Results 21 to 30 of about 287,149 (254)
Dual effects of ketoconazole cis-enantiomers on CYP3A4 in human hepatocytes and HepG2 Cells. [PDF]
PLoS ONE, 2014 Antifungal drug ketoconazole causes severe drug-drug interactions by influencing gene expression and catalytic activity of major drug-metabolizing enzyme cytochrome P450 CYP3A4.
Aneta Novotná +6 more
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Dataset from proteomic analysis of human liver, lung, kidney and intestine microsomes
Data in Brief, 2018 We provide detailed datasets from our analysis of proteins that are identified in human liver, lung, kidney and intestine microsomes by MS-based proteomics.
Wei Song, Longjiang Yu, Zhihong Peng
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Interspecies Variation in NCMN-O-Demethylation in Liver Microsomes from Various Species
Molecules, 2019 NCMN (N-(3-carboxy propyl)-4-methoxy-1,8-naphthalimide), a newly developed ratiometric two-photon fluorescent probe for human Cytochrome P450 1A (CYP1A), shows the best combination of specificity and reactivity for real-time detection of the enzymatic ...
Ziru Dai +8 more
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Characterisation of theophylline metabolism by human liver microsomes [PDF]
Biochemical Pharmacology, 1987 1. A radiometric high performance liquid chromatographic method is described for the assay of theophylline metabolism in vitro by the microsomal fraction of human liver. 2. Formation of the three metabolites of theophylline (3‐methylxanthine, 1‐methylxanthine and 1,3‐ dimethyluric acid) were linear with protein concentrations to 4 mg ml‐1 and with ...
R A, Robson +6 more
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In Vitro Phase I Metabolism of CRV431, a Novel Oral Drug Candidate for Chronic Hepatitis B
Pharmaceutics, 2017 The cytochrome P450-mediated Phase I in vitro metabolism of CRV431 was studied using selective chemical inhibition and recombinant human enzymes. Additionally, the metabolic profile of CRV431 in human, rat, and monkey liver microsomes was investigated ...
Daniel J. Trepanier +2 more
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Simultaneous determination of 9 CYP450 enzymes in human liver microsomes using LC-MS/MS
Di-san junyi daxue xuebao, 2021 Objective To develop a liquid chromatography with tandem mass spectrometry (LC-MS/MS) to simultaneously detect the activities of 9 CYP450 enzymes in human liver microsomes in order to anticipate the possibility of drug-drug interactions.
SHI Zhongbo +5 more
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Angewandte Chemie, EarlyView.Fluorine‐18‐labeled CD73 inhibitor [18F]PSB‐19427 enables noninvasive PET mapping of CD73 overexpression in triple‐negative breast (TNBC) and pancreatic cancer. For [18F]PSB‐19427, specific binding in human tumor tissues, favorable biodistribution with prolonged blood retention, robust tumor uptake, and superiority to [18F]FDG in a TNBC model ...
Clemens Dobelmann +23 more
wiley +2 more sources
Stereoselective glucuronidation of formoterol by human liver microsomes [PDF]
British Journal of Clinical Pharmacology, 2000 Aims Formoterol is a β2‐adrenoceptor agonist marketed as a racemic mixture of the active (R; R)‐ and inactive (S; S)‐enantiomers (rac‐formoterol). The drug produces prolonged bronchodilation by inhalation but there is significant interpatient variability in duration of effect.
M, Zhang +3 more
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Journal of Lipid Research, 1998 In vitro techniques have been used to investigate the nature of microsomal cytochrome P450 involved in the metabolism of oleic acid, a physiological monounsaturated fatty acid. Like lauric acid, which is cur rently used as a model substrate of fatty acid
Fadi Adas +5 more
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Qualification of Human Liver Microsomes for Antibacterial Activity Screening of Drug Metabolites
Applied Microbiology, 2023 Microsomes are commonly used to perform in vitro drug metabolism, predominantly to form phase I drug metabolites. Pooled microsomes from multiple donors can contain microorganisms from underlying microbial diseases.
Navid Jubaer
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