Search Results - "Commandeur, Jan N. M"
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A 3D in vitro model of differentiated HepG2 cell spheroids with improved liver-like properties for repeated dose high-throughput toxicity studies
Published in Archives of toxicology (01-05-2014)“…Immortalized hepatocyte cell lines show only a weak resemblance to primary hepatocytes in terms of gene expression and function, limiting their value in…”
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Structural analysis of Cytochrome P450 BM3 mutant M11 in complex with dithiothreitol
Published in PloS one (24-05-2019)“…The bacterial Cytochrome P450 (CYP) BM3 (CYP102A1) is one of the most active CYP isoforms. BM3 mutants can serve as a model for human drug-metabolizing CYPs…”
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Biosynthesis of a steroid metabolite by an engineered Rhodococcus erythropolis strain expressing a mutant cytochrome P450 BM3 enzyme
Published in Applied microbiology and biotechnology (01-06-2015)“…In the present study, the use of Rhodococcus erythropolis mutant strain RG9 expressing the cytochrome P450 BM3 mutant M02 enzyme has been evaluated for…”
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Reduction and Scavenging of Chemically Reactive Drug Metabolites by NAD(P)H:Quinone Oxidoreductase 1 and NRH:Quinone Oxidoreductase 2 and Variability in Hepatic Concentrations
Published in Chemical research in toxicology (19-02-2018)“…Detoxicating enzymes NAD(P)H:quinone oxidoreductase 1 (NQO1) and NRH:quinone oxidoreductase 2 (NQO2) catalyze the two-electron reduction of quinone-like…”
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Linear Interaction Energy Based Prediction of Cytochrome P450 1A2 Binding Affinities with Reliability Estimation
Published in PloS one (09-11-2015)“…Prediction of human Cytochrome P450 (CYP) binding affinities of small ligands, i.e., substrates and inhibitors, represents an important task for predicting…”
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Application of a cocktail approach to screen cytochrome P450 BM3 libraries for metabolic activity and diversity
Published in Analytical and bioanalytical chemistry (01-02-2016)“…In the present study, the validity of using a cocktail screening method in combination with a chemometrical data mining approach to evaluate metabolic activity…”
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Human NAD(P)H:quinone Oxidoreductase 1 (NQO1)-Mediated Inactivation of Reactive Quinoneimine Metabolites of Diclofenac and Mefenamic Acid
Published in Chemical research in toxicology (21-04-2014)“…NAD(P)H:quinone oxidoreductase 1 (NQO1) is an enzyme capable of reducing a broad range of chemically reactive quinones and quinoneimines (QIs) and can be…”
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Diclofenac inhibits tumor necrosis factor‐α‐induced nuclear factor‐κB activation causing synergistic hepatocyte apoptosis
Published in Hepatology (Baltimore, Md.) (01-06-2011)“…Drug‐induced liver injury (DILI) is an important clinical problem. It involves crosstalk between drug toxicity and the immune system, but the exact mechanism…”
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Cytochrome P450-Mediated Bioactivation of Mefenamic Acid to Quinoneimine Intermediates and Inactivation by Human Glutathione S‑Transferases
Published in Chemical research in toxicology (15-12-2014)“…Mefenamic acid (MFA) has been associated with rare but severe cases of hepatotoxicity, nephrotoxicity, gastrointestinal toxicity, and hypersensitivity…”
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AMAP, the alleged non-toxic isomer of acetaminophen, is toxic in rat and human liver
Published in Archives of toxicology (01-01-2013)“…N -acetyl-meta-aminophenol (AMAP) is generally considered as a non-toxic regioisomer of the well-known hepatotoxicant acetaminophen (APAP). However, so far,…”
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Mass Spectrometric Characterization of Protein Adducts of Multiple P450-Dependent Reactive Intermediates of Diclofenac to Human Glutathione‑S‑transferase P1‑1
Published in Chemical research in toxicology (19-11-2012)“…Use of the nonsteroidal anti-inflammatory drug diclofenac (DF) is associated with serious idiosyncratic hepatotoxicity. Covalent binding of reactive…”
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Effect of Human Glutathione S‑Transferases on Glutathione-Dependent Inactivation of Cytochrome P450-Dependent Reactive Intermediates of Diclofenac
Published in Chemical research in toxicology (18-11-2013)“…Idiosyncratic adverse drug reactions due to the anti-inflammatory drug diclofenac have been proposed to be caused by the generation of reactive acyl…”
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Characterization of Human Cytochrome P450s Involved in the Bioactivation of Tri-ortho-cresyl Phosphate (ToCP)
Published in Chemical research in toxicology (20-04-2015)“…Tri-ortho-cresyl phosphate (ToCP) is a multipurpose organophosphorus compound that is neurotoxic and suspected to be involved in aerotoxic syndrome in humans…”
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Function, essentiality, and expression of cytochrome P450 enzymes and their cognate redox partners in Mycobacterium tuberculosis: are they drug targets?
Published in Applied microbiology and biotechnology (01-05-2019)“…This review covers the current knowledge of the cytochrome P450 enzymes (CYPs) of the human pathogen Mycobacterium tuberculosis (Mtb) and their endogenous…”
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Liquid Chromatography/Tandem Mass Spectrometry Detection of Covalent Binding of Acetaminophen to Human Serum Albumin
Published in Drug metabolism and disposition (01-08-2007)“…Covalent binding of reactive electrophilic intermediates to proteins is considered to play an important role in the processes leading to adverse drug reactions…”
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Determination and identification of estrogenic compounds generated with biosynthetic enzymes using hyphenated screening assays, high resolution mass spectrometry and off-line NMR
Published in Journal of chromatography. B, Analytical technologies in the biomedical and life sciences (01-03-2010)“…This paper describes the determination and identification of active and inactive estrogenic compounds produced by biosynthetic methods. A hyphenated screening…”
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Transcriptomic-based evaluation of trichloroethylene glutathione and cysteine conjugates demonstrate phenotype-dependent stress responses in a panel of human in vitro models
Published in Archives of toxicology (01-02-2023)“…Environmental or occupational exposure of humans to trichloroethylene (TCE) has been associated with different extrahepatic toxic effects, including…”
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Enzyme-Catalyzed Activation of Anticancer Prodrugs
Published in Pharmacological reviews (01-03-2004)“…The rationale for the development of prodrugs relies upon delivery of higher concentrations of a drug to target cells compared to administration of the drug…”
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Trimethoprim: Novel Reactive Intermediates and Bioactivation Pathways by Cytochrome P450s
Published in Chemical research in toxicology (01-11-2008)“…Trimethoprim (TMP) is a widely used antibacterial agent that is usually considered as a safe drug. TMP has, however, been implicated in rare adverse drug…”
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Homology Modeling of Rat and Human Cytochrome P450 2D (CYP2D) Isoforms and Computational Rationalization of Experimental Ligand-Binding Specificities
Published in Journal of medicinal chemistry (02-01-2003)“…The ligand-binding characteristics of rat and human CYP2D isoforms, i.e., rat CYP2D1−4 and human CYP2D6, were investigated by measuring IC50 values of 11 known…”
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