Reversible Ligand Binding

Author : Andrea Bellelli,Jannette Carey
Publisher : John Wiley & Sons
Page : 309 pages
File Size : 48,5 Mb
Release : 2018-01-09
Category : Science
ISBN : 9781119238485

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Reversible Ligand Binding by Andrea Bellelli,Jannette Carey Pdf

Presents the physical background of ligand binding and instructs on how experiments should be designed and analyzed Reversible Ligand Binding: Theory and Experiment discusses the physical background of protein-ligand interactions—providing a comprehensive view of the various biochemical considerations that govern reversible, as well as irreversible, ligand binding. Special consideration is devoted to enzymology, a field usually treated separately from ligand binding, but actually governed by identical thermodynamic relationships. Attention is given to the design of the experiment, which aids in showing clear evidence of biochemical features that may otherwise escape notice. Classical experiments are reviewed in order to further highlight the importance of the design of the experiment. Overall, the book supplies students with the understanding that is necessary for interpreting ligand binding experiments, formulating plausible reaction schemes, and analyzing the data according to the chosen model(s). Topics covered include: theory of ligand binding to monomeric proteins; practical considerations and commonly encountered problems; oligomeric proteins with multiple binding sites; ligand binding kinetics; hemoglobin and its ligands; single-substrate enzymes and their inhibitors; two-substrate enzymes and their inhibitors; and rapid kinetic methods for studying enzyme reactions. Bridges theory of ligand binding and allostery with experiments Applies historical and physical insight to provide a clear understanding of ligand binding Written by a renowned author with long-standing research and teaching expertise in the area of ligand binding and allostery Based on FEBS Advanced Course lectures on the topic Reversible Ligand Binding: Theory and Experiment is an ideal text reference for students and scientists involved in biophysical chemistry, physical biochemistry, biophysics, molecular biology, protein engineering, drug design, pharmacology, physiology, biotechnology, and bioengineering.

Author : Robert A. Copeland
Publisher : John Wiley & Sons
Page : 295 pages
File Size : 55,8 Mb
Release : 2005-04-01
Category : Science
ISBN : 9780471723264

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Evaluation of Enzyme Inhibitors in Drug Discovery by Robert A. Copeland Pdf

Vital information for discovering and optimizing new drugs "Understanding the data and the experimental details that support it has always been at the heart of good science and the assumption challenging process that leads from good science to drug discovery. This book helps medicinal chemists and pharmacologists to do exactly that in the realm of enzyme inhibitors." -Paul S. Anderson, PhD This publication provides readers with a thorough understanding of enzyme-inhibitor evaluation to assist them in their efforts to discover and optimize novel drug therapies. Key topics such as competitive, noncompetitive, and uncompetitive inhibition, slow binding, tight binding, and the use of Hill coefficients to study reaction stoichiometry are all presented. Examples of key concepts are presented with an emphasis on clinical relevance and practical applications. Targeted to medicinal chemists and pharmacologists, Evaluation of Enzyme Inhibitors in Drug Discovery focuses on the questions that they need to address: * What opportunities for inhibitor interactions with enzyme targets arise from consideration of the catalytic reaction mechanism? * How are inhibitors evaluated for potency, selectivity, and mode of action? * What are the advantages and disadvantages of specific inhibition modalities with respect to efficacy in vivo? * What information do medicinal chemists and pharmacologists need from their biochemistry and enzymology colleagues to effectively pursue lead optimization? Beginning with a discussion of the advantages of enzymes as targets for drug discovery, the publication then explores the reaction mechanisms of enzyme catalysis and the types of interactions that can occur between enzymes and inhibitory molecules that lend themselves to therapeutic use. Next are discussions of mechanistic issues that must be considered when designing enzyme assays for compound library screening and for lead optimization efforts. Finally, the publication delves into special forms of inhibition that are commonly encountered in drug discovery efforts, but can be easily overlooked or misinterpreted. This publication is designed to provide students with a solid foundation in enzymology and its role in drug discovery. Medicinal chemists and pharmacologists can refer to individual chapters as specific issues arise during the course of their ongoing drug discovery efforts.

Author : Alexander J. Ninfa,David P. Ballou,Marilee Benore
Publisher : John Wiley & Sons
Page : 480 pages
File Size : 44,6 Mb
Release : 2009-05-26
Category : Science
ISBN : 9780470087664

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Fundamental Laboratory Approaches for Biochemistry and Biotechnology by Alexander J. Ninfa,David P. Ballou,Marilee Benore Pdf

Ninfa/Ballou/Benore is a solid biochemistry lab manual, dedicated to developing research skills in students, allowing them to learn techniques and develop the organizational approaches necessary to conduct laboratory research. Ninfa/Ballou/Benore focuses on basic biochemistry laboratory techniques with a few molecular biology exercises, a reflection of most courses which concentrate on traditional biochemistry experiments and techniques. The manual also includes an introduction to ethics in the laboratory, uncommon in similar manuals. Most importantly, perhaps, is the authors' three-pronged approach to encouraging students to think like a research scientist: first, the authors introduce the scientific method and the hypothesis as a framework for developing conclusive experiments; second, the manual's experiments are designed to become increasingly complex in order to teach more advanced techniques and analysis; finally, gradually, the students are required to devise their own protocols. In this way, students and instructors are able to break away from a "cookbook" approach and to think and investigate for themselves. Suitable for lower-level and upper-level courses; Ninfa spans these courses and can also be used for some first-year graduate work.

