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Optimization in Drug Discovery

In Vitro Methods

  • Book
  • © 2014

Overview

Editors:
  1. Gary W. Caldwell

    1. CREATe Core Science Technologies, Janssen Research & Development, LLC, Spring House, USA

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    You can also search for this editor in PubMed   Google Scholar

  2. Zhengyin Yan

    1. CREATe Core Science Technologies, Janssen Research & Development, LLC, Spring House, USA

    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  • Provides updated variations on assays as well as numerous new protocols for drug discovery optimization
  • Features readily reproducible methods and protocols that are lab-tested and successful
  • Includes expert tips and key implementation advice

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

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Table of contents (34 protocols)

  1. Screening for P-Glycoprotein (Pgp) Substrates and Inhibitors

    • Qing Wang, Tina M. Sauerwald
    Pages 337-352

  2. In Vitro Characterization of Intestinal Transporter, Breast Cancer Resistance Protein (BCRP)

    • Chris Bode, Li-Bin Li
    Pages 353-367

  3. In Vitro Characterization of Intestinal and Hepatic Transporters: MRP2

    • Ravindra Varma Alluri, Peter Ward, Jeevan R. Kunta, Brian C. Ferslew, Dhiren R. Thakker, Shannon Dallas
    Pages 369-404

  4. In Vitro Characterization of Hepatic Transporters OATP1B1 and OATP1B3

    • Blair Miezeiewski, Allison McLaughlin
    Pages 405-416

  5. In Vitro Characterization of Renal Transporters OAT1, OAT3, and OCT2

    • Ying Wang, Nicole Behler
    Pages 417-429

  6. General Guidelines for Setting Up an In Vitro LC/MS/MS Assay

    • John A. Masucci, Gary W. Caldwell
    Pages 431-443

  7. Metabolite Identification in Drug Discovery

    • Wing W. Lam, Jie Chen, Rongfang Fran Xu, Jose Silva, Heng-Keang Lim
    Pages 445-459

  8. Drug, Lipid, and Acylcarnitine Profiling Using Dried Blood Spot (DBS) Technology in Drug Discovery

    • Wensheng Lang, Jenson Qi, Gary W. Caldwell
    Pages 461-475

  9. In Vitro Trapping and Screening of Reactive Metabolites Using Liquid Chromatography-Mass Spectrometry

    • Zhengyin Yan, Gary W. Caldwell
    Pages 477-488

  10. Quantitative Assessment of Reactive Metabolites

    • Jie Chen, Rongfang Fran Xu, Wing W. Lam, Jose Silva, Heng-Keang Lim
    Pages 489-504

  11. In Vitro Assessment of the Reactivity of Acyl Glucuronides

    • Rongfang Fran Xu, Wing W. Lam, Jie Chen, Michael McMillian, Jose Silva, Heng-Keang Lim
    Pages 505-516

  12. In Vitro Comet Assay for Testing Genotoxicity of Chemicals

    • Haixia Lin, Nan Mei, Mugimane G. Manjanatha
    Pages 517-536

  13. Assessing DNA Damage Using a Reporter Gene System

    • Michael Biss, Wei Xiao
    Pages 537-543

  14. Improved AMES Test for Genotoxicity Assessment of Drugs: Preincubation Assay Using a Low Concentration of Dimethyl Sulfoxide

    • Atsushi Hakura
    Pages 545-559

  15. Methods for Using the Mouse Lymphoma Assay to Screen for Chemical Mutagenicity and Photo-Mutagenicity

    • Nan Mei, Xiaoqing Guo, Martha M. Moore
    Pages 561-592

  16. Back Matter

    Pages 593-597
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Keywords

About this book

Thoroughly revised and updated, Optimization in Drug Discovery: In Vitro Methods, Second Edition presents a wide spectrum of in vitro assays including formulation, plasma binding, absorption and permeability, cytochrome P450 (CYP) and UDP-glucuronosyltransferases (UGT) metabolism, CYP inhibition and induction, drug transporters, drug-drug interactions via assessment of reactive metabolites, genotoxicity, and chemical and photo-mutagenicity assays. Written for the Methods in Pharmacology and Toxicology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and tips on troubleshooting and avoiding known pitfalls. Expert authors have developed and utilized these in vitro assays to achieve “drug-like” characteristics in addition to efficacy properties and good safety profiles of drug candidates.

Comprehensive and up-to-date, Optimization in Drug Discovery: In Vitro Methods, Second Edition aims to guide researchers down the difficult path to successful drug discovery and development.

Editors and Affiliations

  • CREATe Core Science Technologies, Janssen Research & Development, LLC, Spring House, USA

    Gary W. Caldwell, Zhengyin Yan

Bibliographic Information

  • Book Title: Optimization in Drug Discovery

  • Book Subtitle: In Vitro Methods

  • Editors: Gary W. Caldwell, Zhengyin Yan

  • Series Title: Methods in Pharmacology and Toxicology

  • DOI: https://doi.org/10.1007/978-1-62703-742-6

  • Publisher: Humana Totowa, NJ

  • eBook Packages: Springer Protocols

  • Copyright Information: Springer Science+Business Media New York 2014

  • Hardcover ISBN: 978-1-62703-741-9Published: 09 November 2013

  • Softcover ISBN: 978-1-4939-6070-5Published: 23 August 2016

  • eBook ISBN: 978-1-62703-742-6Published: 08 November 2013

  • Series ISSN: 1557-2153

  • Series E-ISSN: 1940-6053

  • Edition Number: 2

  • Number of Pages: XVII, 597

  • Number of Illustrations: 64 b/w illustrations, 49 illustrations in colour

  • Topics: Pharmacology/Toxicology

  • Industry Sectors: Biotechnology, Chemical Manufacturing, Consumer Packaged Goods, Health & Hospitals, Pharma

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