Table 1. Posttranslational modifications of FXR.
| Enzyme, modification | Modification target | Function | Reference |
|---|---|---|---|
| PMRT1, methylation | Promoter region | Increases BSEP and SHP mRNA expression Increases FXR transcriptional activity Increases conjugated bile acids (liver) |
88 94 |
| p300, acetylation | Promoter region, FXR lysine 157 and lysine 217 |
Increases SHP expression Prevents FXR/RXRα dimerization |
66 89 |
| SIRT-1, deacetylation | FXR | Increases FXR transcriptional activity Promotes FXR/RXRα dimerization |
66 |
| SUMO1, SUMOylation | FXR | Decreases FXR binding to BSEP and SHP promoters | 98 |
| Src kinase, phosphorylation | FXR tyrosine 67 | Increases FXR transcriptional activity | 95 |
| O-linked-N-acetylglucosamine transferase, O-GlcNAc | FXR serine 62 or 72, isoform-dependent | Increases glycolytic and lipogenic gene expression (in absence of FXR ligands) | 79 93 101 |
Abbreviation: FXR, farnesoid X receptor.