Orphan nuclear receptor-mediated xenobiotic regulation in drug metabolism.
Orphan nuclear receptor-mediated xenobiotic regulation in drug metabolism.
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DOI：
10.1016/s1359-6446(04)03061-2
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发表时间：
2004-05
影响因子：
7.4
通讯作者：
W. Xie;H. Uppal;S. Saini;Ying Mu;J. Little;A. Radomińska-Pandya;M. Zemaitis
中科院分区：
文献类型：
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作者：
W. Xie;H. Uppal;S. Saini;Ying Mu;J. Little;A. Radomińska-Pandya;M. Zemaitis
药物代谢酶和转运蛋白的调节在药物代谢和许多人类疾病中具有重要作用。编码这些酶和转运蛋白的基因可被许多外源物质和内生物质诱导，并且诱导物显示出明显的种属特异性。在过去的4-5年中，孤儿核受体如PXR和CAR已被确定为调节许多解毒酶和转运蛋白表达的物种特异性异种感受器。它们的鉴定代表了理解药物代谢酶表达的药理学和遗传学控制以及这种调节在药物代谢、药物相互作用和人类疾病中的意义的重要一步。
The regulation of drug-metabolizing enzymes and transporters has an important role in drug metabolism and many human diseases. The genes that encode these enzymes and transporters are inducible by numerous xenobiotics and endobiotics and the inducibility shows clear species specificity. In the past 4–5 years, orphan nuclear receptors such as PXR and CAR have been established as species-specific xeno-sensors that regulate the expression of many detoxifying enzymes and transporters. Their identification represents a major step forward in understanding the pharmacological and genetic control of the expression of drug-metabolizing enzymes and the implication of this regulation in drug metabolism, drug–drug interactions, and human diseases.