Enzyme Inhibition In Drug Discovery And Development

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Enzyme Inhibition in Drug Discovery and Development

Chuang Lu,Albert P. Li
Enzyme Inhibition in Drug Discovery and Development Book PDF

Author : Chuang Lu,Albert P. Li
Publisher : John Wiley & Sons
Page : 878 pages
File Size : 52,5 Mb
Release : 2010-01-26
Category : Medical
ISBN : 9780470538944

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Enzyme Inhibition in Drug Discovery and Development by Chuang Lu,Albert P. Li Pdf

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.

Evaluation of Enzyme Inhibitors in Drug Discovery

Robert A. Copeland
Evaluation of Enzyme Inhibitors in Drug Discovery Book PDF

Author : Robert A. Copeland
Publisher : John Wiley & Sons
Page : 295 pages
File Size : 46,8 Mb
Release : 2005-04-01
Category : Science
ISBN : 9780471723264

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Evaluation of Enzyme Inhibitors in Drug Discovery by Robert A. Copeland Pdf

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.

Evaluation of Enzyme Inhibitors in Drug Discovery

Robert A. Copeland
Evaluation of Enzyme Inhibitors in Drug Discovery Book PDF

Author : Robert A. Copeland
Publisher : John Wiley & Sons
Page : 588 pages
File Size : 50,7 Mb
Release : 2013-01-31
Category : Science
ISBN : 9781118540282

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Evaluation of Enzyme Inhibitors in Drug Discovery by Robert A. Copeland Pdf

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.

Enzymes and Their Inhibitors

H. John Smith,Claire Simons
Enzymes and Their Inhibitors Book PDF

Author : H. John Smith,Claire Simons
Publisher : CRC Press
Page : 325 pages
File Size : 53,5 Mb
Release : 2004-11-29
Category : Medical
ISBN : 9780203414583

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Enzymes and Their Inhibitors by H. John Smith,Claire Simons Pdf

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

Evaluation of Enzyme Inhibitors in Drug Discovery

Robert A. Copeland
Evaluation of Enzyme Inhibitors in Drug Discovery Book PDF

Author : Robert A. Copeland
Publisher : John Wiley & Sons
Page : 588 pages
File Size : 49,7 Mb
Release : 2013-03-18
Category : Science
ISBN : 9781118488133

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Evaluation of Enzyme Inhibitors in Drug Discovery by Robert A. Copeland Pdf

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.

Drug Design of Zinc-Enzyme Inhibitors

Claudiu T. Supuran,Jean-Yves Winum
Drug Design of Zinc Enzyme Inhibitors Book PDF

Author : Claudiu T. Supuran,Jean-Yves Winum
Publisher : John Wiley & Sons
Page : 1040 pages
File Size : 41,9 Mb
Release : 2009-10-22
Category : Medical
ISBN : 0470508159

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Drug Design of Zinc-Enzyme Inhibitors by Claudiu T. Supuran,Jean-Yves Winum Pdf

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.

Enzymes as Targets for Drug Design

Michael Palfreyman
Enzymes as Targets for Drug Design Book PDF

Author : Michael Palfreyman
Publisher : Elsevier
Page : 282 pages
File Size : 47,7 Mb
Release : 2012-12-02
Category : Medical
ISBN : 9780323140485

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Enzymes as Targets for Drug Design by Michael Palfreyman Pdf

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 Technologies

Hsiu-Chiung Yang,Wu-Kuang Yeh,J. R. McCarthy
Enzyme Technologies Book PDF

Author : Hsiu-Chiung Yang,Wu-Kuang Yeh,J. R. McCarthy
Publisher : John Wiley & Sons
Page : 356 pages
File Size : 52,5 Mb
Release : 2013-11-22
Category : Science
ISBN : 9781118739891

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Enzyme Technologies by Hsiu-Chiung Yang,Wu-Kuang Yeh,J. R. McCarthy Pdf

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.

