Age (juvenile to aged) and sex effects on in vitro CYP2A6 enzyme activity in African green monkeys using nicotine and coumarin [0.03%]
非洲绿猴的体外CYP2A6酶活性与年龄和性别之间的关系：尼古丁和香豆素的作用
Weilong Gu,Rachel F Tyndale
Weilong Gu
CYP2A6 is the principal human enzyme metabolizing coumarin and nicotine; it demonstrates wide variation from genetics and environmental regulation, complicating the determination of human developmental profile and sex-related differences. A...
Loss of palmitoylation impacts the interaction between the organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 [0.03%]
棕榈酰化损失影响有机阴离子转运多肽(OATP)1B1和OATP1B3的相互作用
Cecilia E Villanueva,Whitney M Nolte,Priscilla Flores-Ascencio et al.
Cecilia E Villanueva et al.
The organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 are hepatic transporters that mediate the uptake of numerous therapeutics like antibiotics and statins. Various post-translational modifications, eg, phosphorylation and glyc...
Advances in organ-on-chip for drug transporter study: Key insights and hurdles [0.03%]
器官芯片在药物转运体研究中的进展：关键见解与挑战
Isy Petit,Jean-Sébastien Bernard,Quentin Faucher et al.
Isy Petit et al.
Membrane transporters play a central role in the absorption, distribution, metabolism, and elimination of drugs. Beyond drug handling, these transporters regulate the transport of endogenous metabolites, contributing to physiological homeos...
Cytochrome P450-mediated metabolism of K31, a Ko143-derived ATP-binding cassette subfamily G member 2 inhibitor [0.03%]
K31的细胞色素P450介导代谢作用，K31是由Ko143衍生的ATP结合盒子G成员2抑制剂
Fu-Ying Qin,Junjie Zhu,Bjoern Brixius et al.
Fu-Ying Qin et al.
Ko143 is a potent inhibitor of ATP-binding cassette subfamily G member 2, but its development is limited by poor metabolic stability due to rapid ester hydrolysis. To address this limitation, K31, an amide analog of Ko143, was recently deve...
In vitro reversible enzyme inhibition assays to predict drug-drug interactions: Current state and industry perspective from the IQ Consortium Enzyme Inhibition Working Group [0.03%]
体外可逆酶抑制试验预测药物相互作用的现状及IQ共识组织酶抑制工作组的行业观点
Carlo Sensenhauser,Sarah M Glass,Upendra P Dahal et al.
Carlo Sensenhauser et al.
Inhibition of drug-metabolizing enzymes such as P450s and uridine 5'-diphosphoglucuronosyltransferase is routinely evaluated in drug discovery and development. Substantial efforts have been made over the years to standardize in vitro assay ...
Physiologically based pharmacokinetics of dexamethasone in rats featuring nonlinear tissue binding [0.03%]
基于生理的糖皮质激素类药物地塞米松在大鼠体内非线性组织结合的动力学特征分析模型研究
Wensi Wu,Nitheesh Yanamandala,William J Jusko
Wensi Wu
Dexamethasone (DEX) is a synthetic glucocorticoid used to manage severe inflammatory conditions, including cytokine release syndrome and autoimmune diseases. Although DEX pharmacokinetics (PK) have been characterized in healthy and inflamed...
Hiroshi Yamazaki
Hiroshi Yamazaki
Proteomic profiling of metabolizing enzymes and transporters in 2 layers of Caucasian human skin [0.03%]
人皮肤角质层和颗粒层代谢酶和转运体的蛋白质组学分析
Seun Seriki,Amin Rostami-Hodjegan,Stacey Warwood et al.
Seun Seriki et al.
Topical and transdermal drug and cosmetic development is advancing across industry; however, the efforts may in part be hindered by paucity of data on the fate of chemicals in human skin, which depend on protein-mediated transport and biotr...
Synergistic hepatotoxicity of azithromycin and acetaminophen involves liver X receptor α-mediated metabolic dysregulation and endoplasmic reticulum stress [0.03%]
阿奇霉素和对乙酰氨基酚联合作用于肝的毒性涉及代谢紊乱及内质网应激
Jiangping Li,Jun Li,Wenhong Zhou et al.
Jiangping Li et al.
Coadministration of azithromycin (AZM) and acetaminophen (APAP) is associated with an increased risk of hepatotoxicity, the underlying mechanism for which remains unclear. Here, we demonstrate that combined AZM and APAP treatment induced li...
Virtual special section: Sex and hormonal influences on drug metabolism and disposition, and related studies [0.03%]
虚拟专题：性激素对药物代谢动力学的影响及相关研究
David S Riddick
David S Riddick