Cytochrome P450 structure–function: insights from molecular dynamics simulations

PC Nair, RA McKinnon, JO Miners - Drug metabolism reviews, 2016 - Taylor & Francis
Abstract Cytochrome P450 (CYP) family 1, 2, and 3 enzymes play an essential role in the
metabolic clearance and detoxification of a myriad of structurally and chemically diverse …

Comparison of xenobiotic-metabolising human, porcine, rodent, and piscine cytochrome P450

V Burkina, MK Rasmussen, N Pilipenko… - Toxicology, 2017 - Elsevier
Cytochrome P450 proteins (CYP450s) are present in most domains of life and play a critical
role in the metabolism of endogenous compounds and xenobiotics. The effects of exposure …

Addressing the Intracellular Vestibule of the Plasmodial Lactate Transporter PfFNT by p-Substituted Inhibitors Amplifies In Vitro Activity

C Nerlich, F Tiedjens, R Hertel, B Henke… - Journal of Medicinal …, 2024 - ACS Publications
Inhibition of the lactate transporter PfFNT is a valid novel mode of action against malaria
parasites. Current pyridine-substituted pentafluoro-3-hydroxy-pent-2-en-1-ones act as …

Meloxicam methyl group determines enzyme specificity for thiazole bioactivation compared to sudoxicam

DA Barnette, MA Schleiff, A Datta, N Flynn… - Toxicology letters, 2021 - Elsevier
Meloxicam is a thiazole-containing NSAID that was approved for marketing with favorable
clinical outcomes despite being structurally similar to the hepatotoxic sudoxicam …

A comprehensive assay for nine major cytochrome P450 enzymes activities with 16 probe reactions on human liver microsomes by a single LC/MS/MS run to support …

Y Peng, H Wu, X Zhang, F Zhang, H Qi, Y Zhong… - Xenobiotica, 2015 - Taylor & Francis
A comprehensive method for the simultaneous characterization of xenobiotic compound
inhibition of nine major CYP enzymes in human liver microsomes was established by using …

Emerging investigator series: human CYP2A6 catalyzes the oxidation of 6: 2 fluorotelomer alcohol

O Daramola, AA Rand - Environmental Science: Processes & Impacts, 2021 - pubs.rsc.org
The biotransformation of 6: 2 fluorotelomer alcohol (6: 2 FTOH) results in the production of
bioactive and persistent metabolites, including perfluorinated carboxylic acids (PFCAs) …

Toxicological implications of mitochondrial localization of CYP2E1

JH Hartman, GP Miller, JN Meyer - Toxicology research, 2017 - academic.oup.com
Abstract Cytochrome P450 2E1 (CYP2E1) metabolizes an extensive array of pollutants,
drugs, and other small molecules, often resulting in bioactivation to reactive metabolites …

CYP2C19 and 3A4 dominate metabolic clearance and bioactivation of terbinafine based on computational and experimental approaches

MA Davis, DA Barnette, NR Flynn… - Chemical research in …, 2019 - ACS Publications
Lamisil (terbinafine) is an effective, widely prescribed antifungal drug that causes rare
idiosyncratic hepatotoxicity. The proposed toxic mechanism involves a reactive metabolite …

The role of cytochrome P450 3A4-mediated metabolism in sorafenib and lapatinib hepatotoxicity

MR McGill, Y Kaufmann, FV LoBianco, MA Schleiff… - Livers, 2023 - mdpi.com
Tyrosine kinase inhibitors (TKIs) are increasingly popular drugs used to treat more than a
dozen different diseases including some forms of cancer. Despite having fewer adverse …

Cytotoxic Homo- and Hetero-Dimers of o-toluidine, o-anisidine, and Aniline Formed by In Vitro Metabolism

T Kobayashi, S Kishimoto, S Watanabe… - Chemical Research …, 2022 - ACS Publications
Several aromatic amine compounds are urinary bladder carcinogens. Activated metabolites
and DNA adducts of polycyclic aromatic amines, such as 4-aminobiphenyl, have been …