Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands.
1 with the Laplacian-corrected Bayesian classifier and molecular descriptors, as previously described for 115 steroidal compounds (namely, androstanes, estratrienes, pregnanes, and bile salts), with hPXR activation determined by a luciferase-based reporter assay (Ekins et al.
Identification of constitutive androstane
receptor and glucocorticoid receptor binding sites in the CYP2C19 promoter.
Reduction in cytochrome P-450 enzyme expression is associated with repression of CAR (constitutive androstane
receptor) and PXR (pregnane X receptor) in mouse liver during the acute phase response.
These UGT isoforms are induced by aryl hydrocarbon receptor (AhR), constitutive androstane
receptor (CAR), and pregnane-X receptor (PXR) agonists.
The environmental pollutant 1,1-dichloro-2,2-bis (p-chlorophenyl)ethylene induces rat hepatic cytochrome P450 2B and 3A expression through the constitutive androstane
receptor and pregnane X receptor.
Pregnane X receptor (PXR), constitutive androstane
receptor (CAR), and benzoate X receptor (BXR) define three pharmacologically distinct classes of nuclear receptors.
Homology modelling of the nuclear receptors: human oestrogen receptor beta (hERbeta), the human pregnane-X-receptor (PXR), the Ah receptor (AhR) and the constitutive androstane
receptor (CAR) ligand binding domains from the human oestrogen receptor alpha (hERalpha) crystal structure, and the human peroxisome proliferator activated receptor alpha (PPARalpha) ligand binding domain from the human PPARgamma crystal structure.
197) Specifically, the court found that, although five of eighteen disclosed androstanes
were claimed, the specification did not identify which androstanes
were useful or what biological properties they possessed: