Nuclear bile acid receptor FXR as pharmacological target: Are we there yet?

被引：78

作者：

Modica, Salvatore

Moschetta, Antonio

机构：

[1] Consorzio Mario Negri Sud, Dept Cell Biol & Oncol, I-66030 Santa Maria Imbaro, CH, Italy

[2] Univ Bari, Clin Med A Murri, I-70124 Bari, Italy

来源：

FEBS LETTERS | 2006年 / 580卷 / 23期

关键词：

cholesterol; farnesoid X receptor; gallstones; hypertriglyceridemia; metabolic syndrome;

D O I：

10.1016/j.febslet.2006.07.082

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily that is primarily expressed in the enterohepatic system where it functions as intracellular sensor for bile acids. Ligand dependent FXR activation induces transcriptional responses to coordinately regulate bile acid, cholesterol, triglyceride and glucose metabolism, and to protect the intestinal mucosa from bacterial overgrowth and inflammatory insults. Here we discuss the latest discoveries in FXR-driven metabolic pathways with relevance to pathophysiology and novel therapeutic approaches of several conditions such as hypertriglyceridemia, type 2 diabetes, cholesterol gallstone disease, steato-hepatitis and metabolic syndrome. (c) 2006 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.

引用

页码：5492 / 5499

页数：8

共 72 条

[1] Human bile salt export pump promoter is transactivated by the farnesoid X receptor/bile acid receptor [J].