核受体在药物代谢中的作用
摘要:核受体是一种配体依赖性转录因子,在外源性物质和内源性物质的代谢中具有重要作用。本文主要对核受体的基本结构、特性、二聚化以及参与核受体转录活化的辅助因子,参与药物代谢的I、II、III相酶做简要介绍,重点综述了核受体在药物代谢中的作用,尤其是PXR和CAR两种核受体在药物代谢中的作用和机制。
关键词:核受体;药物代谢酶;外源性物质;药物
中图分类号:R969.1文献标识码:A文章编号:1672-979X(2008)03-0064-05
Function of Nuclear Receptor in Drug Metabolism
LIU Yan-feng, LI Hong-xing, ZHAO Chang-qi, ZHAI Yong-gong*
(Biomedicine Research Institute, College of Life Sciences, Beijing Normal University, Beijing 100875, China)
Abstract:Nuclear receptor (NR) is a ligand-dependent transcriptional factor which plays an important role in the metabolism of xenobiotics and endobiotics. The structure, characteristic, dimerization of NR are briefly introduced in this paper, and the cofactor which participates in the transcriptional activation of NR is also interpreted. Moreover, the drug metabolizing enzymes in phase I, II, III were showed. The paper reviews the function of NR in drug metabolism, especially the function and mechanism of two NRs of PXR and CAR in drug metabolism. ......
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