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Receptor Pharmacology and Function by Michael Williams,Richard A. Glennon Pdf
Based on a symposium held in Boston, Aug. 1985. Twenty-one studies present the theory and handling of radioligand binding that has revolutionized the study of receptor function and compound discovery. they cover basic principles of receptor theory and data analysis, molecular modeling, and structure
The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems by T. Kenakin,J. A. Angus Pdf
This, the 148th volume of the Handbook of Experimental Pharmacology series, focuses on the very core of pharmacology, namely receptor theory. It is fitting that the originator of receptor pharmacology, A. J. CLARK, authored the fourth volume of this series 63 years ago. In that volume CLARK further developed his version of receptor theory first described four years earlier in his classic book The Mode of Action of Drugs. An examination of the topics covered in volume 4 reveals a striking similarity to the topics covered in this present volume; pharmacologists today are still as interested in unlocking the secrets of dose-response relationships to reveal the biological and che mical basis of drug action as they were over half a century ago. Sections in that 1937 volume such as "Curves relating exposure to drugs with biological effects" and "Implications of monomolecular theory" show Clark's keen insight into the essential questions that required answers to move pharma cology forward. With the advent of molecular biological cloning of human receptors has come a transformation of receptor pharmacology. Thus the expression of human receptors into surrogate host cells helped unlock secrets of receptor mechanisms and stimulus-transduction pathways. To a large extent, this elim inates the leap of faith required to apply receptor activity of drugs tested on animal receptor systems to the human therapeutic arena. However, a new leap of faith concerning the veracity of the effects found in recombinant systems with respect to natural ones is now required.
Textbook of Receptor Pharmacology, Second Edition by John C. Foreman,Torben Johansen Pdf
The bestselling first edition of Textbook of Receptor Pharmacology originated from a renowned course in receptor pharmacology taught at the University College of London for the past three decades. Its innovative format united four major approaches to the study of receptors: molecular biology, quantitative functional studies of agonists and antagonists, ligand binding, and signal transduction systems. The second edition builds on this foundation. This edition streamlines the material and focuses on cell membrane receptors along with their immediate signal transducers. The section on the molecular structure of receptors reflects the advances in this area. This edition also includes two restructured new chapters, one on G-proteins and one on tyrosine kinases, as signal transductors. Several chapters also contain problems for students to solve as well as worked-out solutions. The book contains over one hundred useful diagrams and tables to aid illustration of concepts and a helpful appendix explaining the simple mathematics used in the text. A time-saving resource and comprehensive textbook, Textbook of Receptor Pharmacology, Second Edition provides in-depth, up-to-date coverage of this still rapidly expanding research area that is both fundamental to the science of pharmacology and on the cutting edge of new drug development.
Textbook of Receptor Pharmacology by John C. Foreman,Torben Johansen,Alasdair J. Gibb Pdf
For the past four decades, University College London has offered a renowned course on receptor pharmacology. Originating from this course, the perennially bestselling Textbook of Receptor Pharmacology has presented in-depth coverage of this rapidly expanding area of research. This third edition continues to combine current understanding of classica
Textbook of Receptor Pharmacology, Third Edition by John C. Foreman,Torben Johansen,Alasdair J. Gibb Pdf
For the past four decades, University College London has offered a renowned course on receptor pharmacology. Originating from this course, the perennially bestselling Textbook of Receptor Pharmacology has presented in-depth coverage of this rapidly expanding area of research. This third edition continues to combine current understanding of classical quantitative pharmacology and drug-receptor interactions with the basics of receptor structure and signal transduction mechanisms, providing an integrated analysis of the mechanisms of drug action at membrane receptors. The hallmark of this popular text is the uniting of four major approaches to the study of receptors: Molecular investigation of receptor structure Quantitative functional studies of agonists and antagonists Ligand binding Signal transduction at the cell membrane Maintaining the second edition’s focus on cell membrane receptors and the immediate signal transduction events at the membrane, this edition includes updated chapters on receptor structure and signal transduction by G-proteins and tyrosine kinases as well as enhancements to the quantitative treatment of drug-receptor interactions. Several chapters contain problems and worked-out solutions, giving students the ability to test their comprehension of the material. Hundreds of diagrams and figures further enhance the text. A time-saving resource and comprehensive learning tool, Textbook of Receptor Pharmacology, Third Edition carries on the tradition of providing in-depth, up-to-date coverage of this critical area that is both fundamental to the science of pharmacology and on the cutting edge of new drug development.
Author : Georges Vauquelin,Bengt von Mentzer Publisher : John Wiley & Sons Page : 264 pages File Size : 40,8 Mb Release : 2008-03-11 Category : Medical ISBN : 047051664X
G Protein-coupled Receptors by Georges Vauquelin,Bengt von Mentzer Pdf
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.
