Molecular Aspects of Oxidative Drug Metabolizing Enzymes

Molecular Aspects of Oxidative Drug Metabolizing Enzymes PDF

Author: Emel Arinc

Publisher: Springer Science & Business Media

Published: 2013-06-29

Total Pages: 615

ISBN-13: 3642795285

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Presented here are recent advances in biochemical, toxicological, and regulatory aspects of oxidative drug metabolizing enzymes. Mainly cytochrome P450-dependent and flavin-containing monooxygenases (FMO) are covered. Moreover, the book deals with genotoxicity studies and toxicological interactions of environmental chemicals and mechanisms of mutagenicity and tumor formation. The construction of genetically engineered mammalian cells for the production of a specific P450 isozyme and the application of these cell lines in drug metabolism, mutagenicity and toxicity studies are described in detail. Further, insight is provided into how a number of aquatic species cope with pollutants and their genotoxicity.

Chemistry and Molecular Aspects of Drug Design and Action

Chemistry and Molecular Aspects of Drug Design and Action PDF

Author: E. A. Rekka

Publisher: CRC Press

Published: 2008-04-28

Total Pages: 384

ISBN-13: 1420008277

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An ever-increasing demand for better drugs, elevated safety standards, and economic considerations have all led to a dramatic paradigm shift in the way that drugs are being discovered and developed. Known as rational drug design, this contemporary process is defined by three main steps: the discovery of lead compounds, surgical manipulation to deve

Enzyme Kinetics in Drug Metabolism

Enzyme Kinetics in Drug Metabolism PDF

Author: Swati Nagar

Publisher:

Published: 2014

Total Pages: 538

ISBN-13: 9781627037587

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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.

Drug Metabolism and Transport

Drug Metabolism and Transport PDF

Author: Lawrence H. Lash

Publisher: Springer Science & Business Media

Published: 2008-02-06

Total Pages: 390

ISBN-13: 1592598323

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A compendium of proven experimental approaches and strategies for studying the bioactivation, detoxification, tissue distribution, and elimination of xenobiotics in the metabolism and/or transport of various chemicals. The authors address several of the major drug metabolizing systems, including the cytochrome P450 family, flavin-containing monooxygenases, glutathione, S-transferase, glucuronidation, N-acetylation, and sulfotransferases. Additional chapters present novel approaches to the study of: signaling pathways in the regulation of drug metabolism enzymes, how the modulation of thiols and other low molecular-weight cofactors can alter drug metabolism, and how modulation of drug metabolism pathways can influence antiviral therapy.

Enzyme Kinetics in Drug Metabolism

Enzyme Kinetics in Drug Metabolism PDF

Author: Swati Nagar

Publisher: Humana

Published: 2014-02-13

Total Pages: 0

ISBN-13: 9781627037570

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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.

Drug Metabolism

Drug Metabolism PDF

Author: Jack P. Uetrecht

Publisher: CRC Press

Published: 2020-09-30

Total Pages: 179

ISBN-13: 9780367453022

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In order to understand drug metabolism at its most fundamental level, pharmaceutical scientists must be able to analyze drug compound structure and predict possible metabolic pathways in order to avoid the risk of adverse reactions that lead to the withdrawal of a drug from the market. This title is a comprehensive guide for recognizing the chemical underpinnings of drug metabolism. While there are numerous resources available to medicinal chemists for understanding drug structure, and to pharmacologists for discerning drug metabolism from a biological standpoint, no resource currently exists that links the chemical and biological aspects in language accessible to both-making it challenging for both groups to fully comprehend how a drug is metabolized, as well as the potential effects of the metabolites. Drug Metabolism: Chemical and Enzymatic Aspects provides extensive material to help understand drug metabolism within a biological context, and for predicting and mitigating adverse drug reactions.

Transporters and Drug-Metabolizing Enzymes in Drug Toxicity

Transporters and Drug-Metabolizing Enzymes in Drug Toxicity PDF

Author: Albert P. Li

Publisher: John Wiley & Sons

Published: 2021-07-27

Total Pages: 530

ISBN-13: 1119170842

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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.

Principles of Clinical Pharmacology

Principles of Clinical Pharmacology PDF

Author: Arthur J. Atkinson Jr.

Publisher: Elsevier

Published: 2011-04-28

Total Pages: 567

ISBN-13: 0080466427

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This revised second edition covers the pharmacologic principles underlying the individualization of patient therapy and contemporary drug development, focusing on the fundamentals that underlie the clinical use and contemporary development of pharmaceuticals. Authors drawn from academia, the pharmaceutical industry and government agencies cover the spectrum of material, including pharmacokinetic practice questions, covered by the basic science section of the certifying examination offered by the American Board of Clinical Pharmacology. This unique reference is recommended by the Board as a study text and includes modules on drug discovery and development to assist students as well as practicing pharmacologists. Unique breadth of coverage ranging from drug discovery and development to individualization and quality assessment of drug therapy Unusual cohesive of presentation that stems from author participation in an ongoing popular NIH course Instructive linkage of pharmacokinetic theory and applications with provision of sample problems for self-study Wide-ranging perspective of authors drawn from the ranks of Federal agencies, academia and the pharmaceutical industry Expanded coverage of pharmacogenetics Expanded coverage of drug transporters and their role in interactions Inclusion of new material on enzyme induction mechanisms in chapters on drug metabolism and drug interactions A new chapter on drug discovery that focuses on oncologic agents Inclusion of therapeutic antibodies in chapter on biotechnology products

ADME-Enabling Technologies in Drug Design and Development

ADME-Enabling Technologies in Drug Design and Development PDF

Author: Donglu Zhang

Publisher: John Wiley & Sons

Published: 2012-04-13

Total Pages: 622

ISBN-13: 1118180763

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A comprehensive guide to cutting-edge tools in ADME research The last decade has seen tremendous progress in the development of analytical techniques such as mass spectrometry and molecular biology tools, resulting in important advances in drug discovery, particularly in the area of absorption, distribution, metabolism, and excretion (ADME). ADME-Enabling Technologies in Drug Design and Development focuses on the current state of the art in the field, presenting a comprehensive review of the latest tools for generating ADME data in drug discovery. It examines the broadest possible range of available technologies, giving readers the information they need to choose the right tool for a given application, a key requisite for obtaining favorable results in a timely fashion for regulatory filings. With over thirty contributed chapters by an international team of experts, the book provides: A thorough examination of current tools, covering both electronic/mechanical technologies and biologically based ones Coverage of applications for each technology, including key parameters, optimal conditions for intended results, protocols, and case studies Detailed discussion of emerging tools and techniques, from stem cells and genetically modified animal models to imaging technologies Numerous figures and diagrams throughout the text Scientists and researchers in drug metabolism, pharmacology, medicinal chemistry, pharmaceutics, toxicology, and bioanalytical science will find ADME-Enabling Technologies in Drug Design and Development an invaluable guide to the entire drug development process, from discovery to regulatory issues.