药学学报, 2012, 47(12): 1575-1581
引用本文:
刘志浩, 李 燕. 核受体对药物代谢酶和转运体的调控[J]. 药学学报, 2012, 47(12): 1575-1581.
LIU Zhi-hao, LI Yan. Modulation of nuclear receptors on drug-metabolizing enzymes and transporters[J]. Acta Pharmaceutica Sinica, 2012, 47(12): 1575-1581.

核受体对药物代谢酶和转运体的调控
刘志浩, 李  燕*
(中国医学科学院、北京协和医学院药物研究所药物代谢室, 北京 100050)
摘要:

PXRCARPPAR是核受体家族的重要成员, 体内分布广泛, 经配体激活后可调控药物代谢酶及转运体的表达和活性, 影响药物在体内的处置。肿瘤多药耐药是导致癌症治疗失败的主要原因, 核受体对药物代 谢过程产生的影响可能使其成为逆转肿瘤多药耐药的新药作用靶点。本文主要介绍了核受体家族主要成员PXRCARPPAR的研究进展, 阐述其转录激活机制以及其对药物代谢酶及转运体的调控, 为临床合理用药、克服肿瘤多药耐药的研究等提供参考。

关键词:   
Modulation of nuclear receptors on drug-metabolizing enzymes and transporters
Abstract:

PXR, CAR and PPAR, widely distributed in the body, are important members of the nuclear receptors (NRs) family.  The activities and gene expressions of drug-metabolizing enzymes (DMEs) and transporters can be regulated by the activation of NRs, which effect the drug disposition.  Multidrug resistance (MDR) is the leading cause of failure in cancer therapy.  NRs, including PXR, CAR and PPAR, were shown to regulate the expressions of DMEs and transporters involved in the drug metabolism and clearance, suggesting that the modulation of NRs can be considered as a new target to overcome MDR.  This review described the research progress of NR family members PXR, CAR, PPAR and their transcriptional activation mechanism, the regulation of DMEs and transporters by NRs, which may provide a valuable reference for clinical medication and overcome of MDR.

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