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Author: Patrick M. Dansette
Publisher: MDPI
ISBN: 3036502564
Category : Science
Languages : en
Pages : 286
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Book Description
This book, "Cytochromes P450: Drug Metabolism, Bioactivation and Biodiversity", presents five papers on human cytochrome P450 (CYP) and P450 reductase, three reviews on the role of CYPs in humans and their use as biomarkers, six papers on CYPs in microorganisms, and one study on CYP in insects. The first paper reports the in silico modeling of human CYP3A4 access channels. The second uses structural methods to explain the mechanism-based inactivation of CYP3A4 by mibefradil, 6,7-dihydroxy-bergamottin, and azamulin. The third article compares electron transfer in CYP2C9 and CYP2C19 using structural and biochemical methods, and the fourth uses kinetic methods to study electron transfer to CYP2C8 allelic mutants. The fifth article characterizes electron transfer between the reductase and CYP using in silico and in vitro methods, focusing on the conformations of the reductase. Then, two reviews describe clinical implications in cardiology and oncology and the role of fatty acid metabolism in cardiology and skin diseases. The second review is on the potential use of circulating extracellular vesicles as biomarkers. Five papers analyze the CYPomes of diverse microorganisms: the Bacillus genus, Mycobacteria, the fungi Tremellomycetes, Cyanobacteria, and Streptomyces. The sixth focuses on a specific Mycobacterium CYP, CYP128, and its importance in M. tuberculosis. The subject of the last paper is CYP in Sogatella furcifera, a plant pest, and its resistance to the insecticide sulfoxaflor.
Author: Patrick M. Dansette
Publisher: MDPI
ISBN: 3036502564
Category : Science
Languages : en
Pages : 286
Get Book Here
Book Description
This book, "Cytochromes P450: Drug Metabolism, Bioactivation and Biodiversity", presents five papers on human cytochrome P450 (CYP) and P450 reductase, three reviews on the role of CYPs in humans and their use as biomarkers, six papers on CYPs in microorganisms, and one study on CYP in insects. The first paper reports the in silico modeling of human CYP3A4 access channels. The second uses structural methods to explain the mechanism-based inactivation of CYP3A4 by mibefradil, 6,7-dihydroxy-bergamottin, and azamulin. The third article compares electron transfer in CYP2C9 and CYP2C19 using structural and biochemical methods, and the fourth uses kinetic methods to study electron transfer to CYP2C8 allelic mutants. The fifth article characterizes electron transfer between the reductase and CYP using in silico and in vitro methods, focusing on the conformations of the reductase. Then, two reviews describe clinical implications in cardiology and oncology and the role of fatty acid metabolism in cardiology and skin diseases. The second review is on the potential use of circulating extracellular vesicles as biomarkers. Five papers analyze the CYPomes of diverse microorganisms: the Bacillus genus, Mycobacteria, the fungi Tremellomycetes, Cyanobacteria, and Streptomyces. The sixth focuses on a specific Mycobacterium CYP, CYP128, and its importance in M. tuberculosis. The subject of the last paper is CYP in Sogatella furcifera, a plant pest, and its resistance to the insecticide sulfoxaflor.
Author: Amit S. Kalgutkar
Publisher: John Wiley & Sons
ISBN: 352765576X
Category : Medical
Languages : en
Pages : 445
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Book Description
Closing a gap in the scientifi c literature, this first comprehensive introduction to the topic is based on current best practice in one of the largest pharmaceutical companies worldwide. The first chapters trace the development of our understanding of drug metabolite toxicity, covering basic concepts and techniques in the process, while the second part details chemical toxicophores that are prone to reactive metabolite formation. This section also reviews the various drug-metabolizing enzymes that can participate in catalyzing reactive metabolite formation, including a discussion of the structure-toxicity relationships for drugs. Two chapters are dedicated to the currently hot topics of herbal constituents and IADRs. The next part covers current strategies and approaches to evaluate the reactive metabolite potential of new drug candidates, both by predictive and by bioanalytical methods. There then follows an in-depth analysis of the toxicological potential of the top 200 prescription drugs, illustrating the power and the limits of the toxicophore concept, backed by numerous case studies. Finally, a risk-benefi t approach to managing the toxicity risk of reactive metabolite-prone drugs is presented. Since the authors carefully develop the knowledge needed, from fundamental considerations to current industry standards, no degree in pharmacology is required to read this book, making it perfect for medicinal chemists without in-depth pharmacology training.