Author : Bruce Alberts
Publisher : Unknown
Page : 0 pages
File Size : 52,9 Mb
Release : 2002
Category : Cytology
ISBN : 0815332181

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Molecular Biology of The Cell by Bruce Alberts Pdf

Author : Israel Silman,Hermona Soreq,Lili Anglister,Daniel M. Michaelson,Abraham Fisher
Publisher : CRC Press
Page : 854 pages
File Size : 55,8 Mb
Release : 2004-09-20
Category : Science
ISBN : 1841840750

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Cholinergic Mechanisms by Israel Silman,Hermona Soreq,Lili Anglister,Daniel M. Michaelson,Abraham Fisher Pdf

Providing a cutting-edge profile of research progress in this important field of study, Cholinergic Mechanisms: Function and Dysfunction contains a compilation of the proceedings of the Eleventh ISCM, held in St. Moritz, May 2002. Bringing together 250 contributors from 30 countries, the book presents a comprehensive picture of the cholinergic field. It provides a survey of current understanding of molecular, pharmacological, toxicological, behavioral, and clinical aspects of the cholinergic system. This volume offers a state-of-the-art account of progress in the field from the molecule in the test tube through the cell and the synapse, to the organism and the patient.

Author : Richard C. Pleus,Vladimir Murashov
Publisher : CRC Press
Page : 212 pages
File Size : 47,8 Mb
Release : 2018-07-17
Category : Medical
ISBN : 9781351168588

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Physico-Chemical Properties of Nanomaterials by Richard C. Pleus,Vladimir Murashov Pdf

Throughout human history, we have long encountered the combination of promise, risk, and uncertainty that accompanies emerging technologies. Nanotechnology is a recent example of an emerging technology that promises to drastically improve existing products as well as allow for creative development of new goods and services. This new technology also has its potential downsides. Industry, academia, and regulatory agencies are all working overtime to assess risks accurately while keeping up with the pace of development. Subtle changes in the physicochemical properties of engineered nanomaterials (ENMs) can influence their toxicity and behavior in the environment and so can be used to help control potential ENM risks. This book attempts to encompass the state of the science regarding physicochemical characterization of ENMs. It illuminates the effort to understand these properties and how they may be used to ensure safe ENM deployment in existing or future materials and products.

Author : Reginald Dean,Edward J. Bilsky,S. Stevens Negus
Publisher : Springer Science & Business Media
Page : 757 pages
File Size : 46,6 Mb
Release : 2009-03-12
Category : Medical
ISBN : 9781597451970

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Opiate Receptors and Antagonists by Reginald Dean,Edward J. Bilsky,S. Stevens Negus Pdf

Comprehensive and authoritative, Opioid Receptors and Antagonists: From Bench to Clinic offers neuroscientists, pharmacologists and interested clinicians a unique survey of the extensive and diverse research efforts currently employed with opioid antagonists to develop novel innovative drug therapies. Summarizes the present understanding of the chemistry, pharmacology and molecular biology of opioid receptors and their subtypes Highlights differences and similarities between the opioid pharmacology of animals and human Describes current and potential therapeutic areas for opioid antagonists, including substance abuse, alcohol and ingestive behaviors, behavioral disorders and other medical indications, supported by nonclinical and clinical evidence Focuses on the development of exciting and innovative drug delivery approaches that are being used with opioid antagonists for the above medical indications

Author : Jonathan Bentley,Tilly Bingham
Publisher : Elsevier
Page : 158 pages
File Size : 49,9 Mb
Release : 2023-11-01
Category : Science
ISBN : 9780443137044

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Progress in Medicinal Chemistry by Jonathan Bentley,Tilly Bingham Pdf

Progress in Medicinal Chemistry, Volume 62 provides a review of eclectic developments in medicinal chemistry, with each chapter written by an international board of authors. Provides extended, timely reviews of topics in medicinal chemistry Contains targets and technologies relevant to the discovery of tomorrow’s drugs Presents analyses of successful drug discovery programs

Author : Claudia Binda
Publisher : Springer Nature
Page : 259 pages
File Size : 45,6 Mb
Release : 2022-09-28
Category : Medical
ISBN : 9781071626436

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Monoamine Oxidase by Claudia Binda Pdf

This detailed book examines the main methods to study mammalian monoamine oxidases (MAOs), ranging from cell biology to computational chemistry. Beginning with techniques on how to obtain pure samples of MAO A and MAO B, the volume continues by covering assays and techniques used to measure MAO enzymatic activity and perform inhibition studies, methods to address cellular localization and function of MAOs, either in cell lines or in animal models, as well as computational methods applied to rational drug design approaches that are used to develop new MAO inhibitors. Written for the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step and readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and practical, Monoamine Oxidase: Methods and Protocols serves as a vital resource for scientists who are interested in studying MAOs and other similar amine oxidase enzymes.

