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Author: Albert Lauwers
Publisher: CRC Press
ISBN: 9780824793753
Category : Medical
Languages : en
Pages : 408
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Book Description
This well-integrated, one-of-a-kind resource offers comprehensive, interdisciplinary analyses of the entire pharmaceutical enzyme field-from molecular biology to clinical pharmacology. Highlights practical, previously unpublished information, immediately useful in industry and academic institutions! Emphasizing pharmacology and clinical impact, Pharmaceutical Enzymes discusses robust methods of measurement and evaluation reviews current knowledge on the bioavailability of pharmaceutical enzymes presents different chemical approaches to tailoring enzymes for the improvement of therapeutic effectiveness provides a step-by-step approach to molecular modeling describes recently introduced pharmaceutical products, including glucocerebrosidase for the treatment of Gaucher's disease and deoxyribonuclease for cystic fibrosis furnishes unique laboratory guidelines for the testing and quality control of pharmaceutical enzymes and more! With over 1200 bibliographic citations, figures, and tables, Pharmaceutical Enzymes is an indispensable, day-to-day reference for pharmacologists, enzymologists, microbiologists, organic and medicinal chemists and biochemists, biophysicists, biotechnologists, molecular and membrane biologists, immunologists, physiologists, pharmaceutical development managers, regulatory affairs personnel, and graduate-level students in these disciplines.
Author: Albert Lauwers
Publisher: CRC Press
ISBN: 9780824793753
Category : Medical
Languages : en
Pages : 408
Get Book Here
Book Description
This well-integrated, one-of-a-kind resource offers comprehensive, interdisciplinary analyses of the entire pharmaceutical enzyme field-from molecular biology to clinical pharmacology. Highlights practical, previously unpublished information, immediately useful in industry and academic institutions! Emphasizing pharmacology and clinical impact, Pharmaceutical Enzymes discusses robust methods of measurement and evaluation reviews current knowledge on the bioavailability of pharmaceutical enzymes presents different chemical approaches to tailoring enzymes for the improvement of therapeutic effectiveness provides a step-by-step approach to molecular modeling describes recently introduced pharmaceutical products, including glucocerebrosidase for the treatment of Gaucher's disease and deoxyribonuclease for cystic fibrosis furnishes unique laboratory guidelines for the testing and quality control of pharmaceutical enzymes and more! With over 1200 bibliographic citations, figures, and tables, Pharmaceutical Enzymes is an indispensable, day-to-day reference for pharmacologists, enzymologists, microbiologists, organic and medicinal chemists and biochemists, biophysicists, biotechnologists, molecular and membrane biologists, immunologists, physiologists, pharmaceutical development managers, regulatory affairs personnel, and graduate-level students in these disciplines.
Author: Robert A. Copeland
Publisher: John Wiley & Sons
ISBN: 0471723266
Category : Science
Languages : en
Pages : 295
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Book Description
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.
Author: Albert P. Li
Publisher: John Wiley & Sons
ISBN: 1119170842
Category : Medical
Languages : en
Pages : 530
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Book Description
TRANSPORTERS AND DRUG-METABOLIZING ENZYMES IN DRUG TOXICITY Explore up-to-date coverage on the interaction between drug metabolism enzymes, transporters, and drug toxicity with this leading resources Transporters and Drug-Metabolizing Enzymes in Drug Toxicity delivers a comprehensive and updated review of the relationship between drug metabolism, transporters, and toxicity, providing insights into a major challenge in drug development – accurate assessment of human drug toxicity. Combining two disciplines frequently considered independently of one another, the book combines drug metabolism and toxicology with a focus on the role of biotransformation on drug toxicity and as a major factor for species and individual differences. Mechanism and species differences in drug metabolizing enzymes and transporters are discussed, as are the methods used to investigate the role of drug metabolizing enzymes and transporters in drug toxicity. Finally, the distinguished authors describe promising new experimental approaches to accurately assessing human drug toxicity via the consideration of human-specific drug metabolism in toxicity assays. In addition to topics as diverse as extended clearance models, experimental approaches for the estimation of DILI potential of drug candidates and roles of transporters in renal drug toxicity, readers will also enjoy the inclusion of such subjects as: A thorough overview of and introduction to drug metabolism and transporters and drug toxicity An exploration of drug metabolism enzymes and transporter activities as risk factors of marketed drugs associated with drug-induced fatalities A discussion of human-based in vitro experimental models for the evaluation of metabolism-dependent drug toxicity A treatment of mechanism-based experimental models for the evaluation of BSEP inhibition and DILI An examination of transporters and cochlea toxicity Perfect for scientists, students, and practitioners with interests in metabolism, toxicology, and drug development in the pharmaceutical industry, Transporters and Drug-Metabolizing Enzymes in Drug Toxicity will also earn a place in the libraries of medicinal chemists, pharmacologists, biochemists, toxicologists, and regulators in the pharmaceutical and health industries.
