Enzymes As Targets For Drug Design
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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.
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.
Proteinases As Drug Targets
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Author : Ben Dunn
language : en
Publisher: Royal Society of Chemistry
Release Date : 2011-11-22
Proteinases As Drug Targets written by Ben Dunn and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2011-11-22 with Science categories.
This book provides vital information on a class of enzymes that have emerged as key drug targets in a number of human diseases, including HIV/AIDS, Hypertension, Cancer, and Alzheimer's disease. There is a gap in information due to the lack of recent international meetings on this subject and, thus, no recent summaries of current research have emerged. The book contains up-to-date information, especially with the genomics revolution of recent years, and includes new proteomics techniques. The story of this enzyme family also includes the most significant efforts in computer-aided drug discovery and structure-based drug design. With contributions from experts in the field, the book is edited by the previous President of the International Proteolysis Society, whose academic career in the field has spanned 35 years.
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.
Enzyme Inhibition In Drug Discovery And Development
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Author : Chuang Lu
language : en
Publisher: John Wiley & Sons
Release Date : 2010-01-26
Enzyme Inhibition In Drug Discovery And Development written by Chuang Lu 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 2010-01-26 with Medical categories.
The science and applied approaches of enzyme inhibition in drug discovery and development Offering a unique approach that includes both the pharmacologic and pharmaco-kinetic aspects of enzyme inhibition, Enzyme Inhibition in Drug Discovery and Development examines the scientific concepts and experimental approaches related to enzyme inhibition as applied in drug discovery and drug development. With chapters written by over fifty leading experts in their fields, Enzyme Inhibition in Drug Discovery and Development fosters a cross-fertilization of pharmacology, drug metabolism, pharmacokinetics, and toxicology by understanding the "good" inhibitions—desirable pharmacological effects—and "bad" inhibitions—drug–drug interactions and toxicity. The book discusses: The drug discovery process, including drug discovery strategy, medicinal chemistry, analytical chemistry, drug metabolism, pharmacokinetics, and safety biomarker assessment The manipulations of drug metabolizing enzymes and transporters as well as the negative consequences, such as drug–drug interactions The inhibition of several major drug target pathways, such as the GPCR pathway, the NFkB pathway, and the ion channel pathway Through this focused, single-source reference on the fundamentals of drug discovery and development, researchers in drug metabolism and pharmacokinetics (DMPK) will learn and appreciate target biology in drug discovery; discovery biologists and medicinal chemists will also broaden their understanding of DMPK.
Enzyme Technologies
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Author : Hsiu-Chiung Yang
language : en
Publisher: John Wiley & Sons
Release Date : 2013-11-22
Enzyme Technologies written by Hsiu-Chiung Yang 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 2013-11-22 with Science categories.
Sets the stage for advances in drug discovery using the latest enzyme technology Reviewing new and emerging applications of enzyme technology in drug discovery, this book highlights some of the most promising areas of pharmaceutical and biotechnology research. It covers enzyme assay technology, utilization of enzymology for prodrug design, and the application of enzymes as therapeutic agents. Expert reviews highlight how our latest understanding of enzymology is used to develop new practical applications in drug discovery and design. Filled with case studies, Enzyme Technologies: Pluripotent Players in Discovering Therapeutic Agents enables readers to better understand the diverse functions of enzymes and master specific applications in drug discovery research. In addition to small molecule drug discovery, the book explores new developments in enzymes as therapeutic agents for genetic disorders. Section A, Enzymes – Essential Workhorses in Pharmaceutical Research, offers support in selecting the best enzyme targets for drug discovery, designing enzyme inhibitors for therapeutic agents, and evaluating selective enzyme inhibitors. Section B, Enzymes – Indispensable Tools for Improving Druggability, sets forth the principles alongside real-world examples of exploiting specific properties of enzymes to design successful prodrugs. Section C, Enzymes – Powerful Weapons for Correcting Nature's Errors, provides new insights on applying enzymes as therapeutic agents or diagnostic tools to treat genetic disorders. Chapters are contributed by leading experts from around the world. Their contributions are based on a thorough review of the current literature as well as their own research. Reviewing our latest understanding of the nature of enzymes and their role in drug discovery, this book is recommended for researchers in pharmaceuticals and biotechnology as well as for researchers in enzymology, biochemistry, molecular biology, and medicinal chemistry.