The Organic Chemistry of Drug Design and Drug Action

Richard B. Silverman
The Organic Chemistry of Drug Design and Drug Action Book PDF

Author : Richard B. Silverman
Publisher : Elsevier
Page : 650 pages
File Size : 47,8 Mb
Release : 2012-12-02
Category : Science
ISBN : 9780080513379

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The Organic Chemistry of Drug Design and Drug Action by Richard B. Silverman Pdf

Standard medicinal chemistry courses and texts are organized by classes of drugs with an emphasis on descriptions of their biological and pharmacological effects. This book represents a new approach based on physical organic chemical principles and reaction mechanisms that allow the reader to extrapolate to many related classes of drug molecules. The Second Edition reflects the significant changes in the drug industry over the past decade, and includes chapter problems and other elements that make the book more useful for course instruction. New edition includes new chapter problems and exercises to help students learn, plus extensive references and illustrations Clearly presents an organic chemist's perspective of how drugs are designed and function, incorporating the extensive changes in the drug industry over the past ten years Well-respected author has published over 200 articles, earned 21 patents, and invented a drug that is under consideration for commercialization

Drug Metabolism in Drug Design and Development

Donglu Zhang,Mingshe Zhu,William G. Humphreys
Drug Metabolism in Drug Design and Development Book PDF

Author : Donglu Zhang,Mingshe Zhu,William G. Humphreys
Publisher : John Wiley & Sons
Page : 448 pages
File Size : 53,7 Mb
Release : 2007-11-16
Category : Science
ISBN : 0470191686

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Drug Metabolism in Drug Design and Development by Donglu Zhang,Mingshe Zhu,William G. Humphreys Pdf

The essentials of drug metabolism vital to developing new therapeutic entities Information on the metabolism and disposition of candidate drugs is a critical part of all aspects of the drug discovery and development process. Drug metabolism, as practiced in the pharmaceutical industry today, is a complex, multidisciplinary field that requires knowledge of sophisticated analytical technologies and expertise in mechanistic and kinetic enzymology, organic reaction mechanism, pharmacokinetic analysis, animal physiology, basic chemical toxicology, preclinical pharmacology, and molecular biology. With chapters contributed by experts in their specific areas, this reference covers: * Basic concepts of drug metabolism * The role of drug metabolism in the pharmaceutical industry * Analytical techniques in drug metabolism * Common experimental approaches and protocols Drug Metabolism in Drug Design and Development emphasizes practical considerations such as the data needed, the experiments and analytical methods typically employed, and the interpretation and application of data. Chapters highlight facts, common protocols, detailed experimental designs, applications, and limitations of techniques. This is a comprehensive, hands-on reference for drug metabolism researchers as well as other professionals involved in pre-clinical drug discovery and development.

Enzyme Inhibitors and Activators

Murat Şentürk
Enzyme Inhibitors and Activators Book PDF

Author : Murat Şentürk
Publisher : BoD – Books on Demand
Page : 270 pages
File Size : 52,8 Mb
Release : 2017-03-29
Category : Science
ISBN : 9789535130574

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Enzyme Inhibitors and Activators by Murat Şentürk Pdf

Over the recent years, medicinal chemistry has become responsible for explaining interactions of chemical molecule processes such that many scientists in the life sciences from agronomy to medicine are engaged in medicinal research. This book contains an overview focusing on the research area of enzyme inhibitor and activator, enzyme-catalyzed biotransformation, usage of microbial enzymes, enzymes associated with programmed cell death, natural products as potential enzyme inhibitors, protease inhibitors from plants in insect pest management, peptidases, and renin-angiotensin system. The book provides an overview on basic issues and some of the recent developments in medicinal science and technology. Especially, emphasis is devoted to both experimental and theoretical aspect of modern medicine. The primary target audience for the book includes students, researchers, chemists, molecular biologists, medical doctors, pharmacologists, and professionals who are interested in associated areas. The textbook is written by international scientists with expertise in biochemistry, enzymology, molecular biology, and genetics, many of which are active in biochemical and pharmacological research. I would like to acknowledge the authors for their contribution to the book. We hope that the textbook will enhance the knowledge of scientists in the complexities of some medical approaches; it will stimulate both professionals and students to dedicate part of their future research in understanding relevant mechanisms and applications of pharmacology.

Natural Products as Enzyme Inhibitors

Vijay L. Maheshwari,Ravindra H. Patil
Natural Products as Enzyme Inhibitors Book PDF

Author : Vijay L. Maheshwari,Ravindra H. Patil
Publisher : Springer Nature
Page : 287 pages
File Size : 50,5 Mb
Release : 2022-05-03
Category : Medical
ISBN : 9789811909320

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Natural Products as Enzyme Inhibitors by Vijay L. Maheshwari,Ravindra H. Patil Pdf

