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Novel Multiplexed High Throughput Screening of Selective Inhibitors for Drug-Metabolizing Enzymes Using Human Hepatocytes
Selective chemical inhibitors are critical for reaction phenoty** to identify drug-metabolizing enzymes that are involved in the elimination of...
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Drug Metabolizing Enzymes and Transporters of the Mesentery
Recent research has shown that the mesentery, which was classified as a new organ in 2016, is indeed an unfragmented structure. The mesentery is now...
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Formation of potentially toxic metabolites of drugs in reactions catalyzed by human drug-metabolizing enzymes
Data are presented on the formation of potentially toxic metabolites of drugs that are substrates of human drug metabolizing enzymes. The tabular...
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Effects of marine biotoxins on drug-metabolizing cytochrome P450 enzymes and their regulation in mammalian cells
Marine biotoxins are a heterogenous group of natural toxins, which are able to trigger different types of toxicological responses in animals and...
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Pharmacokinetic modulation of substrate drugs via the inhibition of drug-metabolizing enzymes and transporters using pharmaceutical excipients
BackgroundPharmaceutical excipients are used for formulating drugs to suit their intended use and effect. These excipients influence drug solubility,...
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Ontogeny of Drug-Metabolizing Enzymes
Almost 50% of prescription drugs lack age-appropriate dosing guidelines and therefore are used “off-label.” Only ~10% drugs prescribed to neonates...
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Cocaine regulates antiretroviral therapy CNS access through pregnane-x receptor-mediated drug transporter and metabolizing enzyme modulation at the blood brain barrier
BackgroundAppropriate interactions between antiretroviral therapies (ART) and drug transporters and metabolizing enzymes at the blood brain barrier...
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Characteristics of Major Drug Metabolizing Cytochrome P450 Enzymes
Cytochrome P450 (CYP) enzymes have been widely studied for drug discovery and development. While much has been discovered in terms of characteristics...
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Inhibition of drug-metabolizing enzymes by **gyin granules: implications of herb–drug interactions in antiviral therapy
**gyin granules, a marketed antiviral herbal medicine, have been recommended for treating H1N1 influenza A virus infection and Coronavirus disease...
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Pharmacogenomics in Drug Metabolism Enzymes and Transporters
The safe and effective use of drug therapies play a critical role in treating disease. Interindividual variability in drug metabolism and transport...
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Crystal Structures of Drug-Metabolizing CYPs
The complex enzyme kinetics displayed by drug-metabolizing cytochrome P450 enzymes (CYPs) (see Chapter 9...
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Inducibility of Metabolizing Enzymes
An important toxicologically relevant feature associated with foreign compound metabolism is the inducibility of metabolizing enzymes. Some...
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Abundance and Associated Variations of Cytochrome P450 Drug-Metabolizing Enzymes in the Liver of East Asian Adults: A Meta-Analysis
BackgroundCytochrome P450 (CYP) enzymes are one of the main sources of variability in drug metabolic clearance. Information on their abundance levels...
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Metabolic Enzymes: Polymorphisms and Species Differences
Before elimination from the body, foreign compounds to which humans are exposed undergo metabolic conversion mediated by phase I and phase II...
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Phase I Activation Enzymes
A vast majority of chemical reactions in living cells exhibit kinetic barriers that prevent the reactions from occurring spontaneously. Kinetic...
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Emerging Pathophysiology and Treatment of Prostate Cancer: Future Perspective
There is wide variability in the response of individuals to standard doses of drug therapy. This is an important problem in clinical practice, where...
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The genetic landscape of major drug metabolizing cytochrome P450 genes—an updated analysis of population-scale sequencing data
Genes encoding cytochrome P450 enzymes (CYPs) are extremely polymorphic and multiple CYP variants constitute clinically relevant biomarkers for the...
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Inhibitory Effect of Two Carbonic Anhydrases Inhibitors on the Activity of Major Cytochrome P450 Enzymes
Background and ObjectivesBoth AW-9A (coumarin derivative) and WES-1 (sulfonamide derivative) were designed and synthesized as potential selective...
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Inducibility of Metabolizing Enzymes
Metabolic enzyme inducibility is of major significance, because it plays an important role in the susceptibility of individuals to foreign...
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Phase II Detoxification Enzymes
Phase I enzymes catalyze the activation metabolism of foreign compounds. Their functionalization reactions incorporate a functional group into a...