[HTML][HTML] Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pump
J Cui, LI Huang, A Zhao, JL Lew, J Yu, S Sahoo… - Journal of Biological …, 2003 - ASBMB
Guggulipid is an extract of the guggul treeCommiphora mukul and has been widely used to
treat hyperlipidemia in humans. The plant sterol guggulsterone (GS) is the active agent in
this extract. Recent studies have shown that GS can act as an antagonist ligand for farnesoid
X receptor (FXR) and decrease expression of bile acid-activated genes. Here we show that
GS, although an FXR antagonist in coactivator association assays, enhances FXR agonist-
induced transcription of bile salt export pump (BSEP), a major hepatic bile acid transporter …
treat hyperlipidemia in humans. The plant sterol guggulsterone (GS) is the active agent in
this extract. Recent studies have shown that GS can act as an antagonist ligand for farnesoid
X receptor (FXR) and decrease expression of bile acid-activated genes. Here we show that
GS, although an FXR antagonist in coactivator association assays, enhances FXR agonist-
induced transcription of bile salt export pump (BSEP), a major hepatic bile acid transporter …