This book provides an overview of the latest developments and future challenges in enzyme inhibitor research. It discusses the general enzyme inhibitory principles and mechanisms in enzyme activity regulation and application of enzyme inhibitors in different areas and sectors. The major areas of applications of enzyme inhibitors covered in this book are human health management, agriculture, food processing and research, which leads to drug discovery or enzyme activity mechanisms. The book also identifies the gaps in the existing knowledge and opens up new research ideas in this important area. Currently, most enzyme inhibitors are reported to inhibit various classes of enzymes. These enzyme inhibitors are the focus of the scientific community because they may answer an increasing array of questions in the research area of biological sciences, including biochemistry, medicine, physiology, pharmacy, agriculture, ecology etc. It also serves as a useful tool in the study of enzyme structures and reaction mechanisms and in the development of technologies in agriculture, food processing, and health management. Chapters in this book cover topics such as plant-derived inhibitors of serine proteases, pancreatic lipase (PL) inhibitors from indigenous medicinal plants, amylase inhibitors and their applications in agriculture and food processing industries and advances in silico techniques used in the study of enzyme inhibitors. The book will serve as a valuable resource for students and researchers in Life Sciences, agriculture, medicine, food processing, and allied industries.

Drug Discovery and Evaluation: Safety and Pharmacokinetic Assays

H. Gerhard Vogel,Jochen Maas,Franz J. Hock,Dieter Mayer
Drug Discovery and Evaluation Safety and Pharmacokinetic Assays Book PDF

Author : H. Gerhard Vogel,Jochen Maas,Franz J. Hock,Dieter Mayer
Publisher : Springer
Page : 0 pages
File Size : 42,6 Mb
Release : 2013-02-27
Category : Medical
ISBN : 3642252397

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Drug Discovery and Evaluation: Safety and Pharmacokinetic Assays by H. Gerhard Vogel,Jochen Maas,Franz J. Hock,Dieter Mayer Pdf

-A landmark in the continuously changing world of drugs -Essential reading for scientists and managers in the pharmaceutical industry involved in drug finding, drug development and decision making in the development process -Of use for government institutions and committees working on official guidelines for drug evaluation worldwide

Evaluation of Enzyme Inhibitors in Drug Discovery

Robert Allen Copeland
Evaluation of Enzyme Inhibitors in Drug Discovery Book PDF

Author : Robert Allen Copeland
Publisher : Wiley-Interscience
Page : 310 pages
File Size : 46,5 Mb
Release : 2005-03-28
Category : Medical
ISBN : UVA:X004878940

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Evaluation of Enzyme Inhibitors in Drug Discovery by Robert Allen Copeland Pdf

Most enzymology textbooks, including his own, address biochemists and other researchers, says Copeland, a researcher in enzymology and mechanistic pharmacology at a large pharmaceutical corporation. Here he provides chemists and pharmacologists with key information to answer such questions as what opportunities for inhibitor interactions with enzym.

Computation in BioInformatics

S. Balamurugan,Anand T. Krishnan,Dinesh Goyal,Balakumar Chandrasekaran,Boomi Pandi
Computation in BioInformatics Book PDF

Author : S. Balamurugan,Anand T. Krishnan,Dinesh Goyal,Balakumar Chandrasekaran,Boomi Pandi
Publisher : John Wiley & Sons
Page : 354 pages
File Size : 45,9 Mb
Release : 2021-10-19
Category : Computers
ISBN : 9781119654711

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Computation in BioInformatics by S. Balamurugan,Anand T. Krishnan,Dinesh Goyal,Balakumar Chandrasekaran,Boomi Pandi Pdf

COMPUTATION IN BIOINFORMATICS Bioinformatics is a platform between the biology and information technology and this book provides readers with an understanding of the use of bioinformatics tools in new drug design. The discovery of new solutions to pandemics is facilitated through the use of promising bioinformatics techniques and integrated approaches. This book covers a broad spectrum of the bioinformatics field, starting with the basic principles, concepts, and application areas. Also covered is the role of bioinformatics in drug design and discovery, including aspects of molecular modeling. Some of the chapters provide detailed information on bioinformatics related topics, such as silicon design, protein modeling, DNA microarray analysis, DNA-RNA barcoding, and gene sequencing, all of which are currently needed in the industry. Also included are specialized topics, such as bioinformatics in cancer detection, genomics, and proteomics. Moreover, a few chapters explain highly advanced topics, like machine learning and covalent approaches to drug design and discovery, all of which are significant in pharma and biotech research and development. Audience Researchers and engineers in computation biology, information technology, bioinformatics, drug design, biotechnology, pharmaceutical sciences.