Houck Keith A, Borchert Kristen M, Hepler Christopher D, Thomas Jeffrey S, Bramlett Kelli S, Michael Laura F, Burris Thomas P
RTP Laboratories, Eli Lilly & Company, Research Triangle Park, NC 27709, USA.
Mol Genet Metab. 2004 Sep-Oct;83(1-2):184-7. doi: 10.1016/j.ymgme.2004.07.007.
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.
我们对肝脏X受体（LXRα [NR1H3] 和LXRβ [NR1H2]）激动剂T0901317激活法尼醇X受体（FXR [NR4H4]）的能力进行了表征。尽管T0901317作为LXR的激活剂比作为FXR的激活剂效力要强得多，但该配体实际上激活FXR的效力比天然胆汁酸FXR配体鹅去氧胆酸更强。因此，在将该激动剂用作研究LXR功能的药理学工具时，必须考虑T0901317的FXR活性。
