4.4 Article

T0901317 is a dual LXR/FXR agonist

Journal

MOLECULAR GENETICS AND METABOLISM
Volume 83, Issue 1-2, Pages 184-187

Publisher

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.ymgme.2004.07.007

Keywords

bile acid; oxysterol; nuclear receptor

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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.

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