Pregnane X Receptor and its Potential Role in Drug Resistance in Cancer Treatment

被引：31

作者：

Chen, Yakun

Nie, Daotai ^{[1
]}

机构：

[1] So Illinois Univ, Sch Med, Dept Med Microbiol Immunol & Cell Biol, Springfield, IL 62794 USA

来源：

RECENT PATENTS ON ANTI-CANCER DRUG DISCOVERY | 2009年 / 4卷 / 01期

关键词：

Multi-drug resistance; pregnane X receptor; Drug metabolism enzyme; Drug transporter; Cancer treatment; Nuclear receptor; Steroid X receptor; Inhibitor; Chemotherapeutics; Carcinogenesis; Cancer repressor; ORPHAN NUCLEAR RECEPTOR; CONSTITUTIVE-ANDROSTANE RECEPTOR; REPORTER GENE ASSAY; ST JOHNS WORT; PROLIFERATOR-ACTIVATED RECEPTORS; BLOOD-MONONUCLEAR-CELLS; LIGAND-BINDING DOMAIN; XENOBIOTIC RECEPTOR; CRYSTAL-STRUCTURE; TARGET GENE;

D O I：

10.2174/157489209787002498

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

Multi-drug resistance (MDR) is a significant barrier to effective chemotherapy of cancer. The induction of drug metabolizing enzymes (DMEs) and efflux transporters has been regarded as one of the major mechanisms of drug resistance. As a master transcription factor of DMEs and efflux transporters, pregnane X receptor (PXR), an orphan nuclear receptor known for its activation by structurally diverse compounds, is expressed in some cancer cells and tissues, and is implicated as a novel master regulator of MDR in cancers. This review describes recent publications and patents on the mechanism of PXR transcription, the expression of PXR in cancers, and its potential roles in cancer MDR. We also discuss the recent patents published to overcome PXR-mediated MDR and other potential roles of PXR in cancers.

引用

页码：19 / 27

页数：9

共 154 条

[1]

AGGARWAL BB, 2008, Patent No. 20087368430

[2] Expression of the drug transporters MDR1/ABCB1, MRP1/ABCC1, MRP2/ABCC2, BCRP/ABCG2, and PXR in peripheral blood mononuclear cells and their relationship with the expression in intestine and liver [J].