Biotransformation of bromhexine by Cunninghamella elegans, C. echinulata and C. blakesleeana
Keywords: Cunninghamella sp.; Bromhexine; RLM; CYP3A4; Inhibitor; Metabolism;
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Relationship between NR1I2 polymorphisms and inflammatory bowel disease risk: A systematic review and meta-analysis
Keywords: NR1I2; Homo sapiens nuclear receptor subfamily 1 group I member 2; IBD; inflammatory bowel diseases; UC; Ulcerative Colitis; CD; Crohn's Disease; OR; odd radio; CI; confidence interval; PPARα; peroxisome proliferator-activated receptor alpha; FXR; farnes
QSAR development and profiling of 72,524 REACH substances for PXR activation and CYP3A4 induction
Keywords: AD; applicability domain; AOP; adverse outcome pathway; CYP; cytochrome P450; CYP3A4; human cytochrome P450 isoform 3A4; DTU; Technical University of Denmark; Food; National Food Institute; hPXR; full-length human Pregnane X Receptor; hPXR-LBD; human Preg
Rapid screening the potential mechanism-based inhibitors of CYP3A4 from Tripterygium wilfordi based on computer approaches combined with in vitro bioassay
Keywords: Tripterygium wilfordii; Mechanism-based inhibitors; CYP3A4; Pharmacophore model; Molecular docking; In vitro experiment;
The association among cytochrome P450 3A, progesterone receptor polymorphisms, plasma 17-alpha hydroxyprogesterone caproate concentrations, and spontaneous preterm birth
Keywords: CYP3A4; CYP3A5 and progesterone receptor; prematurity; single nucleotide polymorphisms; spontaneous preterm birth; 17-alpha hydroxyprogesterone caproate;
The consequence of regional gradients of P-gp and CYP3A4 for drug-drug interactions by P-gp inhibitors and the P-gp/CYP3A4 interplay in the human intestine ex vivo
Keywords: 3OH-Qi; 3-hydroxy-quinidine; ADME-Tox; absorption, distribution, metabolism, excretion and toxicity; CP100356; N-(3,4-dimethoxyphenethyl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2[1H]-yl)-6,7-dimethoxyquinazolin-2-amine; CYP; cytochrome P450; DDI(s); drug
No 329-Consensus canadien sur la contraception (4e partie de 4) : chapitre 9 - contraception hormonale combinée
Keywords: Contraception; family planning; Canada; sexual health; hormonal contraception; emergency contraception; combined hormonal contraception; oral contraceptive pill; transdermal contraceptive patch; vaginal contraceptive ring; continuous hormonal contraceptio
Discovery of novel 1,2,3,4-tetrahydrobenzo[4, 5]thieno[2, 3-c]pyridine derivatives as potent and selective CYP17 inhibitors
Keywords: Prostate cancer; Androgens; CYP17; Abiraterone; CYP3A4;
Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites
Keywords: ABC transporters; transporters; skin; P-glycoprotein; tissue partition; ABCB1; ATP binding cassette subfamily B member 1; ABCG2; ATP binding cassette subfamily G member 2; BCRP; breast cancer resistance protein; CRC; colorectal cancer; CYP3A4; cytochrome
Synthesis and pharmacological evaluation of glycine amide derivatives as novel vascular adhesion protein-1 inhibitors without CYP3A4 and CYP2C19 inhibition
Keywords: Vascular adhesion protein-1; Diabetic nephropathy; Glycine amide; CYP2C19; CYP3A4;
Modeling of drug-mediated CYP3A4 induction by using human iPS cell-derived enterocyte-like cells
Keywords: Human iPS cells; Enterocyte-like cells; CYP3A4 induction; Nuclear receptor; CDX2; caudal type homeobox 2; CYP3A4; cytochrome P450 3A4; DEX; dexamethasone; EGF; epidermal growth factor; FGF2; fibroblast growth factor 2; FXR; farnesoid X receptor; GR; gluco
Effects of macroporous hydroxyapatite carriers on the growth and function of human hepatoblasts derived from fetal hepatocytes
