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 : 43. 69 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.

The Organic Chemistry Of Drug Design And Drug Action

Author : Richard B. Silverman
ISBN : 9780123820310
Genre : Medical
File Size : 76. 72 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 the reader to extrapolate those core principles and mechanisms to many related classes of drug molecules. This new edition reflects significant changes in the process of drug design over the last decade. It preserves the successful approach of the previous editions while including significant changes in format and coverage. 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

Simulating Enzyme Reactivity

Author : Inaki Tunon
ISBN : 9781782624295
Genre :
File Size : 40. 42 MB
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Introduction To Enzyme And Coenzyme Chemistry

Author : T. D. H. Bugg
ISBN : 9781118348994
Genre : Science
File Size : 77. 30 MB
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Enzymes are giant macromolecules which catalyse biochemical reactions. They are remarkable in many ways. Their three-dimensional structures are highly complex, yet they are formed by spontaneous folding of a linear polypeptide chain. Their catalytic properties are far more impressive than synthetic catalysts which operate under more extreme conditions. Each enzyme catalyses a single chemical reaction on a particular chemical substrate with very high enantioselectivity and enantiospecificity at rates which approach “catalytic perfection”. Living cells are capable of carrying out a huge repertoire of enzyme-catalysed chemical reactions, some of which have little or no precedent in organic chemistry. The popular textbook Introduction to Enzyme and Coenzyme Chemistry has been thoroughly updated to include information on the most recent advances in our understanding of enzyme action, with additional recent examples from the literature used to illustrate key points. A major new feature is the inclusion of two-colour figures, and the addition of over 40 new figures of the active sites of enzymes discussed in the text, in order to illustrate the interplay between enzyme structure and function. This new edition provides a concise but comprehensive account from the perspective of organic chemistry, what enzymes are, how they work, and how they catalyse many of the major classes of enzymatic reactions, and will continue to prove invaluable to both undergraduate and postgraduate students of organic, bio-organic and medicinal chemistry, chemical biology, biochemistry and biotechnology.

Applications Of Microdialysis In Pharmaceutical Science

Author : Tung-Hu Tsai
ISBN : 1118011287
Genre : Medical
File Size : 48. 79 MB
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Discover new and emerging applications for microdialysis in drug evaluation Microdialysis is a highly valuable sampling tool that can be used in vivo to measure free, unbound analyte concentrations located in interstitial and extracellular spaces. This book explores the full range of clinical applications for microdialysis, focusing on its use in different organ and tissue systems for pharmacokinetic and pharmacodynamic studies. Readers gain a full understanding of the underlying science of microdialysis, current techniques and practices, as well as its many applications in pharmaceutical research. Applications of Microdialysis in Pharmaceutical Science starts with an introduction to basic principles and then covers analytical considerations, pharmacodynamic and pharmacokinetic studies, clinical aspects, and special applications. Topics include: Role of microdialysis in drug development, including crucial sampling considerations and applications for nervous system diseases Continuous measurement of glucose concentrations in diabetics Applications for clinical evaluation and basic research on organ systems, including monitoring exogenous and endogenous compounds in the lungs Pharmacokinetic and pharmacodynamic evaluation of anticancer drugs Comparison of microdialysis with imaging approaches to evaluate in vivo drug distribution Special applications of microdialysis in studies of cell culture assays, drug-drug interactions, and environmental monitoring Throughout the book, readers will find simple models that clarify complex concepts and easy-to-follow examples that guide them through key applications in pharmaceutical research. In short, this book enables pharmaceutical researchers to take full advantage of microdialysis techniques for the preclinical and clinical evaluation of drugs and much more.

Evaluation Of Enzyme Inhibitors In Drug Discovery

Author : Robert A. Copeland
ISBN : 9780471723264
Genre : Science
File Size : 64. 34 MB
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Carrier Bound Immobilized Enzymes

Author : Linqiu Cao
ISBN : 9783527607082
Genre : Science
File Size : 54. 95 MB
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The first systematic overview of this key technique since the early 1990s, this authoritative reference is the only handbook available to include all recent developments. The author draws on his wide-ranging experience in both academia and industry to systematically cover all types of enzyme immobilization methods, such as adsorption-based and covalent immobilization, as well as enzyme entrapment and encapsulation. Throughout, a careful review of materials and techniques for the generation of functional immobilized enzymes benefits both developers and users of carrier-bound enzymes. A must for biotechnologists, biochemists and preparative chemists using enzymes in their daily work.

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