雄激素受体
CYP1A2
CYP2E1
化学
细胞色素P450
核受体
视黄醇X受体
受体
孕烷X受体
视黄醇X受体α
蛋白质组学
下调和上调
内科学
CYP3A4型
内分泌学
酶
药理学
生物化学
生物
医学
基因
转录因子
作者
Atsushi Kawase,Shunsuke Tateishi,Akira Kazaoka
摘要
Abstract Inflammatory conditions alter the expression and activity of factors influencing pharmacokinetics, such as metabolizing enzymes. The study examined alterations of hepatic protein levels of cytochrome P450 (CYP), UDP‐glucuronosyltransferase (UGT) and nuclear receptors in rats with adjuvant‐induced arthritis (AA rats), an inflammatory animal model, by liquid chromatography–tandem mass spectrometry‐based targeted proteomics. The protein levels of CYP1A1, CYP1A2, CYP2A1, CYP2A3, CYP2C6, CYP2C12, CYP2D3, CYP2E1, CYP3A9, UGT1A1 and UGT1A2/3 in liver microsomes of AA rats were significantly lower than those in control rats. The protein levels of constitutive androstane receptor (CAR) and retinoid X receptor α (RXRα) in the cytoplasm and nucleus were also significantly decreased, to approximately 60% of the control levels. The decreased protein levels of CYP1A2, CYP2C6, CYP2D3, CYP2E1 and UGT1A1 were potentially associated with downregulation of CAR or RXRα expression in the nucleus.
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