From Structure To Clinical Development Allosteric Modulation Of G Protein Coupled Receptors

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From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors

Author :
Publisher : Academic Press
ISBN 13 : 0128201886
Total Pages : 328 pages
Book Rating : 4.1/5 (282 download)

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Book Synopsis From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors by :

Download or read book From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors written by and published by Academic Press. This book was released on 2020-05-13 with total page 328 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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. Includes the authority and expertise of leading contributors in pharmacology Presents the latest release in the Advances in Pharmacology series

Allosteric Modulation of G Protein-Coupled Receptors

Author : Robert Laprairie
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

Author : Kjell Fuxe
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:

Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors

Author :
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

Protein Allostery in Drug Discovery

Author : Jian Zhang
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.

Structural Biology in Drug Discovery

Author : Jean-Paul Renaud
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

Quantum Mechanics in Drug Discovery

Author : Alexander Heifetz
Publisher : Humana
ISBN 13 : 9781071602843
Total Pages : 360 pages
Book Rating : 4.6/5 (28 download)

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Book Synopsis Quantum Mechanics in Drug Discovery by : Alexander Heifetz

Download or read book Quantum Mechanics in Drug Discovery written by Alexander Heifetz and published by Humana. This book was released on 2021-02-18 with total page 360 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume looks at applications of quantum mechanical (QM) methods in drug discovery. The chapters in this book describe how QM approaches can be applied to address key drug discovery issues, such as characterizing protein-water-ligand and protein-protein interactions, providing estimates of binding affinities, determining ligand energies and bioactive conformations, refinement of molecular geometries, scoring docked protein–ligand poses, describing molecular similarity, structure–activity-relationship (SAR) analysis, and ADMET prediction. 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 modeling protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and unique, Quantum Mechanics in Drug Discovery is a valuable resource for structural and molecular biologists, computational and medicinal chemists, pharmacologists, and drug designers.

From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors

Author :
Publisher : Academic Press
ISBN 13 : 0128201878
Total Pages : 328 pages
Book Rating : 4.1/5 (282 download)

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Book Synopsis From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors by :

Download or read book From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors written by and published by Academic Press. This book was released on 2020-05-22 with total page 328 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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. Includes the authority and expertise of leading contributors in pharmacology Presents the latest release in the Advances in Pharmacology series

Allosterism in Drug Discovery

Author : Dario Doller
Publisher : Royal Society of Chemistry
ISBN 13 : 1782624597
Total Pages : 458 pages
Book Rating : 4.7/5 (826 download)

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Book Synopsis Allosterism in Drug Discovery by : Dario Doller

Download or read book Allosterism in Drug Discovery written by Dario Doller and published by Royal Society of Chemistry. This book was released on 2016-11-24 with total page 458 pages. Available in PDF, EPUB and Kindle. Book excerpt: Although the concept of allosterism has been known for over half a century, its application in drug discovery has exploded in recent years. The emergence of novel technologies that enable molecular-level ligand-receptor interactions to be studied in studied in unprecedented detail has driven this trend. This book, written by the leaders in this young research area, describes the latest developments in allosterism for drug discovery. Bringing together research in a diverse range of scientific disciplines, Allosterism in Drug Discovery is a key reference for academics and industrialists interested in understanding allosteric interactions. The book provides an in-depth review of research using small molecules as chemical probes and drug candidates that interact allosterically with proteins of relevance to life sciences and human disease. Knowledge of these interactions can then be applied in the discovery of the novel therapeutics of the future. This book will be useful for people working in all disciplines associated with drug discovery in academia or industry, as well as postgraduate students who may be working in the design of allosteric modulators.

Pharmacology of G Protein Coupled Receptors

Author :
Publisher : Academic Press
ISBN 13 : 0123859530
Total Pages : 408 pages
Book Rating : 4.1/5 (238 download)

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Book Synopsis Pharmacology of G Protein Coupled Receptors by :

Download or read book Pharmacology of G Protein Coupled Receptors written by and published by Academic Press. This book was released on 2011-09-08 with total page 408 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Molecular Pharmacology

Author : Angel Catala
Publisher : BoD – Books on Demand
ISBN 13 : 1839629312
Total Pages : 168 pages
Book Rating : 4.8/5 (396 download)

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Book Synopsis Molecular Pharmacology by : Angel Catala

Download or read book Molecular Pharmacology written by Angel Catala and published by BoD – Books on Demand. This book was released on 2020-12-16 with total page 168 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book concentrates on recent developments related to the application of original structural biology, biochemistry, biophysics, physiology, genetics, and molecular biology as well as basic pharmacological problems that offer mechanistic insights that are generally significant for the field of pharmacology. Written by experts, chapters cover such topics as drug transport mechanisms and drug–receptor complexes. This volume offers up-to-date, expert reviews of the fast-moving field of molecular pharmacology.

The Metabotropic Glutamate Receptors

Author : P. Jeffrey Conn
Publisher : Springer Science & Business Media
ISBN 13 : 1475722982
Total Pages : 284 pages
Book Rating : 4.4/5 (757 download)

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Book Synopsis The Metabotropic Glutamate Receptors by : P. Jeffrey Conn

Download or read book The Metabotropic Glutamate Receptors written by P. Jeffrey Conn and published by Springer Science & Business Media. This book was released on 2013-03-09 with total page 284 pages. Available in PDF, EPUB and Kindle. Book excerpt: The Metabotropic Glutamate Receptors offers state-of-the-art summaries and reviews of virtually everything known today about metabotropic glutamate receptors (mGluRs), including their molecular biology, pharmacology, anatomical distribution, and physiological and pathological roles. Illuminating the overall role played by this crucial class of receptors in brain function, the book also pinpoints those areas in which there is the greatest continuing need for focused research. Because mGluRs have the potential for participating in virtually all known functions of the central nervous system (CNS), the opportunity now exists to develop pharmacological agents that can potentially alter many brain disease processes by selective interaction with precise CNS functions. With its critical and insightful reviews, The Metabotropic Glutamate Receptors will immediately become your essential key to the development of novel treatment strategies for the widest variety of neurological disorders.

