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Author: Andrea Bellelli
Publisher: John Wiley & Sons
ISBN: 111923848X
Category : Science
Languages : en
Pages : 309
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Book Description
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: Andrea Bellelli
Publisher: John Wiley & Sons
ISBN: 111923848X
Category : Science
Languages : en
Pages : 309
Get Book Here
Book Description
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
ISBN: 0471723266
Category : Science
Languages : en
Pages : 295
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Book Description
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: Nita K. Pandit
Publisher: Lippincott Williams & Wilkins
ISBN: 0781744784
Category : Medical
Languages : en
Pages : 419
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Book Description
This unique textbook provides an introductory, yet comprehensive overview of the pharmaceutical sciences. It is the first text of its kind to pursue an interdisciplinary approach in this area of study. Readers are introduced to basic concepts related to the specific disciplines in the pharmaceutical sciences, including pharmacology, pharmaceutics, pharmacokinetics, and medicinal chemistry. In an easy-to-read writing style, the book provides readers with up-to-date information on pharmacogenomics and includes comprehensive coverage of industrial drug development and regulatory approval processes. Each chapter includes chapter outlines and critical-thinking exercises, as well as numerous tables and graphs. More than 160 illustrations complement the text.
Author: Benjamin F. Cravatt
Publisher: Springer
ISBN: 3030111431
Category : Medical
Languages : en
Pages : 420
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Book Description
This volume provides a collection of contemporary perspectives on using activity-based protein profiling (ABPP) for biological discoveries in protein science, microbiology, and immunology. A common theme throughout is the special utility of ABPP to interrogate protein function and small-molecule interactions on a global scale in native biological systems. Each chapter showcases distinct advantages of ABPP applied to diverse protein classes and biological systems. As such, the book offers readers valuable insights into the basic principles of ABPP technology and how to apply this approach to biological questions ranging from the study of post-translational modifications to targeting bacterial effectors in host-pathogen interactions.
Author: C. Beckers
Publisher: Springer Science & Business Media
ISBN: 9780792302544
Category : Medical
Languages : en
Pages : 312
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Book Description
Proceedings of a workshop held in Brussels, Belgium within the framework of the European Community Medical and Public Health Research
Author: Holger Gohlke
Publisher: John Wiley & Sons
ISBN: 3527329668
Category : Medical
Languages : en
Pages : 361
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Book Description
Innovative and forward-looking, this volume focuses on recent achievements in this rapidly progressing field and looks at future potential for development. The first part provides a basic understanding of the factors governing protein-ligand interactions, followed by a comparison of key experimental methods (calorimetry, surface plasmon resonance, NMR) used in generating interaction data. The second half of the book is devoted to insilico methods of modeling and predicting molecular recognition and binding, ranging from first principles-based to approximate ones. Here, as elsewhere in the book, emphasis is placed on novel approaches and recent improvements to established methods. The final part looks at unresolved challenges, and the strategies to address them. With the content relevant for all drug classes and therapeutic fields, this is an inspiring and often-consulted guide to the complexity of protein-ligand interaction modeling and analysis for both novices and experts.
Author: Alan A. Boulton
Publisher: Humana
ISBN:
Category : Medical
Languages : en
Pages : 616
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Book Description
Techniques in the neurosciences are evolving rapidly. There are currently very few volumes dedicated to the methodology - ployed by neuroscrentists, and those that are available often seem either out of date or limited in scope. This series is about the methods most widely used by modern-day neuroscientists and 1s written by their colleagues who are practicing experts. Volume 1 will be useful to all neuroscientists since it concerns those procedures used routinely across the widest range of s- drsciplines. Collecting these general techniques together in a single volume stnkes us not only as a service, but will no doubt prove of exceptional utilitarian value as well. Volumes 2 and 3 describe all current procedures for the analyses of ammes and theirmetabolites and of amino acrds, respectively. These collections will clearly be of value to all neuroscientists working in or contemplating research in these fields. Similar reasons exist for Volume 4 on receptor binding techniques since experimental details are provided for many types of ligand-receptor binding, including chapters on general prin- ples, drug discovery and development, and a most useful app- dix on computer programs for Scatchard, nonlinear, and compe- tive displacement analyses. Volume 5 provides procedures for the assessment of enzymes involved in biogenic amine synthesis and catabolism. Volumes in the NEUROMETHODS series will be useful to neurochemists, -pharmacologists, -physrologists, -anatomists, psychopharmacologists, psychiatrists, neurologists, and chemists (organic, analytical, pharmaceutical, medicinal); in fact, everyone involved in the neurosciences, both basic and clinical.
Author: György Keserü
Publisher: John Wiley & Sons
ISBN: 352733582X
Category : Medical
Languages : en
Pages : 360
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Book Description
This practical reference for medicinal and pharmaceutical chemists combines the theoretical background with modern methods as well as applications from recent lead finding and optimization projects. Divided into two parts on the thermodynamics and kinetics of drug-receptor interaction, the text provides the conceptual and methodological basis for characterizing binding mechanisms for drugs and other bioactive molecules. It covers all currently used methods, from experimental approaches, such as ITC or SPR, right up to the latest computational methods. Case studies of real-life lead or drug development projects are also included so readers can apply the methods learned to their own projects. Finally, the benefits of a thorough binding mode analysis for any drug development project are summarized in an outlook chapter written by the editors.
Author: Emma Raven
Publisher: Royal Society of Chemistry
ISBN: 1782622624
Category : Science
Languages : en
Pages : 389
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Book Description
Heme peroxidases are widely distributed in biological systems and are involved in a wide range of processes essential for life. This book provides a comprehensive single source of information on the various aspects of heme peroxidase structure, function and mechanism of action. Chapters written and edited by worldwide experts span a range of heme peroxidases from plants, yeast, bacteria and mammals. Discussed functions of peroxidases range from cell wall synthesis, synthesis of prostaglandins, role in drug suppression of tuberculosis, and antibacterial activity. Included is a discussion of peroxidases that also act as catalases and oxygenases. Heme Peroxidases serves as an essential text for those working in industry and academia in biochemistry and metallobiology.
Author: Christophe Chipot
Publisher: Springer Science & Business Media
ISBN: 3540384472
Category : Language Arts & Disciplines
Languages : en
Pages : 528
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Book Description
Free energy constitutes the most important thermodynamic quantity to understand how chemical species recognize each other, associate or react. Examples of problems in which knowledge of the underlying free energy behaviour is required, include conformational equilibria and molecular association, partitioning between immiscible liquids, receptor-drug interaction, protein-protein and protein-DNA association, and protein stability. This volume sets out to present a coherent and comprehensive account of the concepts that underlie different approaches devised for the determination of free energies. The reader will gain the necessary insight into the theoretical and computational foundations of the subject and will be presented with relevant applications from molecular-level modelling and simulations of chemical and biological systems. Both formally accurate and approximate methods are covered using both classical and quantum mechanical descriptions. A central theme of the book is that the wide variety of free energy calculation techniques available today can be understood as different implementations of a few basic principles. The book is aimed at a broad readership of graduate students and researchers having a background in chemistry, physics, engineering and physical biology.
