P-glycoprotein-mediated impairment of doxorubicin clearance in inflammatory bowel disorders: Mechanistic insights from rat studies and whole-body physiologically based pharmacokinetic modeling [0.03%]
炎症性肠病中由P-糖蛋白介导的多柔比星清除障碍：来自大鼠研究和全身生理药动学模型的机制见解
Mo&#x;tasem M Alsmadi
Mo&#x;tasem M Alsmadi
Doxorubicin (Dox) cardiotoxicity can worsen due to increased cardiac accumulation. P-glycoprotein downregulation, common in irritable bowel syndrome (IBS) and inflammatory bowel disease (IBD), may influence Dox pharmacokinetics (PK) and car...
Characterization of fatty acid amide hydrolase 2 as a drug-metabolizing enzyme: Contribution to the hydrolysis of DS-8500a and its analogs [0.03%]
酰胺酶2的药物代谢研究及其对DS-8500a和同类化合物水解作用的贡献
Chie Makino,Takuma Chiashi,Mayumi Hayashi et al.
Chie Makino et al.
This study evaluated the properties of fatty acid amide hydrolase 2 (FAAH2) as a drug-metabolizing enzyme, specifically its substrate specificity and functionality. We used expression systems and various microsomes, with DS-8500a and its an...
Post-translational regulation of organic anion transporting polypeptide 1B3 transport function by lysine acetylation and lysine deacetylase 6 inhibition [0.03%]
乙酰化和去乙酰酶6抑制对有机阴离子转运多肽1B3运输功能的翻译后调节
Vishakha Tambe,Pascaline Niyonshuti,Vikram Aditya et al.
Vishakha Tambe et al.
Organic anion transporting polypeptide (OATP) 1B3 plays a clinically significant role in hepatic drug disposition. Lysine acetylation, a key post-translational modification, has not been investigated for OATP1B3. This study determined the l...
New strategy to quantify hepatic cytochrome P450 3A activity with deoxyschizandrin as an in vivo probe: A Vmax, app approach [0.03%]
以安格洛苷元为体内探针定量肝细胞色素P450 3A活性的新策略：表观Vmax方法
Xiaodong Li,Cong Hu,Guilin Wei et al.
Xiaodong Li et al.
Interindividual variability in drug response stems largely from metabolic enzyme activity differences, with cytochrome P450 3A (CYP3A) being the predominant enzyme whose fluctuations critically impact exposure to narrow-therapeutic-index dr...
Keratinocyte transport of notoginsenoside R1 via ABCG2: A novel mechanism for RNA N6-methyladenosine modification in UVB induced skin sunburn injury [0.03%]
表皮角质细胞中抗坏血酸通过ABCG2转运胎盘造血素的一种新机制：紫外线诱导皮肤晒伤损伤中RNA上N6-甲基腺苷修饰的新型调控方式
Xiaokang Liu,Shuyun Liang,Xiaobo Sun et al.
Xiaokang Liu et al.
UVB radiation, a major environmental carcinogen, induces cyclobutane pyrimidine dimers and contributes to the development of squamous cell carcinoma. The RNA N6-methyladenosine modification (m6A) plays a critical role in regulating the DNA ...
Tracking the spatiotemporal journey of chitosan nanoparticles across ear physiological barriers: Mechanisms and pathways [0.03%]
追踪壳聚糖纳米颗粒跨耳朵生理屏障的时空旅程：机制和途径
Dingsheng Wen,Liping Zhang,Peiwen Deng et al.
Dingsheng Wen et al.
Effective drug delivery to the inner ear is severely limited by the restrictive nature of the round window membrane (RWM). In this study, coumarin-6-labeled chitosan nanoparticles were administered via intratympanic injection in guinea pigs...
A review on integrated machine learning and deep learning driven artificial intelligence models for pharmacokinetics and toxicokinetics predictions, and their application [0.03%]
基于机器学习和深度学习的药代动力学及毒性预测人工智能模型及其应用综述
Malarvannan M,Monohar S,Sanskruti Sitaram Kate et al.
Malarvannan M et al.
The development of artificial intelligence (AI) tools and technology has made AI-driven drug discovery a more prominent field. We are firmly in the AI era, with hybrid designs that eventually comprise deep learning (DL) and conventional mac...
Combining the novel all-human co-cultured hepatocytes system with physiologically based pharmacokinetic modeling to assess the translatability of cytochrome P450 and uridine 5'-diphospho-glucuronosyltransferase induction data [0.03%]
将全人种共培养肝细胞系统与基于生理的药代动力学建模相结合，以评估细胞色素P450和尿苷二磷酸葡萄糖醛酸转移酶诱导数据的可转化性
Alessandra Pugliano,Aynur Ekiciler,Neil John Parrott et al.
Alessandra Pugliano et al.
Cytochrome P450s (CYPs) 2C subfamily (eg, 2C8, 2C9, and 2C19) and phase II enzymes such as uridine 5'-diphospho-glucuronosyltransferases (UGTs) are increasingly relevant in drug development and key targets for enzymatic induction. However, ...
Differential gene regulation by SR12813 and rifampicin: Insights into PXR and PPARγ activation and metabolic pathway modulation in LS180 colon cancer cells [0.03%]
SR12813和利福平对结肠癌LS180细胞的基因调控差异：PXR和PPARγ激活及代谢途径调节的新见解
Dan Brobst,Jack Hemsath,Abbigail Niewchas et al.
Dan Brobst et al.
SR12813 is an experimental cholesterol-lowering drug that reduces intracellular cholesterol through accelerated proteasomal degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase and is also recognized as a prototypical activator of...
Unveiling polymerization-dependent pharmacokinetics and dual oxidative metabolism of polyethylene glycol 600 oligomers in rats via ultra-high-performance liquid chromatography coupled to tandem mass spectrometry [0.03%]
基于超高液相色谱-串联质谱的聚乙二醇寡聚物聚合物依赖性药代动力学及双重氧化代谢解析研究
Jiye Tian,Jiarui Zhang,Zihan Tang et al.
Jiye Tian et al.
A comprehensive understanding of the in vivo fate of low-molecular-weight polyethylene glycol (PEG) oligomers is essential for optimizing PEGylated therapeutics. This study delineates the polymerization-dependent absorption, distribution, m...