孕烷X受体对细胞色素P450 3A调控机制的研究进展

被引：5

作者：

李越

李燕

机构：

[1] 中国医学科学院/北京协和医学院药物研究所

来源：

国际药学研究杂志 | 2009年 / 36卷 / 03期

关键词：

孕烷X受体; 细胞色素P450 3A; 基因表达调控;

D O I：

10.13220/j.cnki.jipr.2009.03.012

中图分类号：

R962.1 [];

学科分类号：

摘要：

细胞色素P450 3A(CYP3A)是参与临床药物代谢的主要CYP同工酶之一。孕烷X受体(PXR)属于核受体超家族(NR)的NR1Ⅰ亚家族。该受体作为药物代谢的关键转录调控因子,参与CYP3A的诱导表达。药物可通过多种途径激活PXR受体调控cyp3a基因的表达,其中包括PXR与其他核受体、转录因子及细胞信号转导通路间的相互作用等多种途径。目前,基于PXR的筛选方法已广泛应用于早期新药研发。

引用

页码：184 / 188

页数：5

共 7 条

[1] Retinoids induce cytochrome P450 3A4 through RXR/VDR-mediated pathway [J].

Wang, Kun ;

Chen, Shiyonq ;

Xie, Wen ;

Wan, Yu-Jui Yvonne .

BIOCHEMICAL PHARMACOLOGY, 2008, 75 (11) :2204-2213

[2] Interplay of pregnane X receptor with other nuclear receptors on gene regulation [J].

不详 .

DRUG METABOLISM AND PHARMACOKINETICS, 2008, 23 (01) :14-21

[3] Mechanisms of cytochrome P450 induction [J].

Tompkins, Leslie M. ;

Wallace, Andrew D. .

JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY, 2007, 21 (04) :176-181

[4]

Identification of drugs that interact with herbs in drug development[J] . Shu-Feng Zhou,Zhi-Wei Zhou,Chun-Guang Li,Xiao Chen,Xiyong Yu,Charlie Changli Xue,Adrian Herington.Drug Discovery Today . 2007 (15)

[5] Exposure-dependent inhibition of intestinal and hepatic CYP3A4 in vivo by grapefruit juice [J].

Veronese, ML ;

Gillen, LP ;

Burke, JP ;

Dorval, EP ;

Hauck, WW ;

Pequignot, E ;

Waldman, SA ;

Greenberg, HE .

JOURNAL OF CLINICAL PHARMACOLOGY, 2003, 43 (08) :831-839

[6] Pharmaceutical use of mouse models humanized for the xenobiotic receptor [J].

Xie, W ;

Evans, RM .

DRUG DISCOVERY TODAY, 2002, 7 (09) :509-515

[7]

The far and distal enhancers in the CYP3A4gene coordinate the proximal promoter in responding similarly to the pregnane X receptor but differentially to hepatocyte nuclear factor-4alpha .2 Liu FJ,Song X,Yang D,et al. Biochem J . 2008

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