T0901317 is a dual LXR/FXR agonist

Mol Genet Metab. Sep-Oct 2004;83(1-2):184-7. doi: 10.1016/j.ymgme.2004.07.007.

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

  • ATP Binding Cassette Transporter, Subfamily B, Member 11
  • ATP-Binding Cassette Transporters / drug effects
  • ATP-Binding Cassette Transporters / genetics
  • Anticholesteremic Agents / pharmacology*
  • Cells, Cultured
  • Chenodeoxycholic Acid / pharmacology
  • DNA-Binding Proteins / agonists*
  • DNA-Binding Proteins / genetics
  • DNA-Binding Proteins / metabolism
  • Dose-Response Relationship, Drug
  • Humans
  • Hydrocarbons, Fluorinated
  • Ligands
  • Liver X Receptors
  • Orphan Nuclear Receptors
  • Receptors, Cytoplasmic and Nuclear / agonists*
  • Receptors, Cytoplasmic and Nuclear / genetics
  • Receptors, Cytoplasmic and Nuclear / metabolism
  • Sulfonamides
  • Transcription Factors / agonists*
  • Transcription Factors / genetics
  • Transcription Factors / metabolism

Substances

  • ABCB11 protein, human
  • ATP Binding Cassette Transporter, Subfamily B, Member 11
  • ATP-Binding Cassette Transporters
  • Anticholesteremic Agents
  • DNA-Binding Proteins
  • Hydrocarbons, Fluorinated
  • Ligands
  • Liver X Receptors
  • NR1H2 protein, human
  • NR1H3 protein, human
  • Orphan Nuclear Receptors
  • Receptors, Cytoplasmic and Nuclear
  • Sulfonamides
  • TO-901317
  • Transcription Factors
  • farnesoid X-activated receptor
  • Chenodeoxycholic Acid