Optimization in Drug Discovery by Zhengyin YanOptimization in Drug Discovery by Zhengyin Yan

Optimization in Drug Discovery

EditorZhengyin Yan, Gary W. Caldwell

Paperback | November 9, 2010

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A panel of researchers and experts from leading universities and major pharmaceutical companies from all over the world systematically describe cutting-edge experimental protocols for the early in vitro evaluation of new chemical entities (NCE). These readily reproducible assays measure such critical parameters as physicochemical properties, adsorption, plasma binding, metabolism, drug interactions, and toxicity. By uncovering early in the discovery stage the defects that can eliminate candidate drugs from preclinical and clinical development, these techniques can save millions of dollars in time and effort.

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Title:Optimization in Drug DiscoveryFormat:PaperbackDimensions:434 pages, 9.02 × 5.98 × 0.04 inPublished:November 9, 2010Publisher:Humana PressLanguage:English

The following ISBNs are associated with this title:

ISBN - 10:1617374997

ISBN - 13:9781617374999

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Table of Contents

pKa, Solubility and Lipophilicity: Assessing Physicochemical Properties of Lead CompoundsYushen Guo and Hong ShenUse of Caco-2 Cell Monolayers to Study Drug Absorption and MetabolismMing Hu, Jie Ling, Huimin Lin, and Jun ChenAbsorption Screening Using the PAMPA ApproachJeffrey A. Ruell and Alex AvdeefIn Situ Single-Pass Perfused Rat Intestinal Model for Absorption and MetabolismEun Ju Jeong, Yan Liu, Huimin Lin, and Ming HuIn Vitro Permeation Study With Bovine Brain Microvessel Endothelial CellsSeong-Hee Park, Sung-Hack Lee, Yaming Su, and Patrick J. SinkoAn Enzymatic Microplate Assay for Testing P-Glycoprotein Substrates and InhibitorsS. Orlowski, J. Nugier, and Eric EzanEvaluation of Drug-Transporter Interactions Using In Vitro Cell ModelsYaming Su and Patrick J. SinkoPlasma Protein-Binding Methods in Drug DiscoveryLucinda H. CohenIsothermal Titration Calorimetry Characterization of Drug-Binding Energetics to Blood ProteinsGary W. Caldwell and Zhengyin YanMetabolic Stability Assessed by Liver Microsomes and HepatocytesDavid C. Ackley, Kevin T. Rockich, and Timothy R. BakerIn Vitro Drug Metabolite Profiling Using Hepatic S9 and Human Liver MicrosomesWu-Nan Wu and Linda A. McKownIn Vitro Identification of UDP-glucuronosyltransferases Involved in Drug MetabolismMichael H. CourtIn Vitro CYP Induction in Human HepatocytesDaniel R. Mudra and Andrew ParkinsonHigh-Throughput Screening of Human Cytochrome P450 Inhibitors Using Fluorometric Substrates: Methodology for 25 Enzyme/Substrate PairsDavid M. StresserEvaluation of Cytochrome P450 Inhibition in Human Liver MicrosomesZhengyin Yan and Gary W. CaldwellIdentification of CYP Mechanism-Based InhibitorsAmin A. Nomeir, Jairam Palamanda, and Leonard FavreauDetection of DNA Adducts by 32P-Postlabeling AnalysisNaomi Suzuki, Padmaja M. Prabhu, and Shinya ShibutaniCovalent DNA Adduct Formation Mediated by Cytochrome P450Marie StiborováApplication of In Vitro Comet Assay for Genotoxicity TestingBojana Zegura and Metka FilipicAssessing DNA Damage Using a Reporter Gene SystemXuming Jia and Wei XiaoImprovement of the Ames Test Using Human Liver S9 PreparationAtsushi Hakura, Satoshi Suzuki, and Tetsuo SatohScreening for Chemical Mutagens Using the Mouse Lymphoma AssayTao Chen and Martha M. MooreA High-Throughput Binding Assay for HERGKeith Finlayson and John SharkeyIn Vitro Drug Metabolism: Thiol ConjugationWei Tang and Randy R. MillerIn Vitro Screening Assay of the Reactivity of Acyl GlucuronidesSébastien BolzeIndex

Editorial Reviews

"This book covers most of the currently used techniques in lead optimization with respect to ADME and safety profiles. . .would be very useful addition to the library of any drug scientist interested in an introduction to these important methods. Each chapter treats its topic in a concise manner and provides ample references to lead the reader to more detailed information."-Doody's Health Sciences Book Review Journal"...very useful technically...invaluable to those changing roles or joining a pharmaceutical company, it is also very helpful for scientists in the biotech industry who are new to drug discovery." - Immunology News"The book provides a wealth of relevant information...the tome is neatly designed, well constructed and easy to read." - ISSX Newsletter"...a useful reference handbook for in vitro ADMET assays." - ChemBioChem