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Cytochrome P450

In Vitro Methods and Protocols

  • Book
  • © 2021

Overview

Editors:
  1. Zhengyin Yan

    1. Genentech Inc., South San Francisco, USA

    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  2. Gary W. Caldwell

    1. Blue Bell, USA

    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  • Includes cutting-edge techniques
  • Provides the kind of detail necessary for reproducible results
  • Contains key implementation advice from the experts

Part of the book series: Methods in Pharmacology and Toxicology (MIPT)

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Table of contents (22 protocols)

  1. Front Matter

    Pages i-xi
    Download chapter PDF

  2. Cytochrome P450: In Vitro Methods and Protocols

    • Zhengyin Yan, Gary W. Caldwell
    Pages 1-25

  3. Characteristics of Major Drug Metabolizing Cytochrome P450 Enzymes

    • Kevin M. Johnson, Dian Su, Donglu Zhang
    Pages 27-54

  4. Quantitative Determination of Cytochrome P450 Using LC-MS/MS

    • Ryan H. Takahashi, Brahim Achour, Bhagwat Prasad
    Pages 55-69

  5. Spectral Quantitation of Total Cytochrome P450 in Microsomes Using a Single-Beam Spectrophotometer

    • David M. Stresser
    Pages 71-78

  6. Cytochrome P450 Enzyme Kinetics: Km and Vmax Determinations Using Metabolite Formation and Substrate Depletion Methods

    • Jing Wang
    Pages 79-90

  7. Cytochrome P450 Inhibition Assay Using Human Liver Microsomes

    • Jia Jia
    Pages 91-105

  8. Evaluation of Time-Dependent Cytochrome P450 Inhibition Using the Area Under the Curve Shift Method

    • Julie Huang
    Pages 107-119

  9. Assessing Cytochrome P450 Time-Dependent Inhibition (IC50 Shift Assay) Using Both Diluted and Non-Diluted Methods

    • Yu Wang, Lili Xie, Jing Ni
    Pages 121-139

  10. Cytochrome P450 Gene Regulation: Reporter Assays to Assess Pregnane X Receptor (PXR, NR1I2) Activation

    • Marija Pinne, Judy L. Raucy
    Pages 141-155

  11. Cytochrome P450 Gene Regulation: Reporter Assays to Assess Aryl Hydrocarbon Receptor (HLHE76, AhR) Activation and Antagonism

    • Marija Pinne, Judy L. Raucy
    Pages 157-174

  12. Cytochrome P450 Gene Regulation: Reporter Assays to Assess Direct and Indirect Activation of Constitutive Androstane Receptor (CAR, NR1I3)

    • Marija Pinne, Judy L. Raucy
    Pages 175-192

  13. Determination of In Vitro Cytochrome P450 Induction Potential Using Cryopreserved Human Hepatocytes

    • Susan Wong
    Pages 193-215

  14. Assessing Cytochrome P450 3A (CYP3A) Induction and Suppression Using Primary Human Hepatocyte Spheroids

    • Jing Wang, Eugene Chen
    Pages 217-227

  15. Cytochrome P450-Mediated Metabolic Stability Assay in Liver Microsomes

    • Pasquale Carione
    Pages 229-242

  16. Assessment of Cytochrome P450 Metabolic Clearance Using Hepatocyte Suspension

    • Jingwei Cai, Hadil Shalan
    Pages 243-259

  17. Cytochrome P450 Knock-Out Assay with Nonselective Inhibitors

    • Pasquale Carione, Zhengyin Yan
    Pages 261-275

  18. Differentiation of Cytochrome P450-Mediated from Non-CYP-Mediated Metabolism: Aldehyde Oxidase and Xanthine Oxidoreductase

    • Kirk D. Kozminski, Michael A. Zientek
    Pages 277-289

  19. In Vitro Reaction Phenotyping of Cytochrome P450 Enzymes

    • Susan Wong, Zhengyin Yan
    Pages 291-305

  20. Cytochrome P450-Mediated Drug Bioactivation Assay: An Untargeted High Resolution Accurate Mass LC/MS Assay

    • Kevin M. Johnson
    Pages 307-318
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Keywords

About this book

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. 

Editors and Affiliations

  • Genentech Inc., South San Francisco, USA

    Zhengyin Yan

  • Blue Bell, USA

    Gary W. Caldwell

Bibliographic Information

  • Book Title: Cytochrome P450

  • Book Subtitle: In Vitro Methods and Protocols

  • Editors: Zhengyin Yan, Gary W. Caldwell

  • Series Title: Methods in Pharmacology and Toxicology

  • DOI: https://doi.org/10.1007/978-1-0716-1542-3

  • Publisher: Humana New York, NY

  • eBook Packages: Springer Protocols

  • Copyright Information: The Editor(s) (if applicable) and The Author(s), under exclusive license to Springer Science+Business Media, LLC, part of Springer Nature 2021

  • Hardcover ISBN: 978-1-0716-1541-6Published: 10 July 2021

  • Softcover ISBN: 978-1-0716-1544-7Published: 10 July 2022

  • eBook ISBN: 978-1-0716-1542-3Published: 09 July 2021

  • Series ISSN: 1557-2153

  • Series E-ISSN: 1940-6053

  • Edition Number: 1

  • Number of Pages: XI, 379

  • Number of Illustrations: 54 b/w illustrations, 40 illustrations in colour

  • Topics: Pharmacology/Toxicology, Enzymology, Pharmaceutical Sciences/Technology

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