Targeting farnesoid X receptor for liver and metabolic disorders

被引：236

作者：

Fiorucci, Stefano ^{[1
]}

Rizzo, Gianni

Donini, Annibale

Distrutti, Eleonora

Santucci, Luca

机构：

[1] Univ Perugia, Dipartimento Med Clin & Sperimentale, I-06100 Perugia, Italy

[2] Univ Perugia, Dipartimento Sci Chirurg Radiol & Odontostomatol, I-06100 Perugia, Italy

来源：

TRENDS IN MOLECULAR MEDICINE | 2007年 / 13卷 / 07期

关键词：

D O I：

10.1016/j.molmed.2007.06.001

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

The farnesoid X receptor (FXR) is a metabolic nuclear receptor expressed in the liver, intestine, kidney and adipose tissue. By regulating the expression and function of genes involved in bile acid (BA) synthesis, uptake and excretion, FXR has emerged as a key gene involved in the maintenance of cholesterol and BA homeostasis. FXR ligands are currently under clinical investigation for the treatment of chollestasis, dyslipidemic disorders and conditions of insulin resistance in type 2 diabetes and nonalcoholic steatohepatitis (NASH). Because activation of FXR impacts a considerable number of genes, development of FXR modulators that selectively regulate specific pathways will limit potentially undesirable side effects. Interaction of FXR with other BAs and xenobiotics sensors such as the constitutive androstane receptor and the pregnane X receptor might allow the development of combination therapies for liver and metabolic disorders.

引用

收藏

页码：298 / 309

页数：12

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