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Enzymes and Their Inhibitors

2004-11-29 Medical
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Release : 2004-11-29
Genre : Medical
Kind : eBook
Book Rating : 586/5 ( reviews)

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Book Synopsis Enzymes and Their Inhibitors by : H. John Smith

Download or read book Enzymes and Their Inhibitors written by H. John Smith. This book was released on 2004-11-29. Available in PDF, EPUB and Kindle. Book excerpt: 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 mar

Evaluation of Enzyme Inhibitors in Drug Discovery

2005-04-01 Science
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Release : 2005-04-01
Genre : Science
Kind : eBook
Book Rating : 266/5 ( reviews)

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Book Synopsis Evaluation of Enzyme Inhibitors in Drug Discovery by : Robert A. Copeland

Download or read book Evaluation of Enzyme Inhibitors in Drug Discovery written by Robert A. Copeland. This book was released on 2005-04-01. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Evaluation of Enzyme Inhibitors in Drug Discovery

2013-01-31 Science
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Release : 2013-01-31
Genre : Science
Kind : eBook
Book Rating : 28X/5 ( reviews)

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Book Synopsis Evaluation of Enzyme Inhibitors in Drug Discovery by : Robert A. Copeland

Download or read book Evaluation of Enzyme Inhibitors in Drug Discovery written by Robert A. Copeland. This book was released on 2013-01-31. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Enzyme Inhibitors and Activators

2017-03-29 Science
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Release : 2017-03-29
Genre : Science
Kind : eBook
Book Rating : 579/5 ( reviews)

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Book Synopsis Enzyme Inhibitors and Activators by : Murat Şentürk

Download or read book Enzyme Inhibitors and Activators written by Murat Şentürk. This book was released on 2017-03-29. Available in PDF, EPUB and Kindle. Book excerpt: Over the recent years, medicinal chemistry has become responsible for explaining interactions of chemical molecule processes such that many scientists in the life sciences from agronomy to medicine are engaged in medicinal research. This book contains an overview focusing on the research area of enzyme inhibitor and activator, enzyme-catalyzed biotransformation, usage of microbial enzymes, enzymes associated with programmed cell death, natural products as potential enzyme inhibitors, protease inhibitors from plants in insect pest management, peptidases, and renin-angiotensin system. The book provides an overview on basic issues and some of the recent developments in medicinal science and technology. Especially, emphasis is devoted to both experimental and theoretical aspect of modern medicine. The primary target audience for the book includes students, researchers, chemists, molecular biologists, medical doctors, pharmacologists, and professionals who are interested in associated areas. The textbook is written by international scientists with expertise in biochemistry, enzymology, molecular biology, and genetics, many of which are active in biochemical and pharmacological research. I would like to acknowledge the authors for their contribution to the book. We hope that the textbook will enhance the knowledge of scientists in the complexities of some medical approaches; it will stimulate both professionals and students to dedicate part of their future research in understanding relevant mechanisms and applications of pharmacology.

Nutritional and Toxicological Significance of Enzyme Inhibitors in Foods

1986-10-31 Technology & Engineering
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Release : 1986-10-31
Genre : Technology & Engineering
Kind : eBook
Book Rating : /5 ( reviews)

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Book Synopsis Nutritional and Toxicological Significance of Enzyme Inhibitors in Foods by : Mendel Friedman

Download or read book Nutritional and Toxicological Significance of Enzyme Inhibitors in Foods written by Mendel Friedman. This book was released on 1986-10-31. Available in PDF, EPUB and Kindle. Book excerpt: Soybean protei ns are wi de 1 y used inhuman foods ina vari ety of forms, including baby formulas, flour, soy protein concentrates, soy protein isolates, soy sauces, textured soy fibers, and tofu. The presence of inhibitors of digestive enzymes in soy proteins impairs nutritional quality and possible safety of this impportant legume. Normal processing conditions based on the use of heat do not completely inactivate these inhibitors, so that residual amounts of plant protease inhibitors are consumed by animals and man. Inhibitors of digestive enzymes are present not only in legumes, such as soybeans, lima beans, and kidney beans, but also in nearly all plant foods, including cereals and potatoes, albeit in much smaller amounts. The antinutritional effects of inhibitors of proteolytic enzymes have been widely studied and can be ameliorated by processing and/or sulfur amino acid fortification. A more urgent concern is reports that rats fed diets containing even low levels of soybean-derived inhibitors, which are found in foods such as soy-based baby formulas, may develop over their lifespan pancreatic lesions leading eventually to neoplasia or tumor formation. On the other hand, recent stUdies suggest that certain enzyme inhibitors from plant foods may prevent cancer formation in other tissues. A key question, therefore, is whether inhibitors from plant foods constitute a human health hazard.

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