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

Author : Anonim
Publisher : Academic Press
Page : 328 pages
File Size : 52,7 Mb
Release : 2020-05-13
Category : Medical
ISBN : 9780128201886

Get Book

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

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

Author : Robert Laprairie
Publisher : Academic Press
Page : 214 pages
File Size : 52,6 Mb
Release : 2022-02-05
Category : Business & Economics
ISBN : 9780128197721

Get Book

Allosteric Modulation of G Protein-Coupled Receptors by Robert Laprairie Pdf

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

Author : Anonim
Publisher : Academic Press
Page : 495 pages
File Size : 49,8 Mb
Release : 2012-12-02
Category : Science
ISBN : 9780123947918

Get Book

Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors by Anonim Pdf

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

Author : P. Jeffrey Conn,Jitendra Patel
Publisher : Springer Science & Business Media
Page : 284 pages
File Size : 45,6 Mb
Release : 2013-03-09
Category : Medical
ISBN : 9781475722987

Get Book

The Metabotropic Glutamate Receptors by P. Jeffrey Conn,Jitendra Patel Pdf

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.

Author : Kjell Fuxe,Luigi F. Agnati
Publisher : Springer Science & Business Media
Page : 577 pages
File Size : 47,9 Mb
Release : 2013-03-13
Category : Computers
ISBN : 9781468454154

Get Book

Receptor-Receptor Interactions by Kjell Fuxe,Luigi F. Agnati Pdf

Author : Anonim
Publisher : Academic Press
Page : 328 pages
File Size : 52,5 Mb
Release : 2020-05-22
Category : Medical
ISBN : 9780128201879

Get Book

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

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

Author : Jian Zhang,Ruth Nussinov
Publisher : Springer Nature
Page : 384 pages
File Size : 40,7 Mb
Release : 2019-11-09
Category : Medical
ISBN : 9789811387197

Get Book

Protein Allostery in Drug Discovery by Jian Zhang,Ruth Nussinov Pdf

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.

Author : Jean-Paul Renaud
Publisher : John Wiley & Sons
Page : 1367 pages
File Size : 43,5 Mb
Release : 2020-01-09
Category : Medical
ISBN : 9781118900505

Get Book

Structural Biology in Drug Discovery by Jean-Paul Renaud Pdf

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

Author : Anonim
Publisher : Academic Press
Page : 408 pages
File Size : 48,6 Mb
Release : 2011-09-08
Category : Medical
ISBN : 9780123859532

Get Book

Pharmacology of G Protein Coupled Receptors by Anonim Pdf

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

Author : Lakshmi A. Devi
Publisher : Springer Science & Business Media
Page : 412 pages
File Size : 44,6 Mb
Release : 2008-03-01
Category : Medical
ISBN : 9781592599196

Get Book

The G Protein-Coupled Receptors Handbook by Lakshmi A. Devi Pdf

A comprehensive survey of the many recent advances in the field of G protein-coupled receptors (GPCR). The authors describe the current knowledge of GPCR receptor structure and function, the different mechanisms involved in the regulation of GPCR function, and the role of pharmacological chaperones in GPCR folding and maturation. They also present new findings about how GPCR dimerization/oligomerization modifies the properties of individual receptors and show how recent developments are leading to significant advances in drug discovery, such as the detection of ligands for orphan GPCRs. Also discussed are the most recent developments that could lead to new drug discoveries: the role of GPCRs in mediating pain, the development of receptor-type selective drugs based on the structural plasticity of receptor activation, and the identification of natural ligands of orphan GPCRs (deorphanization) as possible drug targets.

Author : Stefan Offermanns,W. Rosenthal
Publisher : Springer Science & Business Media
Page : 1515 pages
File Size : 45,6 Mb
Release : 2008-08-14
Category : Medical
ISBN : 9783540389163

Get Book

Encyclopedia of Molecular Pharmacology by Stefan Offermanns,W. Rosenthal Pdf

An essential text, this is a fully updated second edition of a classic, now in two volumes. It provides rapid access to information on molecular pharmacology for research scientists, clinicians and advanced students. With the A-Z format of over 2,000 entries, around 350 authors provide a complete reference to the area of molecular pharmacology. The book combines the knowledge of classic pharmacology with the more recent approach of the precise analysis of the molecular mechanisms by which drugs exert their effects. Short keyword entries define common acronyms, terms and phrases. In addition, detailed essays provide in-depth information on drugs, cellular processes, molecular targets, techniques, molecular mechanisms, and general principles.

Author : Angel Catala,Usama Ahmad
Publisher : BoD – Books on Demand
Page : 168 pages
File Size : 51,7 Mb
Release : 2020-12-16
Category : Medical
ISBN : 9781839629310

Get Book

Molecular Pharmacology by Angel Catala,Usama Ahmad Pdf

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.

Author : Paul Leff
Publisher : CRC Press
Page : 816 pages
File Size : 40,5 Mb
Release : 1998-04-10
Category : Medical
ISBN : 1420001132

Get Book

Receptor - Based Drug Design by Paul Leff Pdf

Employing a wide range of examples from G-protein-coupled receptors and ligand-gated ion channels, this detailed, single-source reference illustrates the principles of pharmacological analysis and receptor classification that are the basis of rational drug design. Explains the experimental and theoretical methods used to characterize interactions between ligands and receptors-providing the pharmacological information needed to solve treatment problems and facilitate the drug design process! Demonstrating the achievements of the receptor-based approach in therapeutics and indicating future directions, Receptor-Based Drug Design introduces novel computer-assisted strategies for the design of new agonists, antagonists, and inverse agonists for G-protein-coupled receptors shows how to assess agonist concentration-effect curve data discusses radioligand binding assays presents new in vitro multiarray assays for G-protein-coupled receptors explains the use of individual second messenger signaling responses in analyzing drug-receptor interactions examines the role of electrophysiology in finding new drugs and drug targets describes selectively acting b-adrenoceptor agonists and glucocorticoid steroids for asthma treatment outlines the rationale for using angiotensin receptor antagonists and more! Written by over 25 international authorities and containing nearly 1200 bibliographic citations, Receptor-Based Drug Design is a practical resource for pharmacologists, pharmacists, and pharmaceutical scientists; organic and medicinal chemists and biochemists; molecular biologists; biomedical researchers; and upper-level undergraduate and graduate students in these disciplines.

Author : Anonim
Publisher : Unknown
Page : 128 pages
File Size : 45,8 Mb
Release : 19??
Category : Electronic
ISBN : 1461464382

Get Book

Encyclopedia of Signaling Molecules by Anonim Pdf

Author : Antonino Belfiore,Derek LeRoith
Publisher : Springer
Page : 0 pages
File Size : 42,7 Mb
Release : 2018-02-08
Category : Medical
ISBN : 3319446746

Get Book

Principles of Endocrinology and Hormone Action by Antonino Belfiore,Derek LeRoith Pdf

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.