in CNS Drug Discovery
✏Author : Atta-ur Rahman
✏Publisher : Bentham Science Publishers
✏Release Date : 2011-08-12
✏Pages : 653
✏ISBN : 9781608051595
✏Available Language : English, Spanish, And French

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✏Frontiers in CNS Drug Discovery Book Summary : "Frontiers in CNS Drug Discovery" is an Ebook series devoted to publishing the latest and the most important advances in Central Nervous System (CNS) drug design and discovery. Eminent scientists write contributions on all areas of rational drug design an

Neuropeptide Gpcrs In Neuroendocrinology Book PDF
✏Book Title : Neuropeptide GPCRs in neuroendocrinology
✏Author : Jae Young Seong
✏Publisher : Frontiers E-books
✏Release Date : 2014-11-07
✏Pages :
✏ISBN : 9782889192670
✏Available Language : English, Spanish, And French

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✏Neuropeptide GPCRs in neuroendocrinology Book Summary : The human genome encompasses ˜ 860 G protein-coupled receptors (GPCRs) including 374 non-chemosensory GPCRs. Half of these latter GPCRs recognize (neuro)peptides as natural ligands. GPCRs thus play a pivotal role in neuroendocrine communication. In particular, GPCRs are involved in the neuroendocrine control of feeding behavior, reproduction, growth, hydromineral homeostasis and stress response. GPCRs are also major drug targets and hence possess a strong potential for the development of innovative pharmaceuticals. The aim of this Research Topic was to assemble a series of review articles and original research papers on neuropeptide GPCRs and their ligands that would illustrate the different facets of the studies currently conducted in this domain.

Antiarrhythmic Agents Advances In Research And Application 2011 Edition Book PDF
✏Book Title : Antiarrhythmic Agents Advances in Research and Application 2011 Edition
✏Author :
✏Publisher : ScholarlyEditions
✏Release Date : 2012-01-09
✏Pages : 69
✏ISBN : 9781464933752
✏Available Language : English, Spanish, And French

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✏Antiarrhythmic Agents Advances in Research and Application 2011 Edition Book Summary : Antiarrhythmic Agents: Advances in Research and Application: 2011 Edition is a ScholarlyBrief™ that delivers timely, authoritative, comprehensive, and specialized information about Antiarrhythmic Agents in a concise format. The editors have built Antiarrhythmic Agents: Advances in Research and Application: 2011 Edition on the vast information databases of ScholarlyNews.™ You can expect the information about Antiarrhythmic Agents in this eBook to be deeper than what you can access anywhere else, as well as consistently reliable, authoritative, informed, and relevant. The content of Antiarrhythmic Agents: Advances in Research and Application: 2011 Edition has been produced by the world’s leading scientists, engineers, analysts, research institutions, and companies. All of the content is from peer-reviewed sources, and all of it is written, assembled, and edited by the editors at ScholarlyEditions™ and available exclusively from us. You now have a source you can cite with authority, confidence, and credibility. More information is available at http://www.ScholarlyEditions.com/.

Williams Textbook Of Endocrinology E Book Book PDF
✏Book Title : Williams Textbook of Endocrinology E Book
✏Author : Shlomo Melmed
✏Publisher : Elsevier Health Sciences
✏Release Date : 2011-05-12
✏Pages : 1904
✏ISBN : 9781437736007
✏Available Language : English, Spanish, And French

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✏Williams Textbook of Endocrinology E Book Book Summary : The latest edition of Williams Textbook of Endocrinology edited by Drs. Shlomo Melmed, Kenneth S. Polonsky, P. Reed Larsen, and Henry M. Kronenberg, helps you diagnose and treat your patients effectively with up-to-the minute, practical know-how on all endocrine system disorders. Comprehensive yet accessible, this extensively revised 12th Edition updates you on diabetes, metabolic syndrome, obesity, thyroid disease, testicular disorders, and much more so you can provide your patients with the most successful treatments. Find scientific insight and clinical data interwoven in every chapter, reflecting advances in both areas of this constantly changing discipline, and presented in a truly accessible format. You’ll also access valuable contributions from a dynamic list of expert authors and nearly 2.000 full-color images to help you with every diagnosis. This title has everything you need to manage any and all the clinical endocrinopathies you may encounter. Rely on the one reference that integrates rapidly evolving basic and clinical science in a cohesive, user-friendly format, definitively addresses every topic in the field, and has remained a standard for more than half a century. Update your know-how and skills to diagnose and treat your patients most effectively with exhaustively revised content on diabetes, metabolic disease, thyroid cancer, fertility problems, testicular problems, weight issues, and much more. Apply reliable guidance on endocrine conditions of growing interest like hypothyroidism and testicular disorders, with dedicated new chapters that expound on the latest research findings. Overcome any clinical challenge with comprehensive and easy-to-use coverage of everything from hormone activity, diagnostic techniques, imaging modalities, and molecular genetics, to total care of the patient. Apply the latest practices with guidance from expert authors who contribute fresh perspectives on every topic.