Author: Alan Talevi
Publisher: Springer
ISBN: 3319995936
Category : Medical
Languages : en
Pages : 364
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Book Description
Absorption, Distribution, Metabolism and Excretion (ADME) processes and their relationship with the design of dosage forms and the success of pharmacotherapy form the basis of this upper level undergraduate/graduate textbook. As an introduction oriented to pharmacy students, it is also written for scientist from different fields outside of pharmaceutics. (e.g. material scientist, material engineers, medicinal chemists) who might be working in a positions in pharmaceutical companies or whose work might benefit from basic training in the ADME concepts and some biological background. Pedagogical features such as objectives, keywords, discussion questions, summaries and case studies add valuable teaching tools. This book will provide not only general knowledge on ADME processes but also an updated insight on some hot topics such as drug transporters, multi-drug resistance related to pharmacokinetic phenomena, last generation pharmaceutical carriers (nanopharmaceuticals), in vitro and in vivo bioequivalence studies, biopharmaceuticals, pharmacogenomics, drug-drug and food-drug interactions, and in silico and in vitro prediction of ADME properties. In comparison with other similar textbooks, around half of the volume would be focused on the relationship between expanding scientific fields and ADME processes. Each of these burgeoning fields has a separate chapter in the second part of the volume, and was written with leading experts on the correspondent topic, including scientists and academics from USA and UK (Duquesne University School of Pharmacy, Indiana University School of Medicine, University of Utah College of Pharmacy, University of Maryland, University of Bath). Additionally, each of the initial chapters dealing with the generalities of drug absorption, distribution, metabolism and excretion would include relevant, classic examples related to each topic with appropriate illustrations (e.g. importance of active absorption of levodopa, implications in levodopa administration, drug drug interactions and food drug interactions emerging from the active uptake; intoxication with paracetamol as a result of glutathione depletion, CYP induction and its relationship with acute liver failure caused by paracetamol, etc). ADME Processes and Pharmaceutical Sciences is written as a core textbook for ADME processes, pharmacy, pharmacokinetics, drug delivery, biopharmaceutics, drug disposition, drug design and medicinal chemistry courses.
Author: Chang-Hwei Chen
Publisher: Springer Science & Business Media
ISBN: 1461410495
Category : Medical
Languages : en
Pages : 185
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Book Description
Humans are exposed to foreign compounds such as drugs, household products and environmental chemicals by swallowing or breathing. Also, food is considered a foreign compound. Such foreign compounds can be non-essential and non-functional to life, and commonly are referred to as xenobiotics. Some xenobiotics are not toxic; however, many of them are potentially toxic or become toxic after conversion to metabolic intermediates. A considerable number of foreign compounds belong to non-polar, lipophilic substances. Lipophilic compounds are not soluble in water. Metabolic conversion of lipophilic foreign compounds to facilitate their removal from the body is essentially carried out by biochemical reactions catalyzed by two classes of metabolizing enzymes, namely, activation enzymes and detoxification enzymes. Activation enzyme-catalyzed functionalization reaction introduces a functional group to a lipophilic compound. Functionalization modifies many foreign compounds to form reactive intermediates capable of interacting with cellular components (proteins, DNA and lipids), leading to a variety of conditions for diseases. Functionalized compounds are further metabolized through detoxification enzyme-catalyzed reactions, which result in an increase in the solubility of parent compounds and an inactivation of metabolic intermediates, thus facilitating their excretion from the body. To minimize the exposure of potentially toxic metabolic intermediates, it is essential to keep them at a minimum level. Extensive investigations have revealed that foreign compound-metabolizing enzymes exhibit genetic polymorphisms. Variations in their activities can produce different results as to the susceptibility to potential toxic effects. Moreover, the expressions of activation enzymes and detoxification enzymes are inducible. A number of chemical compounds are capable of acting as modulators for these two classes of enzymes. These findings have lead to the proposal of modulating metabolizing enzymes as a useful approach for human health benefits. Importantly, many of these chemical compounds are present in human daily diets. There are many advances that have been made in the past decades towards the understanding of functions and implications of activation enzymes and detoxification enzymes. An organized, concise overview is needed for the readers who are initially exposed to this important subject, particularly for students and researchers in the areas of biomedical sciences, biochemistry, nutrition, pharmacology and chemistry. This book is intended to serve this purpose as an introduction to the subject. Furthermore, major topics in the book, excluding catalytic reactions and structural properties, may have interest to other readers who have knowledge of basic sciences and understanding enzyme related information. The book discusses subjects associated with foreign compound metabolizing enzymes with emphasis on biochemical aspects, including lipophilic foreign compounds, catalytic properties, reactive intermediates, biomedical and biochemical effects, genetic polymorphisms, enzyme inducibility, enzyme modulation for health benefits, dietary related enzyme modulators, and structural characteristics of enzyme inducers.