Keywords: Hydroxyapatite; Cell proliferation; Human fetal hepatocytes; Human hepatoblast; Macroporous carrier; Pore size; Radius of curvature; CYP3A4
Liquid chromatography-tandem mass spectrometric assay for ponatinib and N-desmethyl ponatinib in mouse plasma
Keywords: ALL; acute lymphoblastic leukemia; BCR-ABL; breakpoint cluster region-Abelson murine leukemia viral oncogene homolog; CML; chronic myeloid leukemia; CYP3A4; cytochrome P450 3A4; DMP; N-desmethyl ponatinib; ESI; electrospray Ionization; FVB; friend leukemi
ReviewInfluence of 25-hydroxyvitamin D3 and 1,25-dihydroxyvitamin D3 on expression of P-glycoprotein and cytochrome P450 3A in sheep
Keywords: P-gp,MDR1,ABCB1; P-glycoprotein; CYP3A4; cytochrome P450 3A; VDR; vitamin D receptor; PXR; pregnane X receptor; RXR; αretinoid X receptor; BW; body weight; 25-OHD3; 25-hydroxyvitamin D3; 1,25-(OH)2D3; 1,25-dihydroxyvitamin D3; Cholecalciferol; Ruminant;
SUMOylation of pregnane X receptor suppresses rifampicin-induced CYP3A4 and P-gp expression and activity in LS174T cells
Keywords: Pregnane X receptor; SUMOylation; Transcriptional activity; CYP3A4; P-gpSUMO, small ubiquitin-related modifier; PXR, pregnane X receptor; RIF, rifampicin; CYP3A4, cytochrome P450 3A4; P-gp, p-glycoprotein; MDZ, midazolam; 1′-OHMDZ, 1′-Hydroxymidazolam; Rh
Tryptophan 299 is a conserved residue of human pregnane X receptor critical for the functional consequence of ligand binding
Keywords: PXR; CYP3A4; Xenobiotic receptor; SAR; Transcriptional regulation;
Spectroscopic studies and molecular docking on the interaction of organotin antitumor compound bis[2,4-difluoro-N-(hydroxy-⟨κ⟩O)benzamidato-⟨κ⟩O]diphenyltin(IV) with human cytochrome P450 3A4 protease
Keywords: Organotin compound; CYP3A4; Interaction; Spectroscopic study; Molecular docking
The use of isomeric testosterone dimers to explore allosteric effects in substrate binding to cytochrome P450 CYP3A4
Keywords: Cytochrome P450; CYP3A4; Resonance Raman; Allosteric properties; Nanodiscs; Testosterone dimers
Drug membrane transporters and CYP3A4 are affected by hypericin, hyperforin or aristoforin in colon adenocarcinoma cells
Keywords: Hypericin; Hyperforin; Aristoforin; Drug efflux; CYP3A4; Drug resistance
MicroRNA-877-5p is involved in the trovafloxacin-induced liver injury
Keywords: ABCF1; ATP binding cassette subfamily F member 1; ALT; alanine aminotransferase; APAF1; apoptotic protease activating factor 1; CCl4; carbon tetrachloride; CHOP; CCAAT enhancer-binding protein homologous protein; CYP3A4; cytochrome P450 family 3 subfamily
Hydroxylation of 20-hydroxyvitamin D3 by human CYP3A4
Keywords: 20-Hydroxyvitamin D3; CYP3A4; Hydroxylation; Liver microsomes;
In vitro evaluation of hepatotoxic drugs in human hepatocytes from multiple donors: Identification of P450 activity as a potential risk factor for drug-induced liver injuries
Keywords: Hepatotoxicity; DILI; Idiosyncratic hepatotoxicity; Individual differences; Risk factors; P450; CYP3A4; Acetaminophen; Cyclophosphamide; Ketoconazole; Tamoxifen; Human hepatocytes
Metabolic characterization of pyrotinib in humans by ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry
Keywords: Pyrotinib; UPLC/Q-TOF MS; Metabolism; Human; CYP3A4; Drug-drug interaction;
Developmental regulation of CYP3A4 and CYP3A7 in Chinese Han population
Keywords: CYP3A4; CYP3A7; Ontogeny; Nuclear receptor; Epigenetic modifications;
O-alkylhydroxylamines as rationally-designed mechanism-based inhibitors of indoleamine 2,3-dioxygenase-1