Encyclopedia of Signaling Molecules

Author :
Publisher :
ISBN 13 : 9781461464389
Total Pages : pages
Book Rating : 4.4/5 (643 download)

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Book Synopsis Encyclopedia of Signaling Molecules by :

Download or read book Encyclopedia of Signaling Molecules written by and published by . This book was released on 19?? with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:

Inhibitors of Protein–Protein Interactions

Author : Ali Tavassoli
Publisher : Royal Society of Chemistry
ISBN 13 : 178801569X
Total Pages : 357 pages
Book Rating : 4.7/5 (88 download)

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Book Synopsis Inhibitors of Protein–Protein Interactions by : Ali Tavassoli

Download or read book Inhibitors of Protein–Protein Interactions written by Ali Tavassoli and published by Royal Society of Chemistry. This book was released on 2020-12-07 with total page 357 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein-protein interactions (PPI) are at the heart of the majority of cellular processes, and are frequently dysregulated or usurped in disease. Given this central role, the inhibition of PPIs has been of significant interest as a means of treating a wide variety of diseases. However, there are inherent challenges in developing molecules capable of disrupting the relatively featureless and large interfacial areas involved. Despite this, there have been a number of successes in this field in recent years using both traditional drug discovery approaches and innovative, interdisciplinary strategies using novel chemical scaffolds. This book comprehensively covers the various aspects of PPI inhibition, encompassing small molecules, peptidomimetics, cyclic peptides, stapled peptides and macrocycles. Illustrated throughout with successful case studies, this book provides a holistic, cutting-edge view of the subject area and is ideal for chemical biologists and medicinal chemists interested in developing PPI inhibitors.

Computational Methods for GPCR Drug Discovery

Author : Alexander Heifetz
Publisher : Humana Press
ISBN 13 : 9781493984947
Total Pages : 436 pages
Book Rating : 4.9/5 (849 download)

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Book Synopsis Computational Methods for GPCR Drug Discovery by : Alexander Heifetz

Download or read book Computational Methods for GPCR Drug Discovery written by Alexander Heifetz and published by Humana Press. This book was released on 2018-08-30 with total page 436 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Ion Channels

Author : James N. C. Kew
Publisher :
ISBN 13 : 0199296758
Total Pages : 586 pages
Book Rating : 4.1/5 (992 download)

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Book Synopsis Ion Channels by : James N. C. Kew

Download or read book Ion Channels written by James N. C. Kew and published by . This book was released on 2010 with total page 586 pages. Available in PDF, EPUB and Kindle. Book excerpt: Ion channels are intimately involved in the everyday physiological functions that enable us to live a full and varied life. When disease strikes, malfunction of ion channels or their dependent is often involved, either as the cause or the effect of the illness. Thus, billions of dollars have been, and still are being, invested in research to understand the physiological and pathophysiological functions of ion channels in an attempt to develop novel therapeutic treatments for a wide range of diseases. This book provides a comprehensive overview of ion channel structure and function. It comprises two major parts. Part one is an introductory overview of the ion channel superfamily and the generic aspects of ion channel function. This part also reviews the methodologies by which ion channel function can be studied from the perspective of performing detailed biophysical characterization through to the deployment of high throughput approaches for identifying novel ion channel ligands. Part two of the book provides an in-depth review of the individual ion channel subfamilies and, as such, is subdivided into four broad sections: Voltage-Gated Ion Channels, Extracellular Ligand-Gated Ion Channels, Intracellular Ligand-Gated Ion Channels, and Polymodal-Gated Ion Channels, with each chapter focused on specific family members. These chapters have been written by world leading experts and provide a detailed overview of the structure, biophysics, localization, pharmacology, physiology, and disease relevance of each particular ion channel subfamily. Reviewing both the basic principles of ion channel function and providing a detailed up-to-date review of the phsyiological and pharmacological aspects of individual ion channel sub-families, this book constitutes both an excellent introduction to the field for non-specialists, as well as a highly valuable reference text for experienced researchers already working in the ion channel area.

Principles of Endocrinology and Hormone Action

Author : Antonino Belfiore
Publisher : Springer
ISBN 13 : 9783319446745
Total Pages : 0 pages
Book Rating : 4.4/5 (467 download)

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Book Synopsis Principles of Endocrinology and Hormone Action by : Antonino Belfiore

Download or read book Principles of Endocrinology and Hormone Action written by Antonino Belfiore and published by Springer. This book was released on 2018-02-08 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume provides comprehensive coverage of the current knowledge of the physiology of the endocrine system and hormone synthesis and release, transport, and action at the molecular and cellular levels. It presents essential as well as in-depth information of value to both medical students and specialists in Endocrinology, Gynecology, Pediatrics, and Internal Medicine. Although it is well established that the endocrine system regulates essential functions involved in growth, reproduction, and homeostasis, it is increasingly being recognized that this complex regulatory system comprises not only hormones secreted by the classic endocrine glands but also hormones and regulatory factors produced by many organs, and involves extensive crosstalk with the neural and immune system. At the same time, our knowledge of the molecular basis of hormone action has greatly improved. Understanding this complexity of endocrine physiology is crucial to prevent endocrine disorders, to improve the sensitivity of our diagnostic tools, and to provide the rationale for pharmacological, immunological, or genetic interventions. It is such understanding that this book is designed to foster.