Applications of contemporary tools to measure plasma protein binding of targeted protein degraders [0.03%]
当代工具在测量蛋白降解剂蛋白质结合中的应用
Mark Niosi,Sam Zhang,Woodrow Burchett et al.
Mark Niosi et al.
Assessing the fraction unbound in plasma (fu,p) for highly bound compounds (fu,p < 1%) is challenging, in part due to the compound-specific factors that can influence assay variability and performance. This study investigates human plasma p...
Assessing granisetron as a specific CYP1A1 substrate in primary human hepatocytes: A comprehensive evaluation for drug development studies [0.03%]
评估格拉西特ron作为初级人体肝细胞中CYP1A1的特定底物：药物开发研究中的全面评价
Ann-Kathrin Lenich,Julie Nilles,Vanessa Scherer et al.
Ann-Kathrin Lenich et al.
Cytochrome P450 (CYP) enzymes are essential in metabolic pathways and drug-drug interactions, making their investigation highly relevant during drug development. These studies are typically conducted in liver systems, where primary human he...
Sex-dependent alterations in cardiac cytochrome P450-mediated arachidonic acid metabolism in pressure overload-induced cardiac hypertrophy in rats [0.03%]
压力超负荷诱发的大鼠心脏肥厚中花生四烯酸代谢的性别差异学研究
Samar H Gerges,Sara A Helal,Heidi L Silver et al.
Samar H Gerges et al.
Cardiac hypertrophy is a risk factor for heart failure and is usually less common in young women than in men. Cytochrome P450 (CYP) enzymes in the heart metabolize arachidonic acid into hydroxyeicosatetraenoic acids (HETEs), which generally...
In vitro assessment of ATP-binding cassette transporters and their functional genetic polymorphisms on fluoroquinolone accumulation in human embryonic kidney 293 recombinant cell lines [0.03%]
人胚胎肾293重组细胞系中评估ATP结合盒转运蛋白及其功能遗传多态性对氟喹诺酮类药物积聚的影响体外研究
Gwenaëlle Mahieu,Vincent Haufroid,Françoise Van Bambeke et al.
Gwenaëlle Mahieu et al.
Fluoroquinolone tissue distribution and cellular accumulation are hindered by efflux transporters, including ATP-binding cassette subfamily B member 1 (ABCB1), ATP-binding cassette subfamily G member 2 (ABCG2), and ATP-binding cassette subf...
Cisplatin-induced acute kidney injury increased brain 5-hydroxytryptamine levels partly due to the hippuric acid-induced upregulation of CYP2D4 expression and function in the brain of rats [0.03%]
卡铂诱导的大鼠急性肾损伤增加脑5-羟色胺水平部分是由于hippuric酸诱导的脑CYP2D4表达和功能上调所致
Lingjue Lu,Nan Hu,Haoran Chen et al.
Lingjue Lu et al.
Patients with acute kidney injury (AKI) are often associated with uremic encephalopathy, but its underlying mechanisms remain unclear. This study aimed to investigate how AKI induced neuropsychiatric disorders through cerebral 5-hydroxytryp...
Miki Nakajima,Hiroshi Yamazaki,Kouichi Yoshinari et al.
Miki Nakajima et al.
Japanese researchers have played a pivotal role in advancing the field of drug metabolism and disposition, as demonstrated by their substantial contributions to the journal Drug Metabolism and Disposition (DMD) over the past 5 decades. This...
The strong clinical interaction between bupropion and CYP2D6 is primarily mediated through bupropion metabolites and their stereoisomers: A paradigm for evaluating metabolites in drug-drug interaction risk [0.03%]
布普品与CYP2D6的强临床相互作用主要通过其代谢产物及其立体异构体介导：评估药物相互作用风险中的代谢产物的一个范例
Irin Tanaudommongkon,Amir Rashidian,Brandon T Gufford et al.
Irin Tanaudommongkon et al.
Bupropion (BUP) is a potent clinical inhibitor of CYP2D6, although the specific mechanisms underlying this interaction are not fully understood. We comprehensively evaluated the inhibition potencies of racemic BUP and its stereoisomers, as ...
Erlotinib-A substrate and inhibitor of OATP2B1: pharmacokinetics and CYP3A-mediated metabolism in rSlco2b1-/- and SLCO2B1+/+ rats [0.03%]
厄洛替尼-OATP2B1的底物和抑制剂：携带rSlco2b1-/-和SLCO2B1+/+基因的rats中的药代动力学及CYP3A介导的代谢研究
Marta A Rysz,Anima M Schäfer,Jonny Kinzi et al.
Marta A Rysz et al.
The tyrosine kinase inhibitor erlotinib is recognized as a substrate of cytochrome P450 enzymes and drug transporters. Indeed, erlotinib's extensive metabolism to the active metabolite OSI-420 (desmethyl erlotinib) mainly involves CYP3A enz...
Impact of variation in CYP3A and CYP2C8 on tucatinib metabolic clearance in human liver microsomes [0.03%]
人肝微粒体中CYP3A和CYP2C8多态性对TUCATINIB代谢清除的影响
Bethany D Latham,Pegah Montazeri,Licza F Lobo et al.
Bethany D Latham et al.
Tucatinib is a small molecule tyrosine kinase inhibitor indicated for HER2-positive breast cancer. This recently approved drug is primarily metabolized by cytochrome P450 (P450) 2C8 and CYP3A. Given the interindividual variability in the ph...