Author : Joachim Frank
Publisher : CRC Press
Page : 553 pages
File Size : 43,9 Mb
Release : 2023-10-06
Category : Science
ISBN : 9781000989441

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Novel Developments in Cryo‐EM of Biological Molecules by Joachim Frank Pdf

Cryo-EM, as it is currently practiced in many laboratories, is limited to the visualization of molecules that are in thermal equilibrium at the time before freezing. A further limitation is that the existing software does not fully exploit the information that is contained in the images of large ensembles of molecules in thermal equilibrium. This book is a collection of recent articles by the author, reprinted with introductions, and they mainly describe two novel methods in cryo-EM, one computational and the other experimental that requires the use of a microfluidic device. Both methods have the capacity to shed light on the dynamic behavior of biomolecules. Combined, they greatly expand the range of applications of cryo-EM. The book describes a successful approach in which, based on cryo-EM data, all states visited by the molecule in thermal equilibrium are mapped by manifold embedding—a method of geometric machine learning—and the energy landscape of the molecule is derived. It also discusses methods and biological results of time-resolved cryo-EM, following a reaction in a non-equilibrium system over a short period of time and resulting in the capture of short-lived states that have been inaccessible by standard methods of cryo-EM.

Author : P. Michael Conn
Publisher : Academic Press
Page : 589 pages
File Size : 44,8 Mb
Release : 2013-10-22
Category : Science
ISBN : 9781483268132

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Neuropeptide Technology by P. Michael Conn Pdf

Methods in Neurosciences, Volume 5: Neuropeptide Technology: Gene Expression and Neuropeptide Receptors discusses procedures and tools of assay useful for the identification, purification, and quantification of neuropeptides and their receptors. This volume is divided into two sections—neuropeptide gene expression and neuropeptide receptors. In these sections, this book specifically discusses the assays for peptide products of somatostatin gene expression; molecular assays for rat thyrotropin-releasing hormone gene; and structure, expression, and chromosomal localization of human gene. The gastrin-releasing peptide or mammalian bombesin; semiquantitative analysis of cellular somatostatin mRNA Levels; and atrial natriuretic factor receptor assays are also elaborated. This text likewise covers the receptors for opioid peptides in brain and autoradiography of somatostatin receptors in rat cerebellum. This publication is beneficial to neuroscientists and students intending to acquire knowledge of gene expression and neuropeptide receptors.

Author : John C. Foreman,Torben Johansen,Alasdair J. Gibb
Publisher : CRC Press
Page : 314 pages
File Size : 43,7 Mb
Release : 2010-09-10
Category : Medical
ISBN : 9781420052558

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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

Author : John C. Foreman,Torben Johansen,Alasdair J. Gibb
Publisher : CRC Press
Page : 314 pages
File Size : 52,8 Mb
Release : 2011-06-27
Category : Medical
ISBN : 9781439887578

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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 : R.D. O'Brien
Publisher : Springer Science & Business Media
Page : 356 pages
File Size : 48,7 Mb
Release : 2012-12-06
Category : Science
ISBN : 9781468409796

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General Principles and Procedures by R.D. O'Brien Pdf

The following remarks are intended to serve as an introduction to this particular volume as well as to the whole series of volumes of which this is the first. The intent of the series is to provide an authentic and relatively complete statement about the status of our understanding of the receptors. The models we had in mind while developing this series are The Enzymes, The Proteins, and comparable groups of books. The receptors have received a degree of importance and richness of understanding that makes them deserving of comprehensive and complete coverage. The study of these molecules, which may well include such diverse items as the receptors for hormones, neurohumors, pheromones, taste, and many other chemical signals, have a great deal in common, so that the student of any one of them will wish to know the status of research about the others. This com monality is in part substantive, and in part practical and procedural. Substantively, the receptors are all macromolecules whose function is to re ceive some form of chemical signal and transduce it to a form which is usable by the receiving cell. In this way, a chemical signal may lead to a neural response, to the turning-on of a cell's chromosomes, or to the activation of some enzymic apparatus to produce or release a substance. Because most of these processes are noncatalytic, special techniques not previously commonplace in biochemistry have been developed in order to study the receptors.

Author : JUCKER
Publisher : Birkhäuser
Page : 625 pages
File Size : 50,5 Mb
Release : 2013-03-08
Category : Science
ISBN : 9783034870948

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Progress in Drug Research/Fortschritte der Arzneimittelforschung/Progrés des recherches pharmaceutiques by JUCKER Pdf