Design Of Enzyme Inhibitors As Drugs
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Design Of Enzyme Inhibitors As Drugs
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Author : Merton Sandler
language : en
Publisher:
Release Date : 1989
Design Of Enzyme Inhibitors As Drugs written by Merton Sandler and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 1989 with Enzyme inhibitors categories.
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.
Enzymes As Targets For Drug Design
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Author : Michael Palfreyman
language : en
Publisher: Elsevier
Release Date : 2012-12-02
Enzymes As Targets For Drug Design written by Michael Palfreyman and has been published by Elsevier this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012-12-02 with Medical categories.
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
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Author : H. J. Smith
language : en
Publisher:
Release Date : 1989
Design Of Enzyme Inhibitors As Drugs written by H. J. Smith and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 1989 with Enzyme inhibitors categories.
Drug Design Of Zinc Enzyme Inhibitors
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Author : Claudiu T. Supuran
language : en
Publisher: John Wiley & Sons
Release Date : 2009-10-22
Drug Design Of Zinc Enzyme Inhibitors written by Claudiu T. Supuran and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2009-10-22 with Medical categories.
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.
Evaluation Of Enzyme Inhibitors In Drug Discovery
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Author : Robert A. Copeland
language : en
Publisher: John Wiley & Sons
Release Date : 2005-04-01
Evaluation Of Enzyme Inhibitors In Drug Discovery written by Robert A. Copeland and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2005-04-01 with Science categories.
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.
Drug Action And Design
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Author : Thomas I. Kalman
language : en
Publisher: North-Holland
Release Date : 1979
Drug Action And Design written by Thomas I. Kalman and has been published by North-Holland this book supported file pdf, txt, epub, kindle and other format this book has been release on 1979 with Medical categories.
Structure Based And Mechanism Based Enzyme Inhibitor Drug Design And Drug Action
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Author : Richard B. Silverman
language : en
Publisher:
Release Date : 1996
Structure Based And Mechanism Based Enzyme Inhibitor Drug Design And Drug Action written by Richard B. Silverman and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 1996 with Enzyme inhibitors categories.
Drug Action And Design
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Author :
language : en
Publisher:
Release Date :
Drug Action And Design written by and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on with categories.
Evaluation Of Enzyme Inhibitors In Drug Discovery
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Author : Robert A. Copeland
language : en
Publisher: John Wiley & Sons
Release Date : 2013-01-31
Evaluation Of Enzyme Inhibitors In Drug Discovery written by Robert A. Copeland and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2013-01-31 with Science categories.
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.
An Introduction To Drug Design
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Author : S. N. Pandeya
language : en
Publisher: New Age International
Release Date : 1997
An Introduction To Drug Design written by S. N. Pandeya and has been published by New Age International this book supported file pdf, txt, epub, kindle and other format this book has been release on 1997 with Drugs categories.
The Book Entitled, An Introduction To Drug Design Aims To Optimize The Discovery Of Drugs At A Low Cost And On Occasions To Change Their Pharmacokinetic And Pharmacodyanamic Properties. The Introductory Chapter Which Forms The Basis Of Drug Discovery Is Followed By The Present-Day Thinking Regarding The Best Approaches To Drug Discovery Are Considered. Similarly, There Have Been Major Advances In The Employment Of Computers In Structure-Activity Analysis, And A Discussion Of The State Of The Art In This Area Is Also Included.The Chapter On Qsar Highlights The Role Of Physico-Chemical Parameters In Predicting The Future Course Of Drug Discovery With Rational Drug Design. The Role Of Enzymes In Drug Action Is Well Established, And A Chapter On Design Of Enzyme Inhibitors Is Well Documented. In Addition, The Increased Understanding Of The Design And Utilisation Of Prodrugs Has Led To A Discussion Of The Relevant Issues In This Text.Thus The Book Will Fill The Need Of A Text For Designing New Drugs And The Principles Of New Drug Discovery.