NR | Binding to NR1 | Activation of NR1/PBREM | Suppression of NR1/PBREM | Hepatic NR level in Rodents | Predicted Relevance of CAR Cross-Talk in Vivo |
---|---|---|---|---|---|
CAR | 2-219 | 2-219 +/2-219 + | N.A. | High | N.A. |
PXR | ++ | ++/+ | ++/++ 2-b | Moderate | 2-219 + Human, ++ Mouse |
VDR | 2-219 + | ++/+ | 2-219/+ 2-b | Low | ++ Human, 0 Mouse |
TRα | 2-219 + | ++/+ | 2-219/+ | Moderate | + Human, 0 Mouse |
PPARα | 0 | 0/0 | ++/+ | High2-c | + Human, ++Mouse |
FXR | 0 | 0/0 | ++/++ | High | ++ |
COUP-TFI | + | –/–2-a | 2-219 +/2-219 b | Low | ++ |
RARα | + | +/0 | +/+ | Low | 0 |
LXRβ | + | 0/0 | 0/0 | Low | 0 |
↵2-219 +, Strong effect; +++, significant effect; ++, moderate effect; +, weak effect; 0, no effect; N.A., not applicable.
↵2-a COUP-TFI represses NR1 and PBREM.
↵2-b PXR, VDR, and COUP-TFI suppress hPBREM more than mPBREM.
↵2-c Hepatic expression of hPPARα is significantly lower than that of mPPARα.