Lithocholic acid decreases expression of bile salt export pump through farnesoid X receptor antagonist activity

J Yu, JL Lo, L Huang, A Zhao, E Metzger… - Journal of Biological …, 2002 - ASBMB
Bile salt export pump (BSEP) is a major bile acid transporter in the liver. Mutations in BSEP
result in progressive intrahepatic cholestasis, a severe liver disease that impairs bile flow
and causes irreversible liver damage. BSEP is a target for inhibition and down-regulation by
drugs and abnormal bile salt metabolites, and such inhibition and down-regulation may
result in bile acid retention and intrahepatic cholestasis. In this study, we quantitatively
analyzed the regulation of BSEP expression by FXR ligands in primary human hepatocytes …