Table 3.
RAR/RXR target genes involved in bile acid metabolism.
| Target gene | Regulation | Function | Species | Cell type | References |
|---|---|---|---|---|---|
| CYP7A1\–/RAR/RXR) | Repression | The rate-limiting enzyme in the synthesis of bile acid from cholesterol by catalyzing the formation of 7α-hydroxycholesterol | Human | HepG2 | [45,97] |
| Hepatocytes | [45] | ||||
| FGF19 (RXR/RAR) | Stimulation | The gut-derived hormone for inhibition of CYP7A1 expression via the FGFR4/Klotho-β receptor complexes in the liver | Human | Ileum (HT-29 cell, caco-2 cell) | [46] |
| CYP27A1 (RAR/RXR) | Repression | The enzyme for degradation of cholesterol to bile acids | Human | Hepatocyte | [45,59] |
| NTCP (RAR/RXR) | Repression | The major basolateral bile acid uptake transporter in hepatocytes | Human | HepG2 | [62,63,69,98] |
| Rat | Hepatocytes Stellate cell. Kupffer cell | [99,100] | |||
| Mice | Hepatocytes | [65] | |||
| MRP2 (RAR/RXR) | Stimulation | The hepatic apical transporter for bilirubin, glutathione, bile acids and other organic anions and their conjugates | Human | HepG2 | [63,69] |
| Rat | Hepatocytes | [66] | |||
| MRP3 (RAR/RXR) | Repression | The hepatic basolateral pump for extrude bilirubin, bile acids and other organic anions and their conjugates | Human | HepG2 | [71] |
| OATP1B1,1B3 (RAR/RXR) | Repression | The basolateral uptake transporter for organic anions | Human | Hepatocytes | [70] |
| OCT1 (RAR/RXR) | Repression | The basolateral uptake transporter for organic cations | |||
| OAT2 (RAR/RXR) | Repression | The basolateral uptake of organic anions/dicarboxylate exchanger | |||
| ASBT (RAR/RXR) | Stimulation | The apical bile acid uptake transporter in bile duct and ileum | Human | CT-26, Caco-2, HIBEC | [72-76] |