Keywords: IDO1 inhibition; O-alkylhydroxylamines; Antitumor therapy; Rational drug design; IDO1; indoleamine 2,3-dioxygenase isoform-1; Trp; tryptophan; UV-vis; ultraviolet-visible; CYP3A4; cytochrome P-450 isoform 3A4;
Identification of stable and reactive metabolite(s) of nelfinavir in human liver microsomes and rCYP3A4
Keywords: Nelfinavir; HLM; CYP3A4; Diquinone metabolite; N-Oxide metabolite
Cross-talk between EPAS-1/HIF-2α and PXR signaling pathway regulates multi-drug resistance of stomach cancer cell
Keywords: EPAS-1; Endothelial PAS domain-containing protein 1; PXR; Pregnane X Receptor (PXR); MDR; multi-drugs resistance; CYP3A4; cytochromes P450 3A4; HIF-2α; hypoxia-inducible transcription factors; ARNT; aryl hydrocarbon receptor nuclear translocator; HRE; hy
Modulation of CYP3A4 activity alters the cytotoxicity of lipophilic phycotoxins in human hepatic HepaRG cells
Keywords: Phycotoxins; Hepatocytes; High content analysis; CYP3A4; Cytotoxicity;
Synthesis and metabolic studies of 1α,2α,25-, 1α,4α,25- and 1α,4β,25-trihydroxyvitamin D3
Keywords: Vitamin D3; Trihydroxyvitamin D3; Vitamin D receptor; CYP3A4; CYP24A1; UGT;
Mechanism-based inhibition of Alantolactone on human cytochrome P450 3A4 in vitro and activity of hepatic cytochrome P450 in mice
Keywords: Alantolactone PubChem CID: 72724; Alantolactone; CYP3A4; Human liver microsomes; Noncompetitive inhibition; Drug-drug interaction;
Investigation of the dominant positive effect of porcine farnesoid X receptor (FXR) splice variant 1
Keywords: CAR; constitutive androstane receptor; PXR; pregnane X receptor; FXR; farnesoid X receptor; CYP3A4; cytochrome P450 3A4; SULT2A1; hydroxysteroid sulfotransferase; UGT2B4; UDP-glucuronosyltransferase 2B4; GRβ; glucocorticoid receptor β; ERE; estrogen res
Discovery and optimization of a highly efficacious class of 5-aryl-2-aminopyridines as FMS-like tyrosine kinase 3 (FLT3) inhibitors
Keywords: Feline McDonough sarcoma (FMS)-like tyrosine kinase 3 (FLT3); Aminopyridine; Hinge binding motif; CYP3A4; Time-dependent inhibition
Research ArticleOmbitasvir/paritaprevir/r and dasabuvir plus ribavirin in HCV genotype 1-infected patients on methadone or buprenorphine
Keywords: HCV; hepatitis C virus; CYP3A4; cytochrome P450 isoform 3A4; RNA; ribonucleic acid; HIV; human immunodeficiency virus; LLOD; lower limit of detection; LLOQ; lower limit of quantitation; MedDRA; Medical Dictionary for Regulatory Activities; MEMS; Medicatio
Effects of cytokines on CYP3A4 expression and reversal of the effects by anti-cytokine agents in the three-dimensionally cultured human hepatoma cell line FLC-4
Keywords: CYP3A4; Expression; Cytokine; Tocilizumab; IL-1raC/EBP, CCAAT/enhancer-binding protein; CYP, cytochrome; DMSO, dimethyl sulfoxide; GAPDH, glyceraldehyde-3-phosphate dehydrogenase; IL, interleukin; IL-1ra, interleukin-1 receptor antagonist; LDH, lactate de
Effects of CYP3A4/5 and ABCB1 genetic polymorphisms on carbamazepine metabolism and transport in Chinese patients with epilepsy treated with carbamazepine in monotherapy and bitherapy
Keywords: Carbamazepine; Genetic polymorphism; Plasma concentration; CYP3A4; CYP3A5; ABCB1;
Ontogenic expression of human carboxylesterase-2 and cytochrome P450 3A4 in liver and duodenum: Postnatal surge and organ-dependent regulation
Keywords: CES2; carboxylesterase-2; CYP3A4; cytochrome P450 3A4; GAPDH; glyceradehyde-3-phosphate dehydrogenase; GI; gastrointestinal; PBS; phosphate buffered saline; PPARα; peroxisome proliferator-activated receptor-α; RT-qPCR; reverse transcription-quantitative
A food contaminant ochratoxin A suppresses pregnane X receptor (PXR)-mediated CYP3A4 induction in primary cultures of human hepatocytes
