A Pharmacokinetic-Pharmacodynamic Model of Tamoxifen and Endoxifen to Predict Their Distribution and Effects on Inhibition of Tumor Growth [0.03%]
他莫昔芬和恩多昔芬的药代动力学-药效学模型及其对抑瘤作用分布的预测
Shengyue Yuan,Qingrong Sun,Yao Chen et al.
Shengyue Yuan et al.
Background: Tamoxifen is widely used in the therapy for breast cancer and has three major metabolites, N-desmethyltamoxifen, 4-hydroxytamoxifen, and endoxifen. Endoxifen has played a major role in the inhibition of tumor ...
Quantification of Sulfotransferases 1A1 and 1A3/4 in Tissue Fractions and Cell Lines by Multiple Reaction Monitoring Mass Spectrometry [0.03%]
基于多重反应监测质谱法的组织亚分数及细胞系中硫酸转移酶1A1和1A3/4的定量分析方法研究
Sho Yoshitake,Melissa McKay-Daily,Masaki Tanaka et al.
Sho Yoshitake et al.
Background: Within the sulfotransferase (SULT) superfamily of metabolic enzymes, SULT1A1 and 1A3/4 isoforms are of particular interest, due to their abilities to catalyze the sulfation of phenolic endobiotics and xenobiot...
Mixed Matrix Method Provides A Reliable Metabolite Exposure Comparison for Assessment of Metabolites in Safety Testing (MIST) [0.03%]
混合矩阵法提供了代谢物暴露比较的可靠方法以供进行安全测试中的代谢物评估(MIST)
Ryan H Takahashi,Cyrus Khojasteh,Matthew Wright et al.
Ryan H Takahashi et al.
Background: The regulatory guidances on metabolites in safety testing (MIST) by US Food and Drug Administration (FDA) and International Conference on Harmonisation (ICH) describe the necessity to assess exposures of major...
Comparative Study
Drug metabolism letters. 2017 Nov 17;11(1):21-28. DOI:10.2174/1872312811666170710193229 2017
Masatoshi Masuda,Tsutomu Fujiwara,Masayuki Matsunaga et al.
Masatoshi Masuda et al.
Background: CYP2D6 is one of the most significant polymorphic genes of drugmetabolizing enzymes due to its association with different metabolic activities and the pharmacokinetics of CYP2D6 substrates. ...
The Role of Placental Carbonyl Reducing Enzymes in Biotransformation of Bupropion and 4-methylnitrosamino-1-(3-pyridyl)-1-butanone [0.03%]
胎盘醛还原酶在盐酸舍曲林和4-(甲基亚硝胺)-1-(苯基)-(1-丁酮)生物转化中的作用研究
Valentina M Fokina,Svetlana L Patrikeeva,Cheryl Oncken et al.
Valentina M Fokina et al.
Background: Bupropion (BUP) has a potential to be an effective pharmacotherapy for smoking cessation during pregnancy. Smoking during pregnancy stimulates placental carbonyl reductases that catalyze the biotransformation ...
Metabolic Profile of Flunitrazepam: Clinical and Forensic Toxicological Aspects [0.03%]
氟硝西泮的代谢谱及其临床和法医毒理学意义
Ricardo Jorge Dinis-Oliveira
Ricardo Jorge Dinis-Oliveira
Background: Flunitrazepam (FNZ) is a potent hypnotic, sedative, and amnestic drug used to treat insomnia and as a pre-anesthetic agent. The illicit practice in drug-facilitated sexual assault led to important clinical and...
Effects of Fenofibrate on the Expression of Small Heterodimer Partner (SHP) and Cytochrome P450 (CYP) 2D6 [0.03%]
非诺贝特对小异源二聚体伴侣(SHP)和细胞色素P450(CYP)2D6表达的影响
Rebecca Kent,Hyunyoung Jeong
Rebecca Kent
Background: Cytochrome P450 (CYP) 2D6 is a major drug-metabolizing enzyme, responsible for eliminating 25% of marketed drugs. We recently identified SHP as a negative regulator of CYP2D6 expression and showed that factors...
Gender Difference of Hepatic and Intestinal CYP3A4 in CYP3AHumanized Mice Generated by a Human Chromosome-engineering Technique [0.03%]
通过人类染色体工程技术建立的人肝肠CYP3A4性别差异研究小鼠模型
Kaoru Kobayashi,Chihiro Abe,Mika Endo et al.
Kaoru Kobayashi et al.
Background: Cytochrome P450 3A4 (CYP3A4) is an important drug-metabolizing enzyme that is expressed in the liver and small intestine of humans. Various factors influence the expression of CYP3A4, but gender difference in ...
Inhibitory Effect of Fruit Juices on the Doxorubicin Metabolizing Activity of Carbonyl Reductase 1 [0.03%]
果汁对карбонильдегидрат редуктаза 1型多柔比星代谢活性的抑制作用
Takeshi Miura,Katsutoshi Nagai,Shingo Kaneshiro et al.
Takeshi Miura et al.
Background and objective: Doxorubicin, an anthracycline anti-cancer drug, is effective for breast cancer and childhood lymphoma. Chronic cardiotoxicity has been known as a critical adverse effect of doxorubicin and is att...
Obesity and Inflammation and Altered Clopidogrel Pharmacokinetics and Pharmacodynamics [0.03%]
肥胖、炎症与氯吡格雷药动学和药效学异常的关系
Nicholas B Norgard,Scott V Monte
Nicholas B Norgard
Background: Clopidogrel is a key antiplatelet drug that has substantial interpatient variability in pharmacodynamic response. Patients with lesser degrees of platelet inhibition in response to clopidogrel appear to be at ...