T0901317 is a dual LXR/FXR agonist

被引：157

作者：

Houck, KA

Borchert, KM

Hepler, CD

Thomas, JS

Bramlett, KS

Michael, LF

Burris, TP ^{[1
]}

机构：

[1] Lilly Corp Ctr, Lilly Res Labs, Indianapolis, IN 46285 USA

[2] Eli Lilly & Co, RTP Labs, Res Triangle Pk, NC 27709 USA

[3] Indiana Univ, Sch Med, Dept Pharmacol & Toxicol, Indianapolis, IN 46202 USA

来源：

MOLECULAR GENETICS AND METABOLISM | 2004年 / 83卷 / 1-2期

关键词：

bile acid; oxysterol; nuclear receptor;

D O I：

10.1016/j.ymgme.2004.07.007

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

We characterize the ability of the liver X receptor (LXRalpha [NR1H3] and LXRbeta [NR1H2]) agonist, T0901317, to activate the farnesoid X receptor (FXR [NR4H4]). Although T0901317 is a much more potent activator of LXR than FXR, this ligand actually activates FXR more potently than a natural bile acid FXR ligand, chenodeoxycholic acid. Thus, the FXR activity of T0901317 must be considered when utilizing this agonist as a pharmacological tool to investigate LXR function. (C) 2004 Elsevier Inc. All rights reserved.

引用

收藏

页码：184 / 187

页数：4

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