Pharmacology of G Protein Coupled Receptors by Richard R. Neubig 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
Insights into Receptor Function and New Drug Development Targets by P. Michael Conn,Claude Kordon Pdf
This book describes the current state of knowledge in receptor function in the development of new drugs. Science is on the verge of viewing effector molecules and other regulatory sites as therapeutic targets for the amelioration of human and animal disease. The book reviews the availability of state-of-the-art tools that allow measurement of interactions and afford unprecedented insight into the biomolecular interactions that present novel approaches to drug design.
Pharmacologic Analysis of Drug-receptor Interaction by Terrence P. Kenakin Pdf
A guide to quantitative drug-receptor pharmacology, this new edition aims to cover all receptor systems, whether derived from molecular biology or animal studies. Using existing data, it demonstrates how theoretical models facilitate drug development, and integrates theory with practice. This second edition aims to be a valuable resource for all researchers involved in the drug design and development process. Not only has the text been updated and revised, but reflecting the significant technical breakthroughs of recent years, it now more generally encompasses all receptor systems, whether derived from molecular biology or whole animal studies. These systems are examined within the framework of current drug receptor theories, particularly the receptor occupation theory, the operational model of drug action and the ternary complex model.
G Protein-Coupled Receptors by Jesus Giraldo,Jean-Philippe Pin Pdf
G protein-coupled receptors (GPCRs) are the largest family of cell-surface receptors, with more than 800 members identified thus far in the human genome. They regulate the function of most cells in the body, and represent approximately 3% of the genes in the human genome. These receptors respond to a wide variety of structurally diverse ligands, ranging from small molecules, such as biogenic amines, nucleotides and ions, to lipids, peptides, proteins, and even light. Ligands (agonists and antagonists) acting on GPCRs are important in the treatment of numerous diseases, including cardiovascular and mental disorders, retinal degeneration, cancer, and AIDS. It is estimated that these receptors represent about one third of the actual identified targets of clinically used drugs. The determination of rhodopsin crystal structure and, more recently, of opsin, 1 and 2 adrenergic and A2A adenosine receptors provides both academia and industry with extremely valuable data for a better understanding of the molecular determinants of receptor function and a more reliable rationale for drug design. GPCR structure and function constitutes a hot topic. The book, which lies between the fields of chemical biology, molecular pharmacology and medicinal chemistry, is divided into three parts. The first part considers what receptor structures tell us about the mechanism of receptor activation. Part II focuses on receptor function. It discusses what the data from biophysical and mutational studies, and the analysis of the interactions of the receptor with ligands and regulator proteins, tell us about the process of signal transduction. The final part, on modelling and simulation, details new insights on the link between structure and mechanism and their implications in drug design.
Delta Opioid Receptor Pharmacology and Therapeutic Applications by Emily M. Jutkiewicz Pdf
This volume describes our current understanding of the biological role of the delta-opioid receptor (DOR) system, focusing on its unique mechanisms of receptor trafficking and signaling in disease states. Part 1 covers the endogenous ligands that regulate the DOR system as well as novel compounds and therapies used to modulate the DOR system. Part 2 describes new insights into the localization and trafficking of the DOR and how ligand-directed signaling alters the fate of the receptor. Part 3 concentrates on the potential role of the DOR system in disease states, such as pain, mood, addiction, and Parkinson’s disease. Throughout the book, the DOR system as a target for drug development will be discussed.
GABAb Receptor Pharmacology: A Tribute to Norman Bowery by Anonim Pdf
This monograph was assembled to honor Professor Norman Bowery and his work on the 30th anniversary of his discovery of the GABAB receptor. In the present volume, leading neuroscientists from academia and industry provide a perspective of current research, both basic and translational, in the discovery of drugs acting at the GABAB receptor. The topics covered provide a comprehensive review of the field and the current state of research in this area. Included are chapters on the chemistry of GABAB agonists and antagonists, on the genetics and molecular composition of the site, its regulation and trafficking, and its role in controlling cellular, autonomic, and behavioral function. There are also chapters describing the potential clinical utility of drugs regulating GABAB activity receptor in the areas of hypertension, gastroesophageal reflux disease, Down syndrome, depression, and substance abuse. The information contained in this text will be of particular interest to neuroscientists in general and to neuropharmacologists in particular. Articles written by leading investigators in the field Informs and updates on all the latest developments
Dopamine Receptors and Transporters by Hyman B. Niznik Pdf
"Details the function, characterization, and physiology of various dopamine receptor/transporter systems and explores their role in etiology, diagnosis, and disease management."
Biology of the NMDA Receptor by Antonius M. VanDongen Pdf
The NMDA receptor plays a critical role in the development of the central nervous system and in adult neuroplasticity, learning, and memory. Therefore, it is not surprising that this receptor has been widely studied. However, despite the importance of rhythms for the sustenance of life, this aspect of NMDAR function remains poorly studied. Written
