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http://dx.doi.org/10.5352/JLS.2011.21.4.481

T0901317 as an Inhibitor of Transcriptional Activation of Constitutive Androstane Receptor (CAR)  

Kim, Hyun-Ha (Graduste program of Neuroscience, Inje University)
Seol, Won-Gi (Graduste program of Neuroscience, Inje University)
Publication Information
Journal of Life Science / v.21, no.4, 2011 , pp. 481-485 More about this Journal
Abstract
T0901317 is a potent synthetic ligand for liver X receptor (LXR, NR1H2/3), a member of the nuclear receptor superfamily that functions as a transcription factor. However, T0901317 has been also reported to modulate the activity at least four other nuclear receptors (NRs), acting as agonists for farnesoid X receptor (FXR, NR1H4) and pregnane X receptor (PXR, NR1I2) and as antagonists for androgen receptor (AR, NR3C4) and retinoid-related orphan receptor-${\alpha}$ (ROR-${\alpha}$, NR1F1). We report here that T0901317 can also function as an inhibitor for constitutive androstane receptor (CAR, NR1I3). Since CAR is a major player of xenobiotic and cholesterol metabolism in the liver, along with PXR, FXR and LXR, which are reported to be regulated by T0901317, this further complicates the interpretation of potential results with T0901317 in liver cells.
Keywords
Constitutive androstane receptor (CAR); T0901317; liver X receptor (LXR); PGC-1${\alpha}$; antagonist;
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