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Quantification of P450 protein isoforms in hepatocytes by mass spectrometry

机译:质谱法定量测定肝细胞中P450蛋白亚型

摘要

A method for screening a drug for cytochrome P450 (CYP) induction is provided and can include incubating the drug with a microsome-containing biological sample and then quantitating at least one cytochrome P450 isoform. The isoforms can be selected from 2B6, 3A4, 1A2, and 3A5 isoforms. In some embodiments, the method uses liquid chromatography tandem mass spectrometry (LC-MSMS). A quantitated value can be compared to a threshold value and the drug can be determined to exhibit an acceptable CYP induction potential when the quantitated value does not exceed the threshold value. Isolated peptides are also provided.
机译:提供了一种筛选用于细胞色素P450(CYP)诱导的药物的方法,该方法可以包括将药物与含微粒体的生物样品一起孵育,然后定量至少一种细胞色素P450同工型。所述同工型可以选自2B6、3A4、1A2和3A5同工型。在一些实施方案中,该方法使用液相色谱串联质谱法(LC-MSMS)。可以将定量值与阈值进行比较,并且当定量值不超过阈值时,可以确定药物显示出可接受的CYP诱导潜力。还提供了分离的肽。

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