Abstract
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.
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 11
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ATP-Binding Cassette Transporters / drug effects
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ATP-Binding Cassette Transporters / genetics
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Anticholesteremic Agents / pharmacology*
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Cells, Cultured
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Chenodeoxycholic Acid / pharmacology
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DNA-Binding Proteins / agonists*
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DNA-Binding Proteins / genetics
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DNA-Binding Proteins / metabolism
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Dose-Response Relationship, Drug
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Humans
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Hydrocarbons, Fluorinated
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Ligands
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Liver X Receptors
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Orphan Nuclear Receptors
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Receptors, Cytoplasmic and Nuclear / agonists*
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Receptors, Cytoplasmic and Nuclear / genetics
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Receptors, Cytoplasmic and Nuclear / metabolism
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Sulfonamides
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Transcription Factors / agonists*
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Transcription Factors / genetics
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Transcription Factors / metabolism
Substances
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ABCB11 protein, human
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ATP Binding Cassette Transporter, Subfamily B, Member 11
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ATP-Binding Cassette Transporters
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Anticholesteremic Agents
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DNA-Binding Proteins
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Hydrocarbons, Fluorinated
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Ligands
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Liver X Receptors
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NR1H2 protein, human
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NR1H3 protein, human
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Orphan Nuclear Receptors
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Receptors, Cytoplasmic and Nuclear
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Sulfonamides
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T0901317
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Transcription Factors
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farnesoid X-activated receptor
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Chenodeoxycholic Acid