DNA methylation dynamics in the hepatic CYP3A4 gene promoter
Keywords: Epigenetics; CYP3A4; DNA methylation;
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Drosophila CYP6g1 and its human homolog CYP3A4 confer tolerance to methylmercury during development
Keywords: Methylmercury; Drosophila; Cytochrome P450; CYP6g1; CYP3A4
Intestinal CYP3A4 and midazolam disposition in vivo associate with VDR polymorphisms and show seasonal variation
Keywords: CYP3A4; Vitamin D; VDR; Polymorphism; Seasonal variation;
Semi-physiologically based pharmacokinetic modeling of paclitaxel metabolism and in silico-based study of the dynamic sensitivities in pathway kinetics
Keywords: Paclitaxel metabolism; Mathematical modeling; Pharmacokinetics; Sensitivity analysis; CYP2C8; CYP3A4
Role of human CYP3A4 in the biotransformation of sorafenib to its major oxidized metabolites
Keywords: CYP, cytochrome P450; FMO, flavin-containing monooxygenase; HPLC, high-performance liquid chromatography; LC–MS/MS, liquid chromatography–tandem mass spectrometry; TKI, tyrosine kinase inhibitorSorafenib; CYP3A4; Sorafenib biotransformation; Tyrosine kina
Effects of Radix Astragali and Radix Rehmanniae, the components of an anti-diabetic foot ulcer herbal formula, on metabolism of model CYP1A2, CYP2C9, CYP2D6, CYP2E1 and CYP3A4 probe substrates in pooled human liver microsomes and specific CYP isoforms
Keywords: Radix Astragali; Radix Rehmanniae; CYP1A2; CYP2C9; CYP2D6; CYP2E1; CYP3A4; Human liver microsomes
Stimulation of Human Monocytic THP-1 Cells by Metabolic Activation of Hepatotoxic Drugs
Keywords: adverse drug reactions; bioactivation; monocytes/macrophages; CYP3A4; drug-induced hepatotoxicity; inflammation;
Opioid Therapies and Cytochrome P450 Interactions
Keywords: Adverse drug reactions; cytochrome P450; CYP3A4; CYP2D6; drug-drug interactions; inhibitor; inducer; metabolism; prodrug; substrate; opioids
Regulation of CYP3A4 and CYP3A5 expression and modulation of “intracrine” metabolism of androgens in prostate cells by liganded vitamin D receptor
Keywords: Vitamin D receptor; Prostate; Metabolism; CYP3A4; CYP3A5;
Hepatocyte-like cells differentiated from human induced pluripotent stem cells: Relevance to cellular therapies
Keywords: AFP; alpha fetoprotein; Alb; albumin; ATP5g1; mitochondrial F0 complex, subunit C1 (subunit 9), ATP synthase 5 subunit e; ATP8; ATP synthase 8; BAL; bioartificial liver; BMP4; bone morphogenetic protein 4; CYP; cytochrome P450; CYP2C19; CYP Family 2, Subf
Identification of cytochrome P450 2D6 and 2C9 substrates and inhibitors by QSAR analysis
Keywords: CYP; cytochrome P450; CYP2C9; cytochrome P450 subtype 2C9; CYP2D6; cytochrome P450 subtype 2D6; CYP1A2; cytochrome P450 subtype 1A2; CYP2C19; cytochrome P450 subtype 2C19; CYP3A4; cytochrome P450 subtype 3A4; PLR; partial logistic regression; PLS; partial
Effects of Ketoconazole and Rifampicin on the Pharmacokinetics of Gemigliptin, a Dipeptidyl Peptidase-IV Inhibitor: A Crossover Drug–Drug Interaction Study in Healthy Male Korean Volunteers
Keywords: CYP3A4; drug–drug interaction; gemigliptin; ketoconazole; LC15-0444; rifampicin
Loss of orally administered drugs in GI tract
Keywords: Drug–drug interaction; Efflux transporters; Cytochrome P450; P-glycoprotein; Gut wall/mucosal enzymes; CYP3A4
Thiomers: Inhibition of cytochrome P450 activity
Keywords: Thiomers; Cytochrome P450; CYP3A4; CYP2A6; Inhibition; Fluorescent probe assays
Consequences of POR mutations and polymorphisms
Keywords: Cytochrome P450; P450 oxidoreductase; CYP3A4; CYP2D6; Steroidogenesis; Enzyme kinetics; Drug metabolism; Pharmacogenetics;
Identification of cytochrome P450 enzymes responsible for metabolism of cannabidiol by human liver microsomes
Keywords: Cannabidiol; Metabolism; Human liver microsomes; Cytochrome P450; CYP3A4; CYP2C19
Impact of CYP3A4*1G polymorphism on metabolism of fentanyl in Chinese patients undergoing lower abdominal surgery
Keywords: Gene polymorphism; CYP3A4; Fentanyl; HPLC
Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists
