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Enzymes as Targets for Drug Design

2012-12-02 Medical
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Release : 2012-12-02
Genre : Medical
Kind : eBook
Book Rating : 483/5 ( reviews)

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Book Synopsis Enzymes as Targets for Drug Design by : Michael Palfreyman

Download or read book Enzymes as Targets for Drug Design written by Michael Palfreyman. This book was released on 2012-12-02. Available in PDF, EPUB and Kindle. Book excerpt: Enzymes as Targets for Drug Design is a collection of scientific discussions related to enzyme inhibitors that show the many facets of the drug discovery process from the basic sciences through clinical applications. Topics include the biogenesis of phosphatidylinositol glycosyl membrane proteins, structure and catalytic function of ADP-ribose polymerase (ADPRT), and modulation of the dopaminergic system in cardiovascular therapeutics. The therapeutic utility of selected enzyme-activated irreversible inhibitors, the role of proteinases in the fibrosis of systemic sclerosis, and therapeutic opportunities in eicosanoid biosynthesis are also discussed. This book consists of 18 chapters and begins with examples of enzymes whose activities have recently been elucidated, or for which newer insights have been gleaned, but which do not yet have selective or potent inhibitors. The second part provides examples of enzymes where inhibitors have been identified but it is still not clear whether or not such an enzymatic blockade will be therapeutically beneficial. The final section describes clinical studies of newer, and not so new, enzyme inhibitors that are clearly of therapeutic importance. The therapeutic activity of monoamine oxidase inhibitors and the associated clinical issues are considered. This book is intended for clinicians as well as basic scientists in biochemistry, chemistry, pharmacology, and cell biology.

Design of Enzyme Inhibitors as Drugs

1989 Enzyme inhibitors
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Release : 1989
Genre : Enzyme inhibitors
Kind : eBook
Book Rating : 374/5 ( reviews)

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Book Synopsis Design of Enzyme Inhibitors as Drugs by : Merton Sandler

Download or read book Design of Enzyme Inhibitors as Drugs written by Merton Sandler. This book was released on 1989. Available in PDF, EPUB and Kindle. Book excerpt: A collection of essays examining the major target enzymes and their inhibitors. The underlying physical and chemical processes of enzyme inhibition, the principles of inhibitor design using computer-based techniques, and clinical applications are described.

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.

Design of enzyme inhibitors as drugs

1989 Enzyme inhibitors
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Release : 1989
Genre : Enzyme inhibitors
Kind : eBook
Book Rating : 373/5 ( reviews)

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Book Synopsis Design of enzyme inhibitors as drugs by : H. J. Smith

Download or read book Design of enzyme inhibitors as drugs written by H. J. Smith. This book was released on 1989. Available in PDF, EPUB and Kindle. Book excerpt:

Drug Design of Zinc-Enzyme Inhibitors

2009-10-22 Medical
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Release : 2009-10-22
Genre : Medical
Kind : eBook
Book Rating : 152/5 ( reviews)

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Book Synopsis Drug Design of Zinc-Enzyme Inhibitors by : Claudiu T. Supuran

Download or read book Drug Design of Zinc-Enzyme Inhibitors written by Claudiu T. Supuran. This book was released on 2009-10-22. Available in PDF, EPUB and Kindle. Book excerpt: Brings together functional and structural informationrelevant to the design of drugs targeting zinc enzymes The second most abundant transition element in living organisms, zinc spans all areas of metabolism, with zinc-containing proteins offering both established and potential drug targets. Drug Design of Zinc-Enzyme Inhibitors brings together functional and structural information relevant to these zinc-containing targets. With up-to-date overviews of the latest developments field, this unique and comprehensive text enables readers to understand zinc enzymes and evaluate them in a drug design context. With contributions from the leaders of today's research, Drug Design of Zinc-Enzyme Inhibitors covers such key topics as: Major drug targets like carbonic anhydrases, matrix metalloproteinases, bacterial proteases, angiotensin-converting enzyme, histone deacetylase, and APOBEC3G Roles of recently discovered zinc-containing isozymes in cancer, obesity, epilepsy, pain management, malaria, and other conditions Cross reactivity of zinc-enzyme inhibitors and activators The extensive use of X-ray crystallography and QSAR studies for understanding zinc-containing proteins Clinical applications An essential resource for the discovery and development of new drug molecules, Drug Design of Zinc-Enzyme Inhibitors gives researchers, professionals, students, and academics the foundation to understand and work with zinc enzyme inhibitors and activators.

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