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Role of constitutive androstane receptor in Toll-like receptor-mediated regulation of gene expression of hepatic drug-metabolizing enzymes and transporters.
Synthetic drugs and natural products as modulators of constitutive androstane receptor (CAR) and pregnane X receptor (PXR).
Role of the constitutive androstane receptor in xenobiotic-induced thyroid hormone metabolism.
(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:
Yamazoe, "Constitutive androstane receptor transcriptionally activates human CYP1A1 and CYP1A2 genes through a common regulatory element in the 5'-flanking region," Biochemical Pharmacology, vol.
Homology modelling of the nuclear receptors: Human oestrogen receptorbeta (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.
Negishi et al., "Complementary roles of farnesoid X receptor, pregnane X receptor, and constitutive androstane receptor in protection against bile acid toxicity," Journal of Biological Chemistry, vol.
Induction of CYP3A4, CYP2C19, and CYP2C9 by the prenyloxycinnamic acids is most likely mediated via the pregnane x receptor (PXR), which regulates the expression of many CYPs and which is the major nuclear receptor in LS180 cells lacking the constitutive androstane receptor (CAR) (Gupta et al.
There are two groups of families of neurosteroids: the inhibitory neurotransmitter receptor families of pregnane neurosteroids that include allopregnanolone and aIlotetrahydrodeoxycorticosterone, and the excitatory neurotransmitter receptor families of androstane neurosteroids, such as androstanediol and etiocholanone.
Some PBDEs have been shown to cause pregnane X receptor (PXR)--and constitutive androstane receptor (CAR)-mediated induction of liver enzymes responsible for thyroid hormone clearance, which might compromise brain development by causing thyroid hormone insufficiency (EFSA 2011; Costa and Giordano 2011).
Augustine et al., "The Nrf2 activator oltipraz also activates the constitutive androstane receptor," Drug Metabolism and Disposition, vol.