Computational Prediction of the Site(s) of Metabolism and Binding Modes of Protein Kinase Inhibitors Metabolized by CYP3A4 [0.03%]
CYP3A4代谢的蛋白激酶抑制剂的代谢位点的计算预测及其与蛋白质结合模式
Pramod C Nair,Ross A McKinnon,John O Miners
Pramod C Nair
Protein kinase inhibitors (KIs), which are mainly biotransformed by CYP3A4-catalyzed oxidation, represent a rapidly expanding class of drugs used primarily for the treatment of cancer. Ligand- and structure-based methods were applied here t...
Developmental Expression of the Cytosolic Sulfotransferases in Human Liver [0.03%]
人肝脏中细胞质硫酸转移酶的表达式变化
Sarah Dubaisi,Joseph A Caruso,Roger Gaedigk et al.
Sarah Dubaisi et al.
The liver is the predominant organ of metabolism for many endogenous and foreign chemicals. Cytosolic sulfotransferases (SULTs) catalyze the sulfonation of drugs and other xenobiotics, as well as hormones, neurotransmitters, and sterols, wi...
Mechanistic Evaluation of the Complex Drug-Drug Interactions of Maraviroc: Contribution of Cytochrome P450 3A, P-Glycoprotein and Organic Anion Transporting Polypeptide 1B1 [0.03%]
马拉韦罗复杂药物相互作用的机制评价：细胞色素P450 3A、p-糖蛋白和有机阴离子转运多肽1B1的作用贡献
Emi Kimoto,Manoli Vourvahis,Renato J Scialis et al.
Emi Kimoto et al.
The aim of the present study was to quantitatively evaluate the drug-drug interactions (DDIs) of maraviroc (MVC) with various perpetrator drugs, including telaprevir (TVR), using an in vitro data-informed physiologically based pharmacokinet...
A Novel Depurination Methodology to Assess DNA Alkylation of Chloro-Bis-Seco-Cyclopropylbenzoindoles Allowed for Comparison of Minor-Groove Reactivity [0.03%]
一种新颖的脱氨基方法用于评估氯代-双-环丙基苯并吲哚类化合物DNA烷基化，可用于比较其与小沟反应性的影响
Shuai Wang,Buyun Chen,Peter Dragovich et al.
Shuai Wang et al.
Duocarmycins [including cyclopropyl pyrroloindole (CPI) or cyclopropyl benzoindole (CBI)] are a class of DNA minor-groove alkylators and seco-CPI/CBIs are synthetic pro-forms that can spirocyclize to CPI/CBI. Bis-CPI/CBIs are potential drug...
Role of ABCG2 in Secretion into Milk of the Anti-Inflammatory Flunixin and Its Main Metabolite: In Vitro-In Vivo Correlation in Mice and Cows [0.03%]
ABCG2在抗炎药氟尼辛及其主要代谢物分泌入乳中的作用：小鼠和奶牛的体外-体内相关性研究
Dafne Garcia-Mateos,Alba Maria Garcia-Lino,Indira Alvarez-Fernandez et al.
Dafne Garcia-Mateos et al.
Flunixin meglumine is a nonsteroidal anti-inflammatory drug (NSAID) widely used in veterinary medicine. It is indicated to treat inflammatory processes, pain, and pyrexia in farm animals. In addition, it is one of the few NSAIDs approved fo...
In Vitro Inhibition of Carboxylesterase 1 by Major Cannabinoids and Selected Metabolites [0.03%]
大麻主要成分及选择性代谢产物对羧酸酯酶1的体外抑制作用
Yuli Qian,Xinwen Wang,John S Markowitz
Yuli Qian
The escalating use of medical cannabis and significant recreational use of cannabis in recent years has led to a higher potential for metabolic interactions between cannabis or one or more of its components and concurrently used medications...
Factors Affecting Interindividual Variability of Hepatic UGT2B17 Protein Expression Examined Using a Novel Specific Monoclonal Antibody [0.03%]
新型特异性单克隆抗体检测肝UGT2B17蛋白表达的个体差异及影响因素
Jean-Philippe Émond,Adrien Labriet,Sylvie Desjardins et al.
Jean-Philippe Émond et al.
Accurate quantification of the metabolic enzyme uridine diphospho-glucuronosyltransferase (UGT) UGT2B17 has been hampered by the high sequence identity with other UGT2B enzymes (as high as 94%) and by the lack of a specific antibody. Knowin...
Mechanistic Assessment of Extrahepatic Contributions to Glucuronidation of Integrase Strand Transfer Inhibitors [0.03%]
整合酶链转移抑制剂葡萄糖醛酸化的肝外代谢机制评估研究
Stephanie N Liu,Jessica Bo Li Lu,Christy J W Watson et al.
Stephanie N Liu et al.
Integrase strand transfer inhibitor (INSTI)-based regimens dominate initial human immunodeficiency virus treatment. Most INSTIs are metabolized predominantly via UDP-glucuronosyltransferases (UGTs). For drugs predominantly metabolized by UG...