The 2-Hydroxyiminostilbene Metabolite of Carbamazepine or the Supernatant from Incubation of Hepatocytes with Carbamazepine Activates Inflammasomes: Implications for Carbamazepine-Induced Hypersensitivity Reactions [0.03%]
卡马西匹2-羟氨基茋代谢产物或肝细胞孵育液诱发炎性体活化：与卡马西平引起的过敏反应的关系
Ryuji Kato,Yoshio Ijiri,Tetsuya Hayashi et al.
Ryuji Kato et al.
Although the pathophysiology of carbamazepine-induced idiosyncratic or hypersensitivity reactions is unclear, they are presumed to be immune mediated, involving a complex interaction between drug metabolism and activation of the immune syst...
Efavirenz Metabolism: Influence of Polymorphic CYP2B6 Variants and Stereochemistry [0.03%]
依非韦伦代谢：多态性CYP2B6基因变异和立体化学的影响
Pan-Fen Wang,Alicia Neiner,Evan D Kharasch
Pan-Fen Wang
Efavirenz (more specifically the S-enantiomer) is a cornerstone antiretroviral therapy for treatment of HIV infection. The major primary metabolite is S-8-hydroxyefavirenz, which does not have antiretroviral activity but is neurotoxic. Cyto...
Single Nucleotide Polymorphisms at a Distance from Aryl Hydrocarbon Receptor (AHR) Binding Sites Influence AHR Ligand-Dependent Gene Expression [0.03%]
远处的单核苷酸多态性影响芳香烃受体结合位点的功能及配体依赖的基因表达
Drew R Neavin,Jeong-Heon Lee,Duan Liu et al.
Drew R Neavin et al.
Greater than 90% of significant genome-wide association study (GWAS) single-nucleotide polymorphisms (SNPs) are in noncoding regions of the genome, but only 25.6% are known expression quantitative trait loci (eQTLs). Therefore, the function...
Specificity of the Redox Complex between Cytochrome P450 24A1 and Adrenodoxin Relies on Carbon-25 Hydroxylation of Vitamin-D Substrate [0.03%]
维甲酸-D底物碳-25羟基化决定细胞色素P450 24A1和肾上腺素铁氧蛋白间的氧化还原复合体的特异性
Amit Kumar,D Fernando Estrada
Amit Kumar
Metabolic deactivation of 1,25(OH)2D3 is initiated by modification of the vitamin-D side chain, as carried out by the mitochondrial cytochrome P450 24A1 (CYP24A1). In addition to its role in vitamin-D metabolism, CYP24A1 is involved in cata...
In Vitro Drug-Drug Interaction Evaluation of GalNAc Conjugated siRNAs Against CYP450 Enzymes and Transporters [0.03%]
N-乙酰半乳糖胺偶联的siRNA药物对CYP450酶和转运体的药动学相互作用的体内评价
Diane Ramsden,Jing-Tao Wu,Brad Zerler et al.
Diane Ramsden et al.
Small interfering RNAs (siRNAs) represent a new class of medicines that are smaller (∼16,000 Da) than biologic therapeutics (>150,000 Da) but much larger than small molecules (3000-fold above the therapeutic clinical C max at steady state,...
Drug Concentration Asymmetry in Tissues and Plasma for Small Molecule-Related Therapeutic Modalities [0.03%]
小分子药物组织与血浆浓度不对称性分析及其对治疗模式的影响研究
Donglu Zhang,Cornelis E C A Hop,Gabriela Patilea-Vrana et al.
Donglu Zhang et al.
The well accepted "free drug hypothesis" for small-molecule drugs assumes that only the free (unbound) drug concentration at the therapeutic target can elicit a pharmacologic effect. Unbound (free) drug concentrations in plasma are readily ...
GDC-0810 Pharmacokinetics and Transporter-Mediated Drug Interaction Evaluation with an Endogenous Biomarker in the First-in-Human, Dose Escalation Study [0.03%]
首个剂量递增研究中的药代动力学及基于内源性生物标志物的药物相互作用评估研究报告：GDC-0810案例
Kit Wun Kathy Cheung,Kenta Yoshida,Sravanthi Cheeti et al.
Kit Wun Kathy Cheung et al.
GDC-0810 (Cheeti et al., 2018) is an orally bioavailable, selective estrogen receptor (ER) degrader developed to treat ER-positive breast cancer. A first-in-human (FIH) dose escalation phase I study (n = 41) was conducted to characterize th...
SULT4A1 Protects Against Oxidative-Stress Induced Mitochondrial Dysfunction in Neuronal Cells [0.03%]
硫代谢物SULT4A1保护神经元细胞免受氧化应激诱导的线粒体功能障碍
Mohammed I Hossain,Joshua M Marcus,Jun Hee Lee et al.
Mohammed I Hossain et al.
Sulfotransferase 4A1 (SULT4A1), a member of cytosolic sulfotransferases (SULT), is exclusively expressed in neurons with no known function. Severe phenotype and early postnatal death in SULT4A1 knockout mice revealed that SULT4A1 is an esse...
Interactions between Maraviroc and the ABCB1, ABCG2, and ABCC2 Transporters: An Important Role in Transplacental Pharmacokinetics [0.03%]
马拉韦罗与ABCB1、ABCG2和ABCC2转运体之间的相互作用：胎盘转运药代动力学中的重要作用
Lenka Tupova,Martina Ceckova,Csilla Ambrus et al.
Lenka Tupova et al.
Maraviroc is a chemokine receptor 5 (CCR5) inhibitor used in the treatment of human immunodeficiency virus (HIV) that also shows therapeutic potential for several autoimmune, cancer, and inflammatory diseases that can afflict pregnant women...