Keywords: Cannabinoid; CB1; Antagonist; Indole; Pharmacokinetics; CYP3A4; Glucuronidation
Rapid quantification of quinine and its major metabolite (3S)-3-hydroxyquinine in diluted urine by UPLC–MS/MS
Keywords: UPLC, ultra performance liquid chromatography; MS, mass spectrometry; GC–MS, gas chromatography–mass spectrometryUPLC; Fast gradient; Mass spectrometry; CYP3A4; Metabolism
A comparison of DNA damage induced by aflatoxin B1 in hepatocyte-like cells, their progenitor mesenchymal stem cells and CD34+ cells isolated from umbilical cord blood
Keywords: AFB1; Aflatoxin B1; AU; Arbitrary unit; CYP; Cytochrome P450; IC50; Inhibitory concentration; DMSO; Dimethylsulfoxide; hBMSCs; Human bone marrow mesenchymal stem cells; UCB; Umbilical cord blood; BSA; Bovine serum albumin; SCF; Stem cell factor; TPO; Thro
Potent inhibition of human cytochrome P450 3A isoforms by cannabidiol: Role of phenolic hydroxyl groups in the resorcinol moiety
Keywords: Cannabidiol; Δ9-Tetrahydrocannabinol; Cannabinol; CYP3A4; CYP3A5; CYP3A7; Inhibition
Reactive oxygen species alter autocrine and paracrine signaling
Keywords: Ad3A4; CYP3A4-expressing adenovirus; AdRSV; control adenovirus vector; AmR; amphiregulin; CD14; monocyte differentiation antigen; CYP2E1; cytochrome P450 2E1; CYP3A4; cytochrome P450 3A4; CYPH; cyclophilin A; ER; endoplasmic reticulum; ICAM1; intracellula
The discovery and synthesis of potent zwitterionic inhibitors of renin
Keywords: Renin; Hypertension; Piperidine; Zwitterion; hERG; CYP3A4
Aflatoxins upregulate CYP3A4 mRNA expression in a process that involves the PXR transcription factor
Keywords: PXR; pregnane X receptor; NHR; nuclear hormone receptor; DEX; dexamethasone; VD3; cholecalciferol; DCA; deoxycholic acid; TBHP; tert-butylhydroperoxide; CHX; cycloheximide; CYP3A4; Aflatoxins; PXR; Gene expression;
Effects of the antioxidant baicalein on the pharmacokinetics of nimodipine in rats: a possible role of P-glycoprotein and CYP3A4 inhibition by baicalein
Keywords: nimodipine; baicalein; pharmacokinetics; bioavailability; P-glycoprotein; CYP3A4
Formation of raloxifene homo-dimer in CYP3A4, evidence for multi-substrate binding in a single catalytically competent P450 active site
Keywords: Raloxifene; CYP3A4; Phenoxy radical; Homo-dimer; Binding sites; Metabolism;
The role of human cytochrome P4503A4 in biotransformation of tissue-specific derivatives of 7H-dibenzo[c,g]carbazole
Keywords: DBC; 7H-dibenzo[c,g]carbazole; DiMeDBC; dimethyldibenzo[c,g]carbazole; N-MeDBC; N-methyldibenzo[c,g]carbazole; CYP3A4; cytochrome P4503A4; Hprt gene; hypoxanthine-guanine phosphoribosyltransferase gene; 6-TGr; 6-thioguanine resistant; Human cytochrome P45
The role of CYP3A4 in amiodarone-associated toxicity on HepG2 cells
Keywords: Amiodarone; N-mono-desethylamiodarone; N-di-desethylamiodarone; HepG2 cells; CYP3A4
Reversible time-dependent inhibition of cytochrome P450 enzymes by duloxetine and inertness of its thiophene ring towards bioactivation
Keywords: ACN; acetonitrile; APAP; acetaminophen; CYP1A2; cytochrome P450 1A2 enzyme; CYP2B6; cytochrome P450 2B6 enzyme; CYP2C19; cytochrome P450 2C19 enzyme; CYP2D6; cytochrome P450 2D6 enzyme; CYP3A4; cytochrome P450 3A4 enzyme; CYP450; cytochrome P450 enzymes;
Prediction of time-dependent CYP3A4 drug–drug interactions by physiologically based pharmacokinetic modelling: Impact of inactivation parameters and enzyme turnover
Keywords: Time dependent inhibition; CYP3A4; PBPK models; Turnover of CYP3A4; Inactivation parameters; Prediction of DDIs
Gestion des effets secondaires des thérapies ciblées dans le cancer du rein : effets secondaires iatrogéniques
Keywords: interactions médicamenteuses; CYP3A4; antivitamine K; asthénie; hypothyroïdie; drug interactions; CYP3A4; antivitamin K; asthenia; hypothyroidism;
A prodrug approach towards the development of tricyclic-based FBPase inhibitors
Keywords: FBPase; Prodrug; CYP3A4
