T0901317 is a dual LXR/FXR agonist.
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.
Houck
Keith A
KA
RTP Laboratories, Eli Lilly & Company, Research Triangle Park, NC 27709, USA.
Borchert
Kristen M
KM
Hepler
Christopher D
CD
Thomas
Jeffrey S
JS
Bramlett
Kelli S
KS
Michael
Laura F
LF
Burris
Thomas P
TP
D000074020:ATP Binding Cassette Transporter, Subfamily B, Member 11; D018528:ATP-Binding Cassette Transporters / Q000187:drug effects / Q000235:genetics; D000924:Anticholesteremic Agents / Q000494:pharmacology*; D002478:Cells, Cultured; D002635:Chenodeoxycholic Acid / Q000494:pharmacology; D004268:DNA-Binding Proteins / Q000819:agonists* / Q000235:genetics / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D006801:Humans; D006845:Hydrocarbons, Fluorinated; D008024:Ligands; D000071518:Liver X Receptors; D057093:Orphan Nuclear Receptors; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists* / Q000235:genetics / Q000378:metabolism; D013449:Sulfonamides; D014157:Transcription Factors / Q000819:agonists* / Q000235:genetics / Q000378:metabolism; D000099150:Receptor, Farnesoid X-Activated; D005466:Fluorocarbons; D000096926:Benzenesulfonamides
D000074020:ATP Binding Cassette Transporter, Subfamily B, Member 11; D018528:ATP-Binding Cassette Transporters; D000924:Anticholesteremic Agents; D002635:Chenodeoxycholic Acid; D004268:DNA-Binding Proteins; D006845:Hydrocarbons, Fluorinated; D008024:Ligands; D000071518:Liver X Receptors; D057093:Orphan Nuclear Receptors; D018160:Receptors, Cytoplasmic and Nuclear; D013449:Sulfonamides; D014157:Transcription Factors; D000099150:Receptor, Farnesoid X-Activated; C093491:ABCB11 protein, human; C000605210:NR1H2 protein, human; C000605213:NR1H3 protein, human; C423915:T0901317; D005466:Fluorocarbons; D000096926:Benzenesulfonamides