Evaluating plasma carboxylesterase 1 as a protein biomarker for pharmacokinetics and metabolic dysfunction-associated steatotic liver disease [0.03%]
血浆羧酸酯酶1作为药代动力学和代谢功能异常相关脂肪变性肝病的蛋白质生物标志物的评价研究
Sun Min Jung,Hui Yu,Xinwen Wang et al.
Sun Min Jung et al.
Carboxylesterase 1 (CES1) is the most abundant hepatic hydrolase responsible for metabolizing many clinically important medications. Hepatic CES1 also plays a role in regulating lipid homeostasis. This study aimed to determine whether plasm...
An in vitro approach to predict idiosyncratic drug-induced agranulocytosis using myeloperoxidase-derived reactive metabolites [0.03%]
一种体外预测药物引起异质性粒细胞缺乏症的方法 使用源于髓过氧化物酶的反应性代谢产物
Tomoyuki Kawachi,Tatsuki Fukami,Miki Nakajima
Tomoyuki Kawachi
Idiosyncratic drug-induced agranulocytosis (iDIAG) is a rare but potentially life-threatening adverse reaction characterized by an absolute neutrophil count of fewer than 500 cells/μL. Owing to its complex and poorly understood mechanisms,...
Metabolism of the ionizable lipid SM-102 in liver microsomes, 2D hepatocytes, and 3D liver spheroids [0.03%]
肝微粒体、二维肝细胞和三维肝球体中可离子化脂质SM-102的代谢产物分析
Bo Sun,Zihui Jin,Xinwei Li et al.
Bo Sun et al.
Recent advances in lipid nanoparticle (LNP) delivery systems have enabled the development of mRNA vaccines and oligonucleotide therapeutics. Reliable hepatic in vitro systems are essential for the evaluation of the biodegradation of LNP com...
The effects of amiodarone or dexamethasone on diclofenac-induced hepatotoxicity: Implications of P450s and SIRT1/Nrf2/NF-κb signaling pathways [0.03%]
胺碘酮或.dex核索对diclofenac致肝毒性的效应：P450和SIRT1/Nrf2/NF-κB信号通路的意义
Lamiaa A Khatab,Ihab T Abdel-Raheem,Asser I Ghoneim
Lamiaa A Khatab
Cytochrome P450 (P450)-mediated metabolism may contribute to diclofenac (DCF)-induced hepatotoxicity via reactive metabolites that damage cellular biomolecules. Several drugs inhibit or induce the P450 enzymes and affect DCF hepatotoxicity ...
Biphasic dextromethorphan O-demethylation in tree shrews mediated by liver microsomal cytochromes P450 with high and low affinities [0.03%]
高亲和力和低亲和力的树鼩肝脏微粒体细胞色素P450酶介导的右美沙芬 biphasic O-脱甲基化反应
Genki Ushirozako,Atsushi Asano,Konosuke Otomaru et al.
Genki Ushirozako et al.
Tree shrews (Tupaia belangeri) are nonprimate animal species available for use in biomedical studies. Because the molecular and enzymatic properties of their cytochromes P450 (P450s or CYPs) are similar to human P450s, tree shrews are a pro...
A CYP3A7 metabolically competent human induced pluripotent stem cell-derived hepatocyte-like cell (hHLC3A7) model for drug safety assessment in the newborn [0.03%]
一种用于新生儿药物安全性评估的CYP3A7代谢功能正常的由人诱导多能干细胞来源的肝样细胞（hHLC3A7）模型
Emily G Gracey,Sylvie E Kandel,Jed N Lampe
Emily G Gracey
Drug safety assessment in newborns is limited by ethical constraints and the fact that no appropriate human-relevant in vitro hepatic cell model system currently exists to study and predict drug metabolism and disposition in this fragile po...
Potential herb-drug interaction risk of Sedum sarmentosum Bunge extract and cyclosporine A [0.03%]
石上柏提取物与环孢素A相互作用的可能性研究
Mengling Hou,Shaofei Song,Dali Gan et al.
Mengling Hou et al.
Sedum sarmentosum Bunge extract (SSBE) is widely used in clinical practice to treat various liver diseases. Cyclosporine A (CsA) is a potent immunosuppressant known to cause hepatotoxicity. However, it is unclear whether combining SSBE and ...
Identification of alcohol dehydrogenase (ADH) isoforms catalyzing hydroxyzine oxidation using recombinant human ADH: Serendipitous finding of potent ADH inhibition by organic solvents [0.03%]
利用重组人酒精脱氢酶鉴定羟嗪氧化的酒精脱氢酶（ADH）同工酶：有机溶剂意外地强力抑制酒精脱氢酶作用的发现
Takuya Tonami,Rei Sato,Masataka Nakano et al.
Takuya Tonami et al.
Hydroxyzine, an aliphatic alcohol, is metabolized to the carboxylic acid cetirizine via 2 sequential oxidation steps involving the formation of an aldehyde intermediate. The initial aldehyde formation is considered the rate-limiting step in...
Comparative evaluation of ultrafiltration and EMSA formats for siRNA plasma protein binding: Methodological determinants and artifacts [0.03%]
siRNA与血浆蛋白结合的超滤评价及免疫印迹法格式：方法论决定因素及伪像现象评估
Jie Wang,Mengying Li,Laiwen Fang et al.
Jie Wang et al.
Plasma protein binding (PPB) is a critical pharmacokinetic parameter that modulates renal clearance and systemic safety of therapeutic small interfering RNAs (siRNAs), yet measurements vary significantly across methods. We compared ultrafil...
CYP3A5 polymorphism affects the disposition of tacrolimus and its metabolite in systemic circulation and peripheral tissues of mice introduced with the CYP3A5 gene [0.03%]
CYP3A5多态性影响小鼠体内移植CYP3A5基因后他克莫司及其代谢产物在全身循环和外周组织中的分布
Genki Minegishi,Yuna Hiramatsu,Manami Sugahara et al.
Genki Minegishi et al.
The CYP3A5∗3 allele, which leads to a splicing defect resulting in the absence of the CYP3A5 protein, is the prevalent variant in most populations. Tacrolimus dose is individualized for each patient because the CYP3A5 polymorphism impacts ...