Methyltransferase Like-3-Mediated N6-Methyladenosine Modification of Long Noncoding RNA Hepatocyte Nuclear Factor 1a Antisense RNA 1/Hepatocyte Nuclear Factor 4a Antisense RNA 1 Regulates Cytochrome P450 Enzyme Expression [0.03%]
N6-甲基腺苷修饰长链非编码RNA肝细胞核因子1A反义RNA1/肝细胞核因子4A反义RNA1的甲基转移酶类似物3介导调控细胞色素P450表达
Yihang Yu,Jingya Wang,Zaihuan Xiong et al.
Yihang Yu et al.
Interindividual variations in the expression and activity of cytochrome P450 enzymes (CYPs) led to lower therapeutic efficacy or adverse drug events. We previously demonstrated that CYPs are regulated by the long noncoding RNAs (lncRNAs) he...
Clotrimazole Identified as a Selective UGT2B4 Inhibitor Using Canagliflozin-2'- O-Glucuronide Formation as a Selective UGT2B4 Probe Reaction [0.03%]
特比萘芬是一种选择性的UGT2B4抑制剂：利用坎地硫胺-2'-O-葡萄糖醛酸的形成作为特异性UGT2B4探针反应被鉴定出来
Kimberly Lapham,Nicholas Ferguson,Mark Niosi et al.
Kimberly Lapham et al.
UGT2B4 is a highly expressed drug-metabolizing enzyme in the liver contributing to the glucuronidation of several drugs. To enable quantitatively assessing UGT2B4 contribution toward metabolic clearance, a potent and selective UGT2B4 inhibi...
The Pharmacokinetics, Metabolism, and Clearance Mechanisms of Ritlecitinib, a Janus Kinase 3 and Tyrosine-Protein Kinase Family Inhibitor, in Humans [0.03%]
人源Janus激酶3和酪氨酸蛋白激酶家族抑制剂瑞替累替尼的药代动力学、代谢及清除机制
Jonathan N Bauman,Angela C Doran,Gabrielle M Gualtieri et al.
Jonathan N Bauman et al.
Ritlecitinib is an oral once-daily irreversible inhibitor of Janus kinase 3 and tyrosine-protein kinase family being developed for the treatment of moderate-to-severe alopecia areata. This study examined the disposition of ritlecitinib in m...
Utility of Chimeric Mice with Humanized Livers for Predicting Hepatic Organic Anion-Transporting Polypeptide 1B-Mediated Clinical Drug-Drug Interactions [0.03%]
人源肝嵌合小鼠预测有机阴离子肽转运蛋白1B介导的临床药物相互作用的用途
Bo Feng,Guiqing Liang,Craig Zetterberg et al.
Bo Feng et al.
The influence of transporters on the pharmacokinetics of drugs is being increasingly recognized, and drug-drug interactions (DDIs) via modulation of transporters could lead to clinical adverse events. Organic anion-transporting polypeptide ...
Proof of Concept of an All-in-One System for Measuring Hepatic Influx, Egress, and Metabolic Clearance Based on the Extended Clearance Concept [0.03%]
基于扩展清除概念的测量肝流入、流出和代谢清除的一体化系统验证
Julia A Schulz Pauly,Elizabeth Sande,Mei Feng et al.
Julia A Schulz Pauly et al.
Hepatic clearance (CLH ) prediction is a critical parameter to estimate human dose. However, CLH underpredictions are common, especially for slowly metabolized drugs, and may be attributable to drug properties that pose challenges for conve...
Predicting Clearance with Simple and Permeability-Limited Physiologically Based Pharmacokinetic Frameworks: Comparison of Well-Stirred, Dispersion, and Parallel-Tube Liver Models [0.03%]
基于简单的生理药代动力学框架预测清除率和渗透性限制：全混均一、弥散和并联管肝模型的比较
Swati Nagar,Rachel Parise,Ken Korzekwa
Swati Nagar
One-compartment (1C) and permeability-limited models were used to evaluate the ability of microsomal and hepatocyte intrinsic clearances to predict hepatic clearance. Well-stirred (WSM), parallel-tube (PTM), and dispersion (DM) models were ...
Development of a Novel HEK293 Cell Model Lacking SLC29A1 to Study the Pharmacology of Endogenous SLC29A2-Encoded Equilibrative Nucleoside Transporter Subtype 2 [0.03%]
一种新型的缺乏SLC29A1的HEK293细胞模型的发展，用于研究内源性SLC29A2编码的平衡核苷转运子亚型2的药理学
Nayiar Shahid,Christopher Cromwell,Basil P Hubbard et al.
Nayiar Shahid et al.
Equilibrative nucleoside transporters (ENTs) mediate the transmembrane flux of endogenous nucleosides and nucleoside analogs used clinically. The predominant subtype, ENT1, has been well characterized. However, the other subtype, ENT2, has ...
Shining a Light on Inflammation as a Critical Modulator of Drug Metabolism [0.03%]
炎症作为药物代谢的关键调节因子的研究进展
Edward T Morgan
Edward T Morgan
Since his graduate studies on alcohol induction of a novel cytochrome P450 (P450) enzyme, through his postdoctoral work on hormonal regulation of sexually differentiated cytochrome P450s (P450s), the author has maintained an interest in the...
Impact of OATP2B1 on Pharmacokinetics of Atorvastatin Investigated in rSlco2b1-Knockout and SLCO2B1-Knockin Rats [0.03%]
OATP2B1对阿托伐他汀药动学影响的研究：rSlco2b1敲除和SLCO2B1人源化大鼠模型效应的比较
Jonny Kinzi,Janine Hussner,Isabell Seibert et al.
Jonny Kinzi et al.
The organic anion transporting polypeptide (OATP) 2B1 is considered an emerging drug transporter that is found expressed in pharmacokinetically relevant organs such as the liver, small intestine, and kidney. Despite its interaction with var...
Metabolism and Excretion of [14C]Mobocertinib, a Selective Covalent Inhibitor of Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertion Mutations, in Healthy Male Subjects [0.03%]
健康男性受试者中莫博赛替尼[14C]的代谢和排泄研究：莫博赛替尼是一种选择性共价结合表皮生长因子受体（EGFR）第20号外显子插入突变抑制剂
Hao Chen,Abhi Shah,Suguru Kato et al.
Hao Chen et al.
Mobocertinib (formerly known as TAK-788) is a targeted covalent tyrosine kinase inhibitor of epidermal growth factor receptor with exon 20 insertion mutations. This article describes the metabolism and excretion of mobocertinib in healthy m...