kinetics of enzyme action essential principles for drug hunters

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Kinetics Of Enzyme Action

Author : Ross L. Stein
ISBN : 1118084403
Genre : Science
File Size : 51. 7 MB
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Few scientists have the knowledge to perform the studies that are necessary to discover and characterize enzyme inhibitors, despite the vested interest the pharmaceutical industry has in this field. Beginning with the most basic principles pertaining to simple, one-substrate enzyme reactions and their inhibitors, and progressing to a thorough treatment of two-substrate enzymes, Kinetics of Enzyme Action: Essential Principles for Drug Hunters provides biochemists, medicinal chemists, and pharmaceutical scientists with numerous case study examples to outline the tools and techniques necessary to perform, understand, and interpret detailed kinetic studies for drug discovery.

Enzyme Kinetics

Author : Hans Bisswanger
ISBN : 9783527806478
Genre : Science
File Size : 41. 99 MB
Format : PDF
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Now in full color for a more intuitive learning experience, this new edition of the long-selling reference also features a number of new developments in methodology and the application of enzyme kinetics. Starting with a description of ligand binding equilibria, the experienced author goes on to discuss simple and complex enzyme reactions in kinetic terms. Special cases such as membrane-bound and immobilized enzymes are considered, as is the influence of external conditions, such as temperature and pH value. The final part of the book then covers a range of widely used measurement methods and compares their performance and scope of application. With its unique mix of theory and practical advice, this is an invaluable aid for teaching as well as for experimental work.

The Organic Chemistry Of Drug Design And Drug Action

Author : Richard B. Silverman
ISBN : 9780123820310
Genre : Medical
File Size : 30. 95 MB
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The Organic Chemistry of Drug Design and Drug Action, Third Edition, represents a unique approach to medicinal chemistry based on physical organic chemical principles and reaction mechanisms that rationalize drug action, which allows reader to extrapolate those core principles and mechanisms to many related classes of drug molecules. This new edition includes updates to all chapters, including new examples and references. It reflects significant changes in the process of drug design over the last decade and preserves the successful approach of the previous editions while including significant changes in format and coverage. This text is designed for undergraduate and graduate students in chemistry studying medicinal chemistry or pharmaceutical chemistry; research chemists and biochemists working in pharmaceutical and biotechnology industries. Updates to all chapters, including new examples and references Chapter 1 (Introduction): Completely rewritten and expanded as an overview of topics discussed in detail throughout the book Chapter 2 (Lead Discovery and Lead Modification): Sections on sources of compounds for screening including library collections, virtual screening, and computational methods, as well as hit-to-lead and scaffold hopping; expanded sections on sources of lead compounds, fragment-based lead discovery, and molecular graphics; and deemphasized solid-phase synthesis and combinatorial chemistry Chapter 3 (Receptors): Drug-receptor interactions, cation-π and halogen bonding; atropisomers; case history of the insomnia drug suvorexant Chapter 4 (Enzymes): Expanded sections on enzyme catalysis in drug discovery and enzyme synthesis Chapter 5 (Enzyme Inhibition and Inactivation): New case histories: for competitive inhibition, the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib and Abelson kinase inhibitor, imatinib for transition state analogue inhibition, the purine nucleoside phosphorylase inhibitors, forodesine and DADMe-ImmH, as well as the mechanism of the multisubstrate analog inhibitor isoniazid for slow, tight-binding inhibition, the dipeptidyl peptidase-4 inhibitor, saxagliptin Chapter 7 (Drug Resistance and Drug Synergism): This new chapter includes topics taken from two chapters in the previous edition, with many new examples Chapter 8 (Drug Metabolism): Discussions of toxicophores and reactive metabolites Chapter 9 (Prodrugs and Drug Delivery Systems): Discussion of antibody–drug conjugates

Evaluation Of Enzyme Inhibitors In Drug Discovery

Author : Robert A. Copeland
ISBN : 9781118540282
Genre : Science
File Size : 74. 4 MB
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Offers essential guidance for discovering and optimizing novel drug therapies Using detailed examples, Evaluation of Enzyme Inhibitors in Drug Discovery equips researchers with the tools needed to apply the science of enzymology and biochemistry to the discovery, optimization, and preclinical development of drugs that work by inhibiting specific enzyme targets. Readers will applaud this book for its clear and practical presentations, including its expert advice on best practices to follow and pitfalls to avoid. This Second Edition brings the book thoroughly up to date with the latest research findings and practices. Updates explore additional forms of enzyme inhibition and special treatments for enzymes that act on macromolecular substrates. Readers will also find new discussions detailing the development and application of the concept of drug-target residence time. Evaluation of Enzyme Inhibitors in Drug Discovery begins by explaining why enzymes are such important drug targets and then examines enzyme reaction mechanisms. The book covers: Reversible modes of inhibitor interactions with enzymes Assay considerations for compound library screening Lead optimization and structure-activity relationships for reversible inhibitors Slow binding and tight binding inhibitors Drug-target residence time Irreversible enzyme inactivators The book ends with a new chapter exploring the application of quantitative biochemical principles to the pharmacologic evaluation of drug candidates during lead optimization and preclinical development. The Second Edition of Evaluation of Enzyme Inhibitors in Drug Discovery continues to offer a treatment of enzymology applied to drug discovery that is quantitative and mathematically rigorous. At the same time, the clear and simple presentations demystify the complex science of enzymology, making the book accessible to many fields— from pharmacology to medicinal chemistry to biophysics to clinical medicine.

