Drug Design Of Zinc Enzyme Inhibitors
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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.
Zinc Enzyme Inhibitors
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Author : Claudiu T. Supuran
language : en
Publisher: Springer
Release Date : 2016-11-04
Zinc Enzyme Inhibitors written by Claudiu T. Supuran and has been published by Springer this book supported file pdf, txt, epub, kindle and other format this book has been release on 2016-11-04 with Science categories.
Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.
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.
Enzymes And Their Inhibitors
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Author : H. John Smith
language : en
Publisher: CRC Press
Release Date : 2004-11-29
Enzymes And Their Inhibitors written by H. John Smith and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2004-11-29 with Medical categories.
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
Carbonic Anhydrase As Drug Target
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Author : Daumantas Matulis
language : en
Publisher: Springer
Release Date : 2019-05-21
Carbonic Anhydrase As Drug Target written by Daumantas Matulis and has been published by Springer this book supported file pdf, txt, epub, kindle and other format this book has been release on 2019-05-21 with Science categories.
This book offers deep insights into the thermodynamics and molecular structures of the twelve catalytically active isoforms of human carbonic anhydrase (CA) with a particular focus on inhibitor binding for drug design. X-ray crystallographic structures in combination with enzyme kinetic testing provide information on the interaction of CAs and their inhibitors, knowledge which is crucial for rational drug design. CAs are zinc carrying enzymes that catalyse the reversible interconversion of carbon dioxide and bicarbonate and are involved in numerous cellular processes. They are therefore a common target for drugs. The suppression of CA activities through inhibitory compounds has found application for example in diuretics and in glaucoma therapy. In this book methods used to determine binding thermodynamics of inhibitory compounds (Isothermal titration calorimetry, Fluorescent thermal shift assay/differential scanning fluorimetry and others) will be compared in detail. Also types and chemical synthesis of CA inhibitors, the use of antibodies against CAs as well as inhibitor application in animals are discussed.
Application Of Computer Based Methods To Design Inhibitors Of Zinc Dependent Enzymes
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Author : Jelena Melesina
language : en
Publisher:
Release Date : 2018*
Application Of Computer Based Methods To Design Inhibitors Of Zinc Dependent Enzymes written by Jelena Melesina and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2018* with categories.
Zinc-dependent enzymes; HDAC; LpxC; computer-aided drug design; molecular modeling; homology modeling; molecular docking; binding free energy calculations; virtual screening; antiparasitic
Design Of Enzyme Inhibitors As Drugs
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Author : Merton Sandler
language : en
Publisher: Oxford University Press, USA
Release Date : 1989
Design Of Enzyme Inhibitors As Drugs written by Merton Sandler and has been published by Oxford University Press, USA this book supported file pdf, txt, epub, kindle and other format this book has been release on 1989 with Language Arts & Disciplines 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.
Structure Based Design Of Inhibitors Of The Zinc Dependent Enzymes Histone Deacetylase Hdac And Udp 3 O R 3 Hydroxymyristoylyl N Acetylglucosamine Deacetylase Lpxc
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Author : Emre Fatih Bülbül
language : en
Publisher:
Release Date : 2023*
Structure Based Design Of Inhibitors Of The Zinc Dependent Enzymes Histone Deacetylase Hdac And Udp 3 O R 3 Hydroxymyristoylyl N Acetylglucosamine Deacetylase Lpxc written by Emre Fatih Bülbül and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2023* with categories.
Computer-aided drug design, zinc-dependent enzymes, HDAC, LpxC, tcDAC2, molecular docking, molecular dynamics, binding free energy calculations.
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.
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.