Author: H. John Smith
Publisher: CRC Press
ISBN: 0203414586
Category : Medical
Languages : en
Pages : 325
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Book Description
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
Author: Costas Ioannides
Publisher: John Wiley & Sons
ISBN:
Category : Medical
Languages : en
Pages : 600
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Book Description
This reference work focuses on the enzyme systems that participate in the metabolism of chemicals and other xenobiotics, with emphasis being placed on drug metabolism. Each chapter focuses on a specific enzyme system.
Author: Shuguang Ma
Publisher: Elsevier Science
ISBN: 0128200189
Category : Science
Languages : en
Pages : 708
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Book Description
Identification and Quantification of Drugs, Metabolites, Drug Metabolizing Enzymes, and Transporters, Second Edition, is completely updated to provide an overview of the last decade's numerous advances in analytical technologies for detection and quantification of drugs, metabolites, and biomarkers. This new edition goes beyond LC-MS and features all-new chapters on how to evaluate drug absorption, distribution, metabolism, and excretion, potential for hepatic and renal toxicity, immunogenicity of biotherapeutics and translational tools for predicting human dosage, safety and efficacy of small molecules and biologics. This book will be an important handbook and desk reference for pharmacologists, toxicologists, clinical scientists, and students interested in the fields of pharmacology, biochemistry, and drug metabolism.
Author: Pavel Anzenbacher
Publisher: John Wiley & Sons
ISBN: 352732903X
Category : Medical
Languages : en
Pages : 755
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Book Description
A practice-oriented desktop reference for medical professionals, toxicologists and pharmaceutical researchers, this handbook provides systematic coverage of the metabolic pathways of all major classes of xenobiotics in the human body. The first part comprehensively reviews the main enzyme systems involved in biotransformation and how they are orchestrated in the body, while parts two to four cover the three main classes of xenobiotics: drugs, natural products, environmental pollutants. The part on drugs includes more than 300 substances from five major therapeutic groups (central nervous system, cardiovascular system, cancer, infection, and pain) as well as most drugs of abuse including nicotine, alcohol and "designer" drugs. Selected, well-documented case studies from the most important xenobiotics classes illustrate general principles of metabolism, making this equally useful for teaching courses on pharmacology, drug metabolism or molecular toxicology. Of particular interest, and unique to this volume is the inclusion of a wide range of additional xenobiotic compounds, including food supplements, herbal preparations, and agrochemicals.
Author: Robert A. Copeland
Publisher: John Wiley & Sons
ISBN: 111854028X
Category : Science
Languages : en
Pages : 588
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Book Description
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.
Author: Vladimir P. Torchilin
Publisher: Springer Science & Business Media
ISBN: 3642758215
Category : Science
Languages : en
Pages : 214
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Book Description
The application of immobilized enzymes in medicine is the main objective of this book. The author reviews natural and synthetic carriers for enzyme immobilization, chemistry of enzyme binding, and in-vitro and in-vivo properties of immobilized enzymes. Four chapters are dedicated to clinical use of immobilized enzymes.
Author: Swati Nagar
Publisher: Humana
ISBN: 9781627037570
Category : Medical
Languages : en
Pages : 0
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Book Description
Drug metabolism and transport are very important facets within the discipline of pharmaceutical sciences, with enzyme kinetic concepts utilized regularly in characterizing and modeling the disposition and elimination of drugs. Enzyme Kinetics in Drug Metabolism: Fundamentals and Applications focuses on very practical aspects of applying kinetic principles to drug metabolizing enzymes and transporters. Divided into five convenient sections, topics include the fundamental principles of enzyme kinetics, the kinetics of oxidative and conjugative drug metabolizing enzymes and drug transporters, modeling approaches for both drug metabolizing enzymes and transporters including novel systems biology approaches, understanding of variability both experimental and interindividual (pharmacogenomic), and case studies that provide real life examples of applying these principles. Written in the successful Methods in Molecular Biology series format, chapters include introductions to their respective topics especially suitable for the novice, in some cases step-by-step, readily reproducible protocols, and insights to help with troubleshooting and avoiding known pitfalls with extensive cross referencing to assist in learning. Authoritative and easily accessible, Enzyme Kinetics in Drug Metabolism: Fundamentals and Applications serves as a very practical teaching tool for novice, non-mathematically trained scientists interested in these fundamental concepts and as an aid for their supervisors in teaching these principles.
