Evaluation of Farnesoid X Receptor Target Gene Induction in Human Hepatocytes: Amino Acid Conjugation [0.03%]
人肝细胞中法尼醇X受体靶基因诱导评价：氨基芥化的作用
Jean Simmermacher,Michael Sinz
Jean Simmermacher
Background: The nuclear hormone receptor, Farnesoid X Receptor (FXR) regulates the transcription of genes associated with bile acid metabolism and disposition. ...
Comparative Study
Drug metabolism letters. 2017;11(2):138-143. DOI:10.2174/1872312812666171227213946 2017
Utility of Pooled Cryopreserved Human Enterocytes as an In vitro Model for Assessing Intestinal Clearance and Drug-Drug Interactions [0.03%]
用于评估肠道清除率和药物相互作用的体外人结肠细胞模型的价值研究
Susan Wong,Utkarsh Doshi,Peter Vuong et al.
Susan Wong et al.
Background: A recent advancement in isolation and cryopreservation has resulted in commercially available primary human enterocytes that express various drug metabolizing enzymes (DMEs) and transporters. The main objectiv...
Transactivation Assays that Identify Indirect and Direct Activators of Human Pregnane X Receptor (PXR, NR1I2) and Constitutive Androstane Receptor (CAR, NR1I3) [0.03%]
鉴定人孕烷X受体(PXR，NR1I2)和 constitutive androstane 受体(CAR，NR1I3)间接激活剂和直接激活剂的转录激活试验
Marija Pinne,Elsa Ponce,Judy L Raucy
Marija Pinne
Background: Nuclear Receptors (NRs), including PXR and CAR, are presumed to be ligand-dependent transcription factors, but ligand binding is not an absolute requirement for activation. Indeed, many compounds activate PXR ...
Suresh K Balani
Suresh K Balani
Selective Suppression of CYP3A4 mRNA and Enzyme Activity by Epidermal Growth Factor in Plated Human Hepatocytes [0.03%]
表皮生长因子选择性地抑制人类肝细胞中CYP3A4 mRNA和酶活性
J George Zhang,Duan Wang,Thuy Ho et al.
J George Zhang et al.
Background: Epidermal Growth Factor (EGF) is a well-known mitogen that has importance in cell proliferation and differentiation. This property has led to the common use of EGF as an additive to some cell culture media. EG...
Therapeutic Potentials and Cytochrome P450-Mediated Interactions Involving Herbal Products Indicated for Diabetes Mellitus [0.03%]
糖尿病治疗的潜在疗法及中药与细胞色素P450介导的相互作用
Cyprian O Onyeji,Sharon I Igbinoba,Gbola Olayiwola
Cyprian O Onyeji
Background: There has been an increase in the use of herbal products to complement conventional drugs in the treatment of various diseases especially in developing countries. This may be attributable to the potential cost...
Analysis of Elevated Levels of Nandrolone Decanoate Induced Cytochrome- P450 Alterations in Mice [0.03%]
nandrolone decanoate诱导的小鼠细胞色素P450变化分析
Parmita Chowdhury,Rita Mahanta
Parmita Chowdhury
Background: Frequent recreational use of Anabolic Androgenic Steroids (AAS) is an instance of substance abuse which mimics the status of a natural hormone and upon prolonged exposure may lead to adverse drug reactions. Th...
Genotoxicity of 4-(piperazin-1-yl)-8-(trifluoromethyl)pyrido[2,3-e][1,2,4] triazolo[4,3-a]pyrazine, a Potent H4 Receptor Antagonist for the Treatment of Allergy: Evidence of Glyoxal Intermediate Involvement [0.03%]
一种有效的H4受体拮抗剂的遗传毒性：4-(哌嗪-1-基)-8-(三氟甲基)吡啶并[2,3-e][1,2,4]三氮杂萘并[4,3-a]吡嗪[potential highly toxic]的遗传毒性：焦谷氨酸中间体参与证据
Mithat Gunduz,Amanda L Cirello,Peter Klimko et al.
Mithat Gunduz et al.
Background: 4-(piperazin-1-yl)-8-(trifluoromethyl)pyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazine (1) is a small-molecule which demonstrated a sub-nM inhibitory potency toward the histamine H4 receptor (H4R). However, it was ...
The Effects of Drug Metabolizing Enzyme Inhibitors on Hepatic Efflux and Uptake Transporters [0.03%]
药物代谢酶抑制剂对肝脏外排和摄取转运蛋白的影响
Jonathan Cheong,Jason S Halladay,Emile Plise et al.
Jonathan Cheong et al.
Background: Non-selective chemical inhibitors of phase I and phase II enzymes are commonly used in in vitro metabolic studies to elucidate the biotransformation pathways of drugs. However, the inhibition of the inhibitors...
Investigation of Ocular Bioactivation Potential and the Role of Cytochrome P450 2D Enzymes in Rat [0.03%]
大鼠眼内生物活化潜力及细胞色素P450 2D酶作用的研RID198究
Jennifer L Dumouchel,Upendra A Argikar,Jaimie Spear et al.
Jennifer L Dumouchel et al.
Background: Timolol is clinically administered topically (ocular) to reduce intraocular pressure and treat open-angle glaucoma. Ocular administration of timolol in low doses (0.5% w/v in the form of eye drops) has led to ...