Burger S Medicinal Chemistry Drug Discovery And Development
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Author : Donald J. Abraham
language : en
Publisher:
Release Date : 2021
Burger S Medicinal Chemistry Drug Discovery And Development written by Donald J. Abraham and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2021 with Drug development categories.
"Burger's is a flagship reference source for medicinal chemists and pharmaceutical professionals. This updated and expanded 8th edition has been thoroughly revised and improved to incorporate the concepts of drug hunting along with its existing coverage of the entire process of drug discovery and development. Bringing in a new and expert editorial board, this new edition updates existing chapters and adds 35 new ones, with topics including: opioid addiction treatments, antibody and gene therapy for cancer, blood-brain barrier, HIV treatments, and industrial-academic collaboration structures"--
Enzyme Technologies
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Author : Hsiu-Chiung Yang
language : en
Publisher: Wiley-Interscience
Release Date : 2013-12-27
Enzyme Technologies written by Hsiu-Chiung Yang and has been published by Wiley-Interscience this book supported file pdf, txt, epub, kindle and other format this book has been release on 2013-12-27 with Science categories.
Sets the stage for advances in drug discovery using the latest enzyme technology Reviewing new and emerging applications of enzyme technology in drug discovery, this book highlights some of the most promising areas of pharmaceutical and biotechnology research. It covers enzyme assay technology, utilization of enzymology for prodrug design, and the application of enzymes as therapeutic agents. Expert reviews highlight how our latest understanding of enzymology is used to develop new practical applications in drug discovery and design. Filled with case studies, Enzyme Technologies: Pluripotent Players in Discovering Therapeutic Agents enables readers to better understand the diverse functions of enzymes and master specific applications in drug discovery research. In addition to small molecule drug discovery, the book explores new developments in enzymes as therapeutic agents for genetic disorders. Section A, Enzymes – Essential Workhorses in Pharmaceutical Research, offers support in selecting the best enzyme targets for drug discovery, designing enzyme inhibitors for therapeutic agents, and evaluating selective enzyme inhibitors. Section B, Enzymes – Indispensable Tools for Improving Druggability, sets forth the principles alongside real-world examples of exploiting specific properties of enzymes to design successful prodrugs. Section C, Enzymes – Powerful Weapons for Correcting Nature's Errors, provides new insights on applying enzymes as therapeutic agents or diagnostic tools to treat genetic disorders. Chapters are contributed by leading experts from around the world. Their contributions are based on a thorough review of the current literature as well as their own research. Reviewing our latest understanding of the nature of enzymes and their role in drug discovery, this book is recommended for researchers in pharmaceuticals and biotechnology as well as for researchers in enzymology, biochemistry, molecular biology, and medicinal chemistry.
Proteinase And Peptidase Inhibition
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Author : H. John Smith
language : en
Publisher: CRC Press
Release Date : 2002-03-28
Proteinase And Peptidase Inhibition 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 2002-03-28 with Medical categories.
Cellular proteinases and their physiological role in normal and disease states have been the subject of great interest over recent decades. At present, specific protease inhibitors are exploited both as tools in unraveling the role of individual proteinases in particular cellular processes and for the development of chemotherapeutic agents for the
Bacterial Enzymes As Targets For Drug Discovery
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Author : Punit Kaur
language : en
Publisher: Academic Press
Release Date : 2024-11-01
Bacterial Enzymes As Targets For Drug Discovery written by Punit Kaur and has been published by Academic Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2024-11-01 with Medical categories.
Bacterial Enzymes as Targets for Drug Discovery: Meeting the Challenges of Antibiotic Resistance addresses the gap between medical microbiology, structural biology, and genomic science in the development of new antibacterial drug development. This book consolidates detailed profiling of bacterial target enzyme families for the drug discovery process and methodologies for use and validation of the potential drug targets. The content covers the foundations of antibiotic drug discovery process and focuses on bacterial enzymes as drug targets, building a bridge between microbiology, structural biology, and genomic science. This is the ideal reference for antibiotic drug discovery researchers in the pharma industry and academia. Biochemists, microbiologists, and medicinal chemists will also benefit from this books’ content.