Table 1.
Bile acid-activated nuclear receptor target genes in bile acid metabolism
| Receptors | Target genes | regulation | Function and pathways |
|---|---|---|---|
| FXR | CYP7A1 | Down | Enzyme in bile acid synthesis |
| CYP8B1 | Down | Enzyme in bile acid synthesis | |
| CYP27A1 | Down | Enzyme in bile acid synthesis | |
| SHP | Up | Negative regulator of bile acid synthesis | |
| FGF15/FGF19 | Up | Negative regulator of bile acid synthesis | |
| BSEP | Up | Canalicular bile acid secretion | |
| OSTα/OSTβ | Up | Basolateral bile acid secretion | |
| NTCP | Down | Basolateral bile acid uptake | |
| UGT2B4/UGT2B7 | Up | Bile acid conjugation | |
|
| |||
| PXR | CYP3A | Up | Phase-I bile acid/drug metabolism |
| CYP2B/CYP2C | Up | Phase-I bile acid/drug metabolism | |
| MRP1/MRP2/MRP3 | Up | Bile acid/drug transport | |
| UGT1A3 | Up | Bile acid conjugation | |
| SULT2A1 | Up | Bile acid conjugation | |
| OATP2 | Up | Basolateral bile acid/drug uptake | |
| CYP7A1 | Down | Enzyme in bile acid synthesis | |
|
| |||
| CAR | CYP3A | Up | Phase-I bile acid/drug metabolism |
| CYP2B, CYP2C | Up | Phase-I bile acid/drug metabolism | |
| UGT1A1 | Up | Bile acid conjugation | |
| MRP2 | Up | Bile acid/drug transport | |
| CYP7A1 | Down | Enzyme in bile acid synthesis | |
|
| |||
| VDR | CYP3A | Up | Phase-I bile acid/drug metabolism |
| CYP2B/CYP2C | Up | Phase-I bile acid/drug metabolism | |
| SULT2A1 | Up | Bile acid conjugation | |
| MRP3/MRP4 | Up | Bile acid/drug transport | |
| ASBT | Up | Canalicular bile acid uptake | |
| CYP7A1 | Down | Enzyme in bile acid synthesis | |