Author: Bernard Testa
Publisher:
ISBN:
Category :
Languages : en
Pages :
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Book Description
Offering a conceptual and factual presentation of the metabolism of drugs and other xenobiotics, these two volumes distinctly focus on the biochemistry, with an emphasis on xenobiotic-metabolizing enzymes, their reactions and regulations. The first volume is divided into three parts. Part One begins by introducing xenobiotics in the broad context of physiological metabolism, and continues with an overview of the processes of drug disposition and metabolism. It then goes on to summarize the macroscopic and microscopic locations of drug ...
Author: Ian R. Phillips
Publisher: Humana Press
ISBN: 9781627033206
Category : Science
Languages : en
Pages : 0
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Book Description
Cytochromes P450 (CYPs) comprise a large superfamily of proteins that are of central importance in the detoxification or activation of a tremendous number of natural and synthetic hydrophobic xenobiotics, including many therapeutic drugs, chemical carcinogens and environmental pollutants. CYPs are important in mediating interactions between an organism and its chemical environment and in the regulation of physiological processes. Cytochrome P450 Protocols, Third Edition focuses on high-throughput methods for the simultaneous analysis of multiple CYPs, substrates or ligands. Although the emphasis is on CYPs of mammalian origin, it reflects an increasing interest in CYPs of bacterial species. Also included are chapters on cytochrome P450 reductase (the redox partner of CYPs) and the flavin-containing monooxygenases (FMOs), and metabolomic and lipidomic approaches for identification of endogenous substrates of CYPs (‘de-orphanizing’ CYP substrates). Written in the successful Methods in Molecular BiologyTM series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and notes on troubleshooting and avoiding known pitfalls. Authoritative and easily accessible, Cytochrome P450 Protocols, Third Edition provides a wide range of techniques accessible to researchers in fields as diverse as biochemistry, molecular biology, pharmacology, toxicology, environmental biology and genetics.
Author: Paul R. Ortiz de Montellano
Publisher: Springer Science & Business Media
ISBN: 0387274472
Category : Medical
Languages : en
Pages : 702
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Book Description
Cytochrome P450: Structure, Mechanism, and Biochemistry, third edition is a revision of a review that summarizes the current state of research in the field of drug metabolism. The emphasis is on structure, mechanism, biochemistry, and regulation. Coverage is interdisciplinary, ranging from bioinorganic chemistry of cytochrome P450 to its relevance in human medicine. Each chapter provides an in-depth review of a given topic, but concentrates on advances of the last 10 years.
