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Targeting Enzymes for Pharmaceutical Development

Targeting Enzymes for Pharmaceutical Development
Author: Nikolaos E. Labrou
Publisher: Humana
Total Pages: 290
Release: 2020-12-11
Genre: Medical
ISBN: 9781071601655

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This volume explores detailed methods and experimental protocols evaluating the effect of a compound or a mixture of compounds on the action of enzymes that are significant targets in pharmaceuticals. Consisting of three sections, the book delves into recent biocomputing and bioinformatics protocols, state-of-the art modern biophysical, electrophoretic, and chromatographic methods and high-throughput screening approaches, as well as detailed protocols and examples of the inhibition analysis and evaluation of selected enzymes. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and cutting-edge, Targeting Enzymes for Pharmaceutical Development: Methods and Protocols serves as a vital reference for academics and industry professionals working on expanding our understanding of the wide range of important enzyme targets.


Enzymes as Targets for Drug Design

Enzymes as Targets for Drug Design
Author: Michael Palfreyman
Publisher: Elsevier
Total Pages: 282
Release: 2012-12-02
Genre: Medical
ISBN: 0323140483

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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.


Enzyme Inhibition in Drug Discovery and Development

Enzyme Inhibition in Drug Discovery and Development
Author: Chuang Lu
Publisher: John Wiley & Sons
Total Pages: 878
Release: 2010-01-26
Genre: Medical
ISBN: 0470538945

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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

Enzyme Technologies
Author: Hsiu-Chiung Yang
Publisher: John Wiley & Sons
Total Pages: 356
Release: 2013-11-22
Genre: Science
ISBN: 1118739892

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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.


Enzymes and Their Inhibitors

Enzymes and Their Inhibitors
Author: H. John Smith
Publisher: CRC Press
Total Pages: 325
Release: 2004-11-29
Genre: Medical
ISBN: 0203414586

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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


Drug Design of Zinc-Enzyme Inhibitors

Drug Design of Zinc-Enzyme Inhibitors
Author: Claudiu T. Supuran
Publisher: John Wiley & Sons
Total Pages: 1040
Release: 2009-10-22
Genre: Medical
ISBN: 9780470508152

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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.


Biopharmaceutical Drug Design and Development

Biopharmaceutical Drug Design and Development
Author: Susanna Wu-Pong
Publisher: Springer Science & Business Media
Total Pages: 374
Release: 2010-01-11
Genre: Medical
ISBN: 1597455326

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This book provides a comprehensive examination of the newest biopharmaceutical drugs. Among the drugs discussed are ones in the categories of monoclonal antibodies for in-vivo use, cytokines, growth factors, enzymes, immunomodulators, thrombolytics, and immonotherapies including vaccines. Additionally, the volume examines new and emerging technologies, and contains a review of the Human Genome Project.


Natural Products Targeting Clinically Relevant Enzymes

Natural Products Targeting Clinically Relevant Enzymes
Author: Paula B. Andrade
Publisher: John Wiley & Sons
Total Pages: 418
Release: 2017-08-29
Genre: Medical
ISBN: 3527805931

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The past decade has seen the reappearance of natural products as a valuable source of potent therapeutics. Here, experts on bioactive natural products cover the full spectrum of clinically relevant enzymes that are known to be targeted by natural products. Key enzymes include acetylcholine esterase, angiotensin-I-converting enzyme, cyclooxygenase, dihydrofolate reductase, phospholipase A2, respiratory complexes, and many more. By connecting the diversity of medicinal natural product sources with their potential clinical applications, this volume serves as a companion for the medicinal chemist looking for innovative small molecule compounds as well as for pharmacologist interested in the clinical effects and mode of action of herbal and traditional medicines.


Enzyme Technologies

Enzyme Technologies
Author: Hsiu-Chiung Yang
Publisher: Wiley-Interscience
Total Pages: 356
Release: 2013-12-27
Genre: Science
ISBN: 9781118739938

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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.


Therapeutic Enzymes: Function and Clinical Implications

Therapeutic Enzymes: Function and Clinical Implications
Author: Nikolaos Labrou
Publisher: Springer Nature
Total Pages: 388
Release: 2019-09-03
Genre: Science
ISBN: 981137709X

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Therapeutic enzymes exhibit fascinating features and opportunities, and represent a significant and promising subcategory of modern biopharmaceuticals for the treatment of several severe diseases. Research and drug developments efforts and the advancements in biotechnology over the past twenty years have greatly assisted the introduction of efficient and safe enzyme-based therapies for a range of both rare and common disorders. The introduction and regulatory approval of twenty different recombinant enzymes has enabled effective enzyme-replacement therapy. This volume aims to overview these therapeutic enzymes, focusing in particular on more recently approved enzymes produced by recombinant DNA technology. This volume is composed of four sections. Section 1 provides an overview of the production process and biochemical characterization of therapeutic enzymes, while Section 2 focuses upon the engineering strategies and delivery methods of therapeutic enzymes. Section 3 highlights the clinical applications of approved therapeutic enzymes, including aspects on their structure, indications and mechanisms of action. Together with information on these mechanisms, safety and immunogenicity issues and various adverse events of the recombinant enzymes used for therapy are discussed. Section 4, provides discussion on the prospective and future developments of new therapeutic enzymes. This book is aimed at academics, researchers and students undertaking advanced undergraduate/postgraduate programs in the biopharmaceutical/biotechnology area who wish to gain a comprehensive understanding of enzyme-based therapeutic molecules.