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Titlebook: Cytochrome P450; In Vitro Methods and Zhengyin Yan,Gary W. Caldwell Book 2021 The Editor(s) (if applicable) and The Author(s), under exclus

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书目名称Cytochrome P450
副标题In Vitro Methods and
编辑Zhengyin Yan,Gary W. Caldwell
视频videohttp://file.papertrans.cn/243/242609/242609.mp4
概述Includes cutting-edge techniques.Provides the kind of detail necessary for reproducible results.Contains key implementation advice from the experts
丛书名称Methods in Pharmacology and Toxicology
图书封面Titlebook: Cytochrome P450; In Vitro Methods and Zhengyin Yan,Gary W. Caldwell Book 2021 The Editor(s) (if applicable) and The Author(s), under exclus
描述This collection explores detailed experimental protocols necessary for setting up a variety of .in vitro. cytochrome P450 (CYP) assays that are vital in selecting drug candidates in a drug discovery pipeline. Major factors affecting drug metabolism include CYP expression levels, kinetic parameters for individual CYP enzymes, CYP inhibition and induction, time-dependent inhibition (TDI), CYP stability, non-CYP stability, UDP-glucuronosyltransferases (UGT) stability, excretion mechanisms, and drug-drug interactions (DDI), all addressed in this volume. Written for the .Methods in Pharmacology and Toxicology. series, chapters include helpful background information on the .in vitro. assay, a list of all the materials, reagents, and equipment necessary to carry out the assay, a step-by-step protocol, notes containing common and unexpected experimental problems in the assay, as well as references containing important supplementary reading. .Authoritativeand practical, .Cytochrome P450: In Vitro Methods and Protocols. serves as a key guide for researchers in the area of discovery and development of new medicines. .
出版日期Book 2021
关键词Drug candidates; Therapeutic targets; CYP enzymes; Drug metabolites; Drug discovery and development; Meta
版次1
doihttps://doi.org/10.1007/978-1-0716-1542-3
isbn_softcover978-1-0716-1544-7
isbn_ebook978-1-0716-1542-3Series ISSN 1557-2153 Series E-ISSN 1940-6053
issn_series 1557-2153
copyrightThe Editor(s) (if applicable) and The Author(s), under exclusive license to Springer Science+Busines
The information of publication is updating

书目名称Cytochrome P450影响因子(影响力)




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Quantitative Determination of Cytochrome P450 Using LC-MS/MS,reclinical, and individual data to population pharmacokinetics. For example, quantitative proteomics data can be utilized for in vitro-in vivo extrapolation (IVIVE), in vitro model validation, and determination of interindividual and species differences. Here, we describe a detailed methodology for
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Spectral Quantitation of Total Cytochrome P450 in Microsomes Using a Single-Beam Spectrophotometer,obtaining the difference spectrum of the reduced form of cytochrome P450 subtracted from the spectrum of the carbon monoxide bound, reduced form. The resulting spectrum can then be analyzed to determine the difference between the absorbance at 450 nm and an isosbestic value (usually at 490 nm). The
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Cytochrome P450 Enzyme Kinetics: Km and Vmax Determinations Using Metabolite Formation and Substratst important drug metabolizing enzymes (DMEs), which are responsible for converting structurally diverse exogenous xenobiotics to more water-soluble form to facilitate excretion from the body. By understanding the basic principles of kinetic, function, and mechanism of CYP enzymes will help to deter
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Cytochrome P450 Inhibition Assay Using Human Liver Microsomes,y and development of new drugs, metabolic inhibitor drug interactions are important to consider since they can produce adverse effects. A robust LC/MS-based cytochrome P450 (CYP) inhibition assay using human liver microsomes has been fully developed and validated for major human CYPs, which could pr
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Evaluation of Time-Dependent Cytochrome P450 Inhibition Using the Area Under the Curve Shift Methodor drug–drug interactions (DDIs). DDIs occur when one drug affects the metabolism of a coadministered drug. This changes the exposure and clearance of a coadministered drug. The consequences are a risk of therapeutic efficacy of a drug to severe adverse drug reactions, leading to death. Thus, it is
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Assessing Cytochrome P450 Time-Dependent Inhibition (IC50 Shift Assay) Using Both Diluted and Non-D is usually studied by measuring the half-maximal inhibitory concentration (IC50) shift of a drug candidate after a 30-min incubation with human liver microsomes (HLMs) in the presence and absence of NADPH. There are two main methods to assess the IC50 shift, dilution method, and non-dilution method
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