Pub. Date : 2012
PMID : 22291955
6 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Exposure of HepG2 cells to theonellasterol antagonizes the effect of natural and synthetic FXR agonists on FXR-regulated genes, including SHP, OSTalpha, BSEP and MRP4. | 7-hydroxytheonellasterol | nuclear receptor subfamily 1 group H member 4 | Homo sapiens |
| 2 | Discovery that theonellasterol a marine sponge sterol is a highly selective FXR antagonist that protects against liver injury in cholestasis. | 7-hydroxytheonellasterol | nuclear receptor subfamily 1 group H member 4 | Homo sapiens |
| 3 | Here, we have characterized the activity of this theonellasterol on FXR-regulated genes and biological functions. | 7-hydroxytheonellasterol | nuclear receptor subfamily 1 group H member 4 | Homo sapiens |
| 4 | PRINCIPAL FINDINGS: Interrogation of HepG2 cells, a human hepatocyte cell line, by microarray analysis and transactivation assay shows that theonellasterol is a selective FXR antagonist, devoid of any agonistic or antagonistic activity on a number of human nuclear receptors including the vitamin D receptor, PPARs, PXR, LXRs, progesterone, estrogen, glucorticoid and thyroid receptors, among others. | 7-hydroxytheonellasterol | nuclear receptor subfamily 1 group H member 4 | Homo sapiens |
| 5 | Exposure of HepG2 cells to theonellasterol antagonizes the effect of natural and synthetic FXR agonists on FXR-regulated genes, including SHP, OSTalpha, BSEP and MRP4. | 7-hydroxytheonellasterol | nuclear receptor subfamily 1 group H member 4 | Homo sapiens |
| 6 | Analysis of genes involved in bile acid uptake and excretion by hepatocytes revealed that theonellasterol increases the liver expression of MRP4, a basolateral transporter that is negatively regulated by FXR. | 7-hydroxytheonellasterol | nuclear receptor subfamily 1 group H member 4 | Homo sapiens |