Reduction in hepatic drug metabolizing CYP3A4 activities caused by P450 oxidoreductase mutations identified in patients with disordered steroid metabolism
Keywords: CYP3A4; NADPH P450 oxidoreductase; POR; CPR; Steroid metabolism; Antely-Bixler syndrome; Adrenal hyperplasia; Drug metabolism
Addressing time-dependent CYP 3A4 inhibition observed in a novel series of substituted amino propanamide renin inhibitors, a case study
Keywords: CYP3A4; Time-dependent inhibition; Renin; Hypertension
Enantioselective capillary electrophoresis for identification and characterization of human cytochrome P450 enzymes which metabolize ketamine and norketamine in vitro
Keywords: Capillary electrophoresis; Ketamine; Norketamine; CYP3A4; CYP2A6; CYP2B6; Pharmacokinetics; Stereoselective metabolism
An in vitro drug-induced hepatotoxicity screening system using CYP3A4-expressing and γ-glutamylcysteine synthetase knockdown cells
Keywords: CYP3A4; Hepatotoxicity; Glutathione; AdenovirusCYP, cytochrome P450; GAPDH, glyceraldehydes-3-phosphate dehydrogenase; GCSh, γ-glutamylcysteine synthetase heavy chain; GFP, green fluorescence protein; GSH, glutathione; MOI, multiplicity of infection; PFU,
Major tanshinones of Danshen (Salvia miltiorrhiza) exhibit different modes of inhibition on human CYP1A2, CYP2C9, CYP2E1 and CYP3A4 activities in vitro
Keywords: Danshen (Salvia miltiorrhiza); Tanshinones; CYP1A2; CYP2C9; CYP2E1; CYP3A4; Human liver microsomes; In vitro
Overcoming drug resistance by regulating nuclear receptors
Keywords: Drug resistance; MDR1; PXR; CYP3A4; ABC transporters; Drug-metabolizing enzymes
The computational model to predict accurately inhibitory activity for inhibitors towardsCYP3A4
Keywords: CYP3A4; SVM; IC50; Predictive model
Endosulfan induces CYP2B6 and CYP3A4 by activating the pregnane X receptor
Keywords: Pesticide; Endosulfan; PXR; CAR; CYP3A4; CYP2B6; Human hepatocytes; HepG2 cell line
Induction of CYP3A4 and MDR1 gene expression by baicalin, baicalein, chlorogenic acid, and ginsenoside Rf through constitutive androstane receptor- and pregnane X receptor-mediated pathways
Keywords: Pregnane X receptor; Constitutive androstane receptor; CYP3A4; MDR1; Herbal product
Analysis of CYP3A4-HIV-1 protease drugs interactions by computational methods for Highly Active Antiretroviral Therapy in HIV/AIDS
Keywords: CYP3A4; Combination therapy; HAART; HIV-1 protease drug; Molecular docking; Salvage therapy
Up-regulation of CYP expression in hepatoma cells stably transfected by chimeric nuclear receptors
Keywords: Cytochrome P450; Drug metabolism; Nuclear receptor; CAR; PXR; CYP3A4
Design, synthesis, and pharmacological and pharmacokinetic evaluation of 3-phenyl-5-pyridyl-1,2,4-triazole derivatives as xanthine oxidoreductase inhibitors
Keywords: Gout; Xanthine oxidoreductase; XO; Hyperuricemia; Triazole derivatives; CYP3A4; Structure–activity relationship
A novel class of highly potent multidrug resistance reversal agents: Disubstituted adamantyl derivatives
Keywords: Multidrug resistance; MES-SA/DX5; ABC transporter; P-glycoprotein; Adamantane; CYP3A4
Novel therapeutic biosensor for indinavir—A protease inhibitor antiretroviral drug
Keywords: Drug metabolism biosensor; CYP3A4; Indinavir; Amperometric biosensor; Bioelectrode
The effects of diets enriched in beta-glucans on blood lipoprotein concentrations
Keywords: Beta-glucans; Lipoprotein; Cholesterol; CYP7A1; CYP3A4; Bile acids; LDLR
Discovery of 3-(3-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051-a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia
Keywords: Gout; Xanthine oxidoreductase inhibitor; XO; Hyperuricemia; Triazole derivatives; CYP3A4; Structure–activity relationships
Selective cytochrome P450 3A4 inhibitory activity of Amaryllidaceae alkaloids
Keywords: Cytochrome P450 3A4; CYP3A4; Amaryllidaceae alkaloid; Anticancer agent; Pancratistatin; Narciclasine; Galanthamine
Structure–activity studies on seco-pancratistatin analogs: Potent inhibitors of human cytochrome P450 3A4
Keywords: Cytochrome P450 3A4; CYP3A4; Pancratistatin; Anticancer agent; Ketoconazole