Simulating Enzyme Reactivity

Author : Inaki Tunon
ISBN : 9781782624295
Genre : Science
File Size : 78. 11 MB
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Exploring the theories, methodologies and applications in simulations of enzymatic reactions, this book is a great resource for postgraduate students and researchers.

Enzyme Kinetics Catalysis And Control

Author : Daniel L. Purich
ISBN : 9780123809254
Genre : Science
File Size : 88. 4 MB
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Far more than a comprehensive treatise on initial-rate and fast-reaction kinetics, this one-of-a-kind desk reference places enzyme science in the fuller context of the organic, inorganic, and physical chemical processes occurring within enzyme active sites. Drawing on 2600 references, Enzyme Kinetics: Catalysis & Control develops all the kinetic tools needed to define enzyme catalysis, spanning the entire spectrum (from the basics of chemical kinetics and practical advice on rate measurement, to the very latest work on single-molecule kinetics and mechanoenzyme force generation), while also focusing on the persuasive power of kinetic isotope effects, the design of high-potency drugs, and the behavior of regulatory enzymes. Historical analysis of kinetic principles including advanced enzyme science Provides both theoretical and practical measurements tools Coverage of single molecular kinetics Examination of force generation mechanisms Discussion of organic and inorganic enzyme reactions

Drug Metabolism And Pharmacokinetics Quick Guide

Author : Siamak Cyrus Khojasteh
ISBN : 1441956298
Genre : Medical
File Size : 43. 85 MB
Format : PDF
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Drug Metabolism and Pharmacokinetics Quick Guide covers a number of aspects of drug assessment at drug discovery and development stages, topics such as pharmacokinetics, absorption, metabolism, enzyme kinetics, drug transporters, drug interactions, drug-like properties, assays and in silico calculations. It covers key concepts, with useful tables on physiological parameters (eg. blood flow to organs in x-species, expression and localization of enzymes and transporters), chemical structure, nomenclature, and moieties leading to bioactivation (with examples). Overall it includes a number of key topics useful at the drug discovery stage, which would serve as a quick reference with several examples from the literature to illustrate the concept.

Enzyme Biocatalysis

Author : Andrés Illanes
ISBN : 9781402083617
Genre : Technology & Engineering
File Size : 48. 75 MB
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This book was written with the purpose of providing a sound basis for the design of enzymatic reactions based on kinetic principles, but also to give an updated vision of the potentials and limitations of biocatalysis, especially with respect to recent app- cations in processes of organic synthesis. The ?rst ?ve chapters are structured in the form of a textbook, going from the basic principles of enzyme structure and fu- tion to reactor design for homogeneous systems with soluble enzymes and hete- geneous systems with immobilized enzymes. The last chapter of the book is divided into six sections that represent illustrative case studies of biocatalytic processes of industrial relevance or potential, written by experts in the respective ?elds. We sincerely hope that this book will represent an element in the toolbox of gr- uate students in applied biology and chemical and biochemical engineering and also of undergraduate students with formal training in organic chemistry, biochemistry, thermodynamics and chemical reaction kinetics. Beyond that, the book pretends also to illustrate the potential of biocatalytic processes with case studies in the ?eld of organic synthesis, which we hope will be of interest for the academia and prof- sionals involved in R&D&I. If some of our young readers are encouraged to engage or persevere in their work in biocatalysis this will certainly be our more precious reward.

Enzymes And Their Inhibitors

Author : H. John Smith
ISBN : 9780203414583
Genre : Medical
File Size : 54. 66 MB
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Focusing on the development of enzyme inhibitors as therapeutic drugs, Enzymes and Their Inhibitors: Drug Development provides a concise overview of the chemistry of major types of enzymes and their inhibitors. The opening chapters introduce readers to the structure, functions, mechanisms, and kinetics of enzymes, including their use as disease markers, analytical reagents, and in industrial processes. Subsequent chapters discuss the different types of enzyme inhibitors and the principles involved in developing them into effective drugs. This outstanding text, also valuable as a professional reference, will be useful to all students of pharmacology and medicinal chemistry.

Thermodynamics And Kinetics Of Drug Binding

Author : György Keserü
ISBN : 9783527335824
Genre : Medical
File Size : 54. 83 MB
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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.

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