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Cytochrome P450

In Vitro Methods and Protocols
BuchKartoniert, Paperback
379 Seiten
Englisch
Springererschienen am10.07.20221st ed. 2021
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.mehr
Verfügbare Formate
BuchGebunden
EUR181,89
BuchKartoniert, Paperback
EUR128,39

Produkt

KlappentextThis 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.
Zusammenfassung
Includes cutting-edge techniques

Provides the kind of detail necessary for reproducible results

Contains key implementation advice from the experts
Details
ISBN/GTIN978-1-0716-1544-7
ProduktartBuch
EinbandartKartoniert, Paperback
Verlag
Erscheinungsjahr2022
Erscheinungsdatum10.07.2022
Auflage1st ed. 2021
ReiheMethods in Pharmacology and Toxicology
Seiten379 Seiten
SpracheEnglisch
IllustrationenXI, 379 p. 94 illus., 40 illus. in color.
Artikel-Nr.50925075
Rubriken
GenreMedizin

Inhalt/Kritik

Inhaltsverzeichnis
Cytochrome P450: In Vitro Methods and Protocols.- Characteristics of Major Drug Metabolizing Cytochrome P450 Enzymes.- Quantitative Determination of Cytochrome P450 Using LC/MS/MS.- Spectral Quantitation of Total Cytochrome P450 in Microsomes Using a Single-Beam Spectrophotometer.- Cytochrome P450 Enzyme Kinetics: Km and Vmax Determinations Using Metabolite Formation and Substrate Depletion Methods.- Cytochrome P450 Inhibition Assay Using Human Liver Microsomes.- Evaluation of Time-Dependent Cytochrome P450 Inhibition Using the Area Under the Curve Shift Method.- Assessing Cytochrome P450 Time Dependent Inhibition (IC50 Shift Assay) Using Both Diluted and Non-Diluted Methods.- Cytochrome P450 Gene Regulation: Reporter Assays to Assess Pregnane X Receptor (PXR, NR1I2) Activation.- Cytochrome P450 Gene Regulation: Reporter Assays to Assess Aryl Hydrocarbon Receptor (HLHE76, AhR) Activation and Antagonism.- Cytochrome P450 Gene Regulation: Reporter Assays to Assess Direct and Indirect Activation of Constitutive Androstane Receptor (CAR, NR1I3).- Determination of In Vitro Cytochrome P450 Induction Potential Using Cryopreserved Human Hepatocytes.- Assessing Cytochrome P450 3A (CYP3A) Induction and Suppression Using Primary Human Hepatocyte Spheroids.- Cytochrome P450-Mediated Metabolic Stability Assay in Liver Microsomes.- Assessment of Cytochrome P450 Metabolic Clearance Using Hepatocyte Suspension.- Cytochrome P450 Knock-Out Assay with Non-Selective Inhibitors.- Differentiation of Cytochrome P450-Mediated from Non-CYP-Mediated Metabolism: Aldehyde Oxidase and Xanthine Oxidoreductase.- In Vitro Reaction Phenotyping of Cytochrome P450 Enzymes.- Cytochrome P450-Mediated Drug Bioactivation Assay: An Untargeted High Resolution Accurate Mass LC/MS Assay.- Simultaneously Assessing Concentration Changes in 20 Biochemical Pathways as a Result of Drug Dosing and Cytochrome P450 and Non-Cytochrome P450-Mediated Metabolism: An Untargeted Metabolomics GC/MS Assay.-Simultaneously Assessing Concentration Changes in 17 Biochemical Pathways as a Result of Drug Dosing and Cytochrome P450 and Non-Cytochrome P450-Mediated Metabolism: A Quasi-Untargeted Metabolomics LC/MS Assay.- Assessing Amino Acid Concentration Changes as a Result of Drug Dosing and Cytochrome P450 and Non-Cytochrome P450-Mediated Metabolism.mehr