Titlebook: Optimization in Drug Discovery; Zhengyin Yan,Gary W. Caldwell Book 2004 Humana Press 2004

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In Vitro Drug Metabolite Profiling Using Hepatic S9 and Human Liver Microsomes,a this organ. In general, drugs are predominantly metabolized by the oxidation of parent drug, which is typically mediated by cytochrome P450 (CYP450) enzymes. To a lesser degree, flavin monooxidation (FMO), as well as the reduction or cleavage of the parent drug via enzymatic (i.e., esterase and am

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In Vitro CYP Induction in Human Hepatocytes,nsively as possible. For this reason, laboratories have developed various in vitro techniques that can help to minimize undue investment in developmental compounds that may have undesirable pharmacokinetic properties and/or the potential to cause adverse effects, such as toxicity and drug-drug inter

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Evaluation of Cytochrome P450 Inhibition in Human Liver Microsomes, potential. This chapter describes a detailed traditional CYP inhibition protocol for six major isoforms: 1A2, 2C9, 2C19, 2D6, 2E1, and 3A4. Microsomal incubation conditions were optimized and kinetic parameters determined to initially establish the inhibition assay. In CYP inhibition assay, separat

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Identification of CYP Mechanism-Based Inhibitors,ing the activity of the enzyme(s) that metabolize drug B. Inhibitory drug-drug interactions could result in serious adverse effects, including fatalities in patients receiving multiple medications. Cytochrome P450 superfamily (CYPs) are the major oxidative enzymes that participate in the metabolism

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Covalent DNA Adduct Formation Mediated by Cytochrome P450,s (drugs) to be activated to reactive species, leading to the formation of covalent deoxyribonucleic acid (DNA) adducts. Methods for the isolation of subcellular fractions containing activating enzymes (microsomes or cytosols containing cytochromes P450 or other activating enzymes such as reductases

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Application of In Vitro Comet Assay for Genotoxicity Testing,eic acid (DNA) damage at the level of individual eukaryotic cells. The types of DNA damage that can be observed with this method are DNA double-strand breaks (DSB) and single-strand breaks (SSB), alkali labile sites (ALS) such as apurinic/apyrimidinic (AP) sites, DNA-DNA and DNA-protein cross-links,

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