The liver X receptor agonist T0901317 acts as androgen receptor antagonist in human prostate cancer cells

Biochem Biophys Res Commun. 2007 Jun 1;357(2):341-6. doi: 10.1016/j.bbrc.2007.03.116. Epub 2007 Mar 28.


T0901317 is a potent non-steroidal synthetic liver X receptor (LXR) agonist. T0901317 blocked androgenic stimulation of the proliferation of androgen-dependent LNCaP 104-S cells and androgenic suppression of the proliferation of androgen-independent LNCaP 104-R2 cells, inhibited the transcriptional activation of an androgen-dependent reporter gene by androgen, and suppressed gene and protein expression of prostate specific antigen (PSA), a target gene of androgen receptor (AR) without affecting gene and protein expression of AR. T0901317 also inhibited binding of a radiolabeled androgen to AR, but inhibition was much weaker compared to the effect of the antiandrogens, bicalutamide and hydroxyflutamide. The LXR agonist T0901317, therefore, acts as an antiandrogen in human prostate cancer cells.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Androgen Receptor Antagonists*
  • Angiogenesis Inhibitors / administration & dosage
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • DNA-Binding Proteins / agonists*
  • Dose-Response Relationship, Drug
  • Humans
  • Hydrocarbons, Fluorinated
  • Liver X Receptors
  • Male
  • Orphan Nuclear Receptors
  • Prostatic Neoplasms / metabolism*
  • Receptors, Androgen / metabolism*
  • Receptors, Cytoplasmic and Nuclear / agonists*
  • Sulfonamides / administration & dosage*


  • Androgen Receptor Antagonists
  • Angiogenesis Inhibitors
  • DNA-Binding Proteins
  • Hydrocarbons, Fluorinated
  • Liver X Receptors
  • Orphan Nuclear Receptors
  • Receptors, Androgen
  • Receptors, Cytoplasmic and Nuclear
  • Sulfonamides
  • TO-901317