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核受体FXR代谢调控作用及肿瘤细胞增殖机制研究进展

谢杨, 周雪妍, 郝海平, 王广基^*

中国药科大学天然药物活性组分与药效国家重点实验室，药物代谢动力学重点实验室，南京 210009

摘要

类法尼酯衍生物X受体(farnesoid X receptor, FXR)是配体激活的转录因子，为核受体超家族的主要成员。FXR在胆汁酸代谢、胆固醇代谢、脂代谢以及糖代谢中发挥重要作用。近期研究显示，FXR在代谢性疾病，如高糖血症和高脂血症，以及肠道炎症性疾病、肝再生，甚至肿瘤细胞的增殖和凋亡中发挥重要的调控作用。然而现阶段对于FXR的代谢调控作用在肿瘤发生、发展中的意义尚不明了，甚至存在争议。本文综述了FXR对代谢的调控作用，以及FXR对肿瘤细胞增殖的不同作用和相关机制研究的新进展。

关键词： 类法尼酯衍生物X受体; 代谢调控; 肿瘤; 增殖

分类号：R329

[Progress in the role of farnesoid X receptor in metabolic regulation and tumor cell proliferation.] [Article in Chinese]

XIE Yang, ZHOU Xue-Yan, HAO Hai-Ping, WANG Guang-Ji^*

State Key Laboratory of Natural Medicines, Key Laboratory of Drug Metabolism &； Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, China

Abstract

Farnesoid X receptor (FXR) is a ligand-activated transcriptional factor belonged to the superfamily of nuclear receptors. In the past decades, FXR has been found with important roles in the regulation of metabolic homeostasis of bile acids, cholesterol, lipids and carbohydrates. Recent studies further demonstrate the potential protective effect of FXR against metabolic diseases, such as hyperglycemia and hyperlipidemia, as well as inflammatory bowel diseases (IBD). In addition, FXR plays an essential role in liver regeneration, tumor cell proliferation and apoptosis. However, the role of FXR in the development of tumor is still obscure and even with discrepancy. This article reviews the function of FXR in metabolic regulation and recent progress in basic, clinical and pharmacological researches related to tumor cell proliferation involving FXR.

Key words: farnesoid X receptor; metabolic regulation; tumor; proliferation

收稿日期：2013-08-30　　录用日期：2013-10-08

通讯作者：王广基　　E-mail: guangjiwang@hotmail.com

引用本文：

谢杨, 周雪妍, 郝海平, 王广基. 核受体FXR代谢调控作用及肿瘤细胞增殖机制研究进展[J]. 生理学报 2014; 66 (2): 252-258.

XIE Yang, ZHOU Xue-Yan, HAO Hai-Ping, WANG Guang-Ji. [Progress in the role of farnesoid X receptor in metabolic regulation and tumor cell proliferation.] [Article in Chinese]. Acta Physiol Sin 2014; 66 (2): 252-258 (in Chinese with English abstract).