Author: Thomas Ternes
Publisher: IWA Publishing
ISBN: 1843390930
Category : Science
Languages : en
Pages : 475
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Book Description
The observed concentrations of pharmaceuticals and personal care products (PPCPs) in raw wastewater confirm that municipal wastewater represents the main disposal pathway for the PPCPs consumed in households, hospitals and industry. In sewage treatment plant effluents most PPCPs are still present, since many of these polar and persistent compounds are being removed only partially or, in some cases, not at all. Treated wastewater therefore represents an important point source for PPCPs into the environment. After passing a sewage treatment plant the treated wastewater is mostly discharged into rivers and streams or sometimes used to irrigate fields. If drinking water is produced using resources containing a substantial proportion of treated wastewater (e.g. from river water downstream of communities) the water cycle is closed and indirect potable reuse occurs. Human Pharmaceuticals, Hormones and Fragrances provides an overview of the occurrence, analytics, removal and environmental risk of pharmaceuticals and personal care products in wastewater, surface water and drinking water. The book covers all aspects of the fate and removal of PPCPs in the whole water cycle: consumption and occurrence, analytical methods, the legal background, environmental risk assessment, human and animal toxicology, source control options, wastewater and drinking water treatment as well as indirect reuse. The book presents a summary of the results obtained during the EU project "Poseidon", combined with further expert knowledge on the field, and is written at a level appropriate for professionals involved in management of water resource quality. Professionals in the field including decision makers, engineers and scientists, as well as students entering the field, will find this an invaluable source of information. First comprehensive study on the assessment, fate and removal of pharmaceuticals and personal care products in wastewater and drinking water treatment. Emphasises the importance of micropollutants in the water cycle, provides methods for quantifying their fate and technologies for their removal.
Author: Anne E. Osbourn
Publisher: Springer Science & Business Media
ISBN: 0387854983
Category : Science
Languages : en
Pages : 588
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Book Description
Plants produce a huge array of natural products (secondary metabolites). These compounds have important ecological functions, providing protection against attack by herbivores and microbes and serving as attractants for pollinators and seed-dispersing agents. They may also contribute to competition and invasiveness by suppressing the growth of neighboring plant species (a phenomenon known as allelopathy). Humans exploit natural products as sources of drugs, flavoring agents, fragrances and for a wide range of other applications. Rapid progress has been made in recent years in understanding natural product synthesis, regulation and function and the evolution of metabolic diversity. It is timely to bring this information together with contemporary advances in chemistry, plant biology, ecology, agronomy and human health to provide a comprehensive guide to plant-derived natural products. Plant-derived natural products: synthesis, function and application provides an informative and accessible overview of the different facets of the field, ranging from an introduction to the different classes of natural products through developments in natural product chemistry and biology to ecological interactions and the significance of plant-derived natural products for humans. In the final section of the book a series of chapters on new trends covers metabolic engineering, genome-wide approaches, the metabolic consequences of genetic modification, developments in traditional medicines and nutraceuticals, natural products as leads for drug discovery and novel non-food crops.
Author: Patrick M. Dansette
Publisher:
ISBN: 9783036502571
Category :
Languages : en
Pages : 286
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Book Description
This book, "Cytochromes P450: Drug Metabolism, Bioactivation and Biodiversity", presents five papers on human cytochrome P450 (CYP) and P450 reductase, three reviews on the role of CYPs in humans and their use as biomarkers, six papers on CYPs in microorganisms, and one study on CYP in insects. The first paper reports the in silico modeling of human CYP3A4 access channels. The second uses structural methods to explain the mechanism-based inactivation of CYP3A4 by mibefradil, 6,7-dihydroxy-bergamottin, and azamulin. The third article compares electron transfer in CYP2C9 and CYP2C19 using structural and biochemical methods, and the fourth uses kinetic methods to study electron transfer to CYP2C8 allelic mutants. The fifth article characterizes electron transfer between the reductase and CYP using in silico and in vitro methods, focusing on the conformations of the reductase. Then, two reviews describe clinical implications in cardiology and oncology and the role of fatty acid metabolism in cardiology and skin diseases. The second review is on the potential use of circulating extracellular vesicles as biomarkers. Five papers analyze the CYPomes of diverse microorganisms: the Bacillus genus, Mycobacteria, the fungi Tremellomycetes, Cyanobacteria, and Streptomyces. The sixth focuses on a specific Mycobacterium CYP, CYP128, and its importance in M. tuberculosis. The subject of the last paper is CYP in Sogatella furcifera, a plant pest, and its resistance to the insecticide sulfoxaflor.