Keywords: Ochratoxin A; CYP3A4; PXR; miR-148a;
Association of CYP3A4 and CYP3A5 polymorphisms with Iranian breast cancer patients
Keywords: Breast cancer; CYP3A4; CYP3A5; Polymorphism; Iranian population
Effects of HMG-CoA reductase inhibitors on the pharmacokinetics of nifedipine in rats: Possible role of P-gp and CYP3A4 inhibition by HMG-CoA reductase inhibitors
Keywords: Nifedipine; HMG-CoA reductase inhibitors; Pharmacokinetics; P-gp; CYP3A4
Bioinformatic analysis of miRNAs targeting the key nuclear receptors regulating CYP3A4 gene expression: The challenge of the CYP3A4 “missing heritability” enigma
Keywords: miRNA; Gene regulation; CYP3A4; Cytochrome P450; Metabolism
3-Hydroxyflavone and structural analogues differentially activate pregnane X receptor: Implication for inflammatory bowel disease
Keywords: 3-Hydroxyflavone (PubChem CID: 11349); Galangin (PubChem CID: 5281616); Datiscetin (PubChem CID: 5281610); Kaempferol (PubChem CID: 5280863); Morin (PubChem CID: 5281670); Quercetin dihydrate (PubChem CID: 5284452); Isorhamnetin (PubChem CID: 5281654); Ta
Effect of CKD and Dialysis Modality on Exposure to Drugs Cleared by Nonrenal Mechanisms
Keywords: Nonrenal drug clearance; drug metabolism; pharmacokinetics; cytochrome P450; CYP3A4; hepatic and intestinal drug transporters; hemodialysis (HD); peritoneal dialysis (PD); chronic kidney disease (CKD); adverse effects; medication exposure;
Identification of 2-aminopyrimidine derivatives as inhibitors of the canonical Wnt signaling pathway
Keywords: APC; adenomatous polyposis coli; CK1; casein kinase-1; CYP3A4; Cytochrome P450 3A4; FPSA; fractional polar surface area; Fz; frizzled; GSK3; glycogen synthase kinase 3; LEF; lymphoid enhancer-binding factor; LRP; lipoprotein receptor-related protein; MW;
Molecular docking of chemotherapeutic agents to CYP3A4 in non-small cell lung cancer
Keywords: CYP3A4; Binding affinity; Drug metabolism; Chemotherapeutics; Non-small cell lung cancer
Environmental pollutants parathion, paraquat and bisphenol A show distinct effects towards nuclear receptors-mediated induction of xenobiotics-metabolizing cytochromes P450 in human hepatocytes
Keywords: Human hepatocytes; CYP3A4; TAT; PXR; AhR
Discovery of an 8-methoxytetrahydroisoquinoline derivative as an orally active N-type calcium channel blocker for neuropathic pain without CYP inhibition liability
Keywords: N-type calcium channel; CaV2.2; Pain; CYP2D6; CYP3A4;
Impact of gender on efficacy and acute toxicity of alkylating agent -based chemotherapy in Ewing sarcoma: Secondary analysis of the Euro-Ewing99-R1 trial
Keywords: Ewing sarcomas; Alkylating agent; Gender; Efficacy; Toxicity; Interaction; Metabolism; Constitutive androstane receptor; CYP3A4; CYP2B6;
Discovery of a 1-isopropyltetrahydroisoquinoline derivative as an orally active N-type calcium channel blocker for neuropathic pain
Keywords: N-type calcium channel; CaV 2.2; Pain; CYP2D6; CYP3A4;
Optimization of a novel series of N-phenylindoline-5-sulfonamide-based acyl CoA:monoacylglycerol acyltransferase-2 inhibitors: Mitigation of CYP3A4 time-dependent inhibition and phototoxic liabilities
Keywords: ACAT; acyl CoA:cholesterol acyltransferase; ADME; absorption, distribution, metabolism and excretion; APCI; atomospheric pressure chemical ionization; CM; chylomicron; dba; dibenzylideneacetone; CYP; cytochrome P450; DDI; drug-drug interaction; DGAT; ac
Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD2 receptors CRTH2 and DP
Keywords: CRTH2; DP; CYP3A4; Indole; Phenylacetic acid;