Results 21 to 30 of about 23,100 (164)

Regioselective Hydroxylation of Phloretin, a Bioactive Compound from Apples, by Human Cytochrome P450 Enzymes

open access: yesPharmaceuticals, 2020
Phloretin, the major polyphenol compound in apples and apple products, is interesting because it shows beneficial effects on human health. It is mainly found as a form of glucoside, phlorizin. However, the metabolic pathway of phloretin in humans has not
Ngoc Anh Nguyen   +9 more
doaj   +1 more source

Analysis of in vitro and in vivo metabolism of zidovudine and gemfibrozil in trans‐chromosomic mouse line expressing human UGT2 enzymes

open access: yesPharmacology Research & Perspectives, 2022
UDP‐glucuronosyltransferases (UGTs) catalyze the conjugation of various substrates with sugars. Since the UGT2 family forms a large cluster spanning 1.5 Mb, transgenic mouse lines carrying the entire human UGT2 family have not been constructed because of
Kaoru Kobayashi   +9 more
doaj   +1 more source

Dual effects of ketoconazole cis-enantiomers on CYP3A4 in human hepatocytes and HepG2 Cells. [PDF]

open access: yesPLoS 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
doaj   +1 more source

In vitro metabolic characterization of the SARS-CoV-2 papain-like protease inhibitors GRL0617 and HY-17542

open access: yesFrontiers in Pharmacology, 2023
The SARS-CoV-2 pandemic requires a new therapeutic target for viral infection, and papain-like protease (Plpro) has been suggested as a druggable target.
Hyunki Cho   +6 more
doaj   +1 more source

Dataset from proteomic analysis of human liver, lung, kidney and intestine microsomes

open access: yesData 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
doaj   +1 more source

Interspecies Variation in NCMN-O-Demethylation in Liver Microsomes from Various Species

open access: yesMolecules, 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
doaj   +1 more source

In Vitro Phase I Metabolism of CRV431, a Novel Oral Drug Candidate for Chronic Hepatitis B

open access: yesPharmaceutics, 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
doaj   +1 more source

Simultaneous determination of 9 CYP450 enzymes in human liver microsomes using LC-MS/MS

open access: yesDi-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
doaj   +1 more source

Involvement of cytochrome P450 2E1 in the (ω–1)-hydroxylation of oleic acid in human and rat liver microsomes

open access: yesJournal 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
doaj   +1 more source

Qualification of Human Liver Microsomes for Antibacterial Activity Screening of Drug Metabolites

open access: yesApplied 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
doaj   +1 more source

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