Structural context of NADPH-cytochrome P450 reductase mutations that alter cytochrome P450 1A2 substrate regioselectivity [0.03%]
NADPH-细胞色素P450还原酶突变体的结构背景，这些突变体改变了细胞色素P450 1A2底物区域选择性
Sarah D Burris-Hiday,Francisco Esteves,Michel Kranendonk et al.
Sarah D Burris-Hiday et al.
NADPH-cytochrome P450 (P450) reductase serves as the obligate redox partner for the majority of human P450 enzymes, those responsible for both drug metabolism and homeostasis. NADPH-derived electrons are accepted by the reductase FAD-contai...
Evaluation of the disconnect between hepatocyte and microsomal intrinsic clearance at intracellular and extracellular pH [0.03%]
评估肝细胞和微粒体固有清除率在细胞内和细胞外pH值之间的差异
Christine Katharina Maurer,Zhizhou Fang,Stephanie Harlfinger et al.
Christine Katharina Maurer et al.
In vitro-in vivo extrapolation using human hepatocytes (HHs) and human liver microsomes (HLMs) is a well established method for predicting metabolic blood clearance. Typically, in vitro incubations with HLM are conducted at an extracellular...
High-Altitude Hypoxia Dysregulates the Organic Anion Transport Network to Alter Acetazolamide Disposition and Renal Metabolic Homeostasis: Validation of the Remote Sensing and Signaling Theory [0.03%]
高原低氧通过有机阴离子转运系统调控失常致乙酰唑胺药动学变化及肾脏代谢稳态失衡：支持远程感知与信号传导理论的证据
Bohong Zheng,Mengran Wang,Jingtao Wang et al.
Bohong Zheng et al.
Acute high-altitude hypoxia (AHH) disrupts systemic homeostasis and alters the pharmacokinetic (PK) profiles of drugs, yet the role of the organic anion transport network in mediating altered drug disposition and the link to regulation by t...
MegaTrans-machine learning models for drug transporters corresponding to the FDA guidance [0.03%]
基于FDA指南的药物转运体机器学习模型-MegaTrans
Patricia A Vignaux,Melanie Tojong,Alexander Kyu et al.
Patricia A Vignaux et al.
Regulatory guidances (eg, FDA and European Medicines Agency) require an understanding of the interactions of novel drugs, natural products, and environmental toxicants with key transporters to avoid compounds with undesirable side effects. ...
Advancing precision treatment in preterm infants: Population pharmacokinetics of caffeine for apnea of prematurity [0.03%]
早产儿精确治疗研究进展：应用于呼吸暂停的咖啡因药代动力学模型研究
Yaodong He,Xianhuan Shen,Sengpeng Wong et al.
Yaodong He et al.
This study aimed to develop a population pharmacokinetic (PopPK) model for caffeine in apnea of prematurity, identify clinically significant covariates that influence pharmacokinetic (PK) parameters, and establish an evidence-based, individ...
A minimal physiologically based pharmacokinetic model for predicting the metabolism of tenofovir prodrugs in the liver of human with fibrosis [0.03%]
用于预测人类肝纤维化肝脏中替诺福韦前药代谢的最小生理药代动力学模型
Hua He,Jinwei Zhu,Jiahao Chen et al.
Hua He et al.
The antiviral efficacy of tenofovir (TFV) prodrugs is dependent on their intracellular conversion to the active metabolite, TFV diphosphate (TFV-DP). Because hepatitis B virus principally infects hepatocytes, accurate quantification of intr...
In Vitro Reaction Phenotyping and Projection of Drug Interactions Mediated by Cytochrome P450 Enzymes for Central Nervous System Drugs as Victims: Implications for Safety in Vulnerable Populations [0.03%]
体外反应表型测定和中枢神经系统药物作为受者时经细胞色素P450酶介导的药物相互作用预测：对易感人群安全性的启示
Veera Raghava Chowdary Palacharla,Ramakrishna Nirogi,Nitesh Kumar et al.
Veera Raghava Chowdary Palacharla et al.
Accurate prediction of cytochrome P450-mediated victim drug-drug interactions (DDIs) is critical for the safe use of central nervous system (CNS) drugs, particularly in populations at high risk of polypharmacy. This study evaluated the util...
A drug-to-metabolite ratio-based quantitative analytical approach for evaluation of combination therapy through impact assessment of brigatinib on the pharmacokinetics of tazemetostat and its primary metabolite [0.03%]
基于药物与代谢物比率的定量分析方法评估联合用药并通过brigatinib对tazemetostat及其主要代谢产物药代动力学的影响进行评价
Niraj Rajput,Karuna Chandnani,Tarang Jadav et al.
Niraj Rajput et al.
Coadministration of multiple drugs may significantly alter each other's therapeutic profiles by altering their in vivo drug metabolism and pharmacokinetics. Quantitative profiling of metabolites along with the parent drug may be critical fo...
Development of a generic physiologically based pharmacokinetic model to predict clinical pharmacokinetics and assess drug-drug interaction risks for valine-citrulline-monomethyl auristatin E-based antibody-drug conjugates [0.03%]
缬氨霉素-单甲基奥瑞他汀E抗体药物偶联物的生理药动学模型开发及临床药动学和药物相互作用预测评估研究
Chaozhuang Shen,Rui Wang,Jiapin Yan et al.
Chaozhuang Shen et al.
Valine-citrulline-monomethyl auristatin E (vcMMAE)-based antibody-drug conjugates (ADCs) are potent anticancer therapeutics; however, the intricate kinetic interplay between the ADC and liberated monomethyl auristatin E (MMAE) complicates c...
Design, expression, purification, and application of novel recombinant miR-491 molecules to define the biogenesis and function of miR-491-3p versus -5p in posttranscriptional regulation of UDP-glucuronosyltransferase 1A1 [0.03%]
新型重组miR-491分子的设计、表达、纯化及其在定义miR-491-3P与-5P的生成以及对UDP-葡萄糖醛酸转移酶1A1的转录后调控中的作用方面的应用
Yimei Wang,Mei-Juan Tu,Neelu Batra et al.
Yimei Wang et al.
Interindividual variations in drug metabolism involve various factors, including posttranscriptional gene regulation mechanisms controlled by microRNAs (miRNAs or miRs) derived from the genome. The aim of this study was to use RNA bioengine...