The constitutive androstane receptor (CAR) was identified as a member of the orphan nuclear hormone receptor family in 1994. Although constitutively acitve, it can be further activated by ′phenobarbitol-like′ compounds, the most potent being the synthetic compound TCPOBOP. Upon activation, CAR regulates the xenobiotic drug metabolizing enzymes, cytochrome P450s. There are several overlapping functions between the nuclear receptors PXR and CAR. Recently, CAR, as well as PXR, have been shown to place a role in bile acid clearance and cholestatic liver injury.
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The pharmacogenomics journal, 2(2), 117-126 (2002-06-07)
The products of the cytochrome P450 (CYP) genes play an important role in the detoxification of xenobiotics and environmental contaminants, and many foreign chemicals or xenobiotics can induce their expression. We have previously shown that the nuclear hormone receptor CAR
Molecular and cellular biology, 14(3), 1544-1552 (1994-03-01)
We have identified and characterized a new orphan member of the nuclear hormone receptor superfamily, called MB67, which is predominantly expressed in liver. MB67 binds and transactivates the retinoic acid response elements that control expression of the retinoic acid receptor
Organisms encounter a wide range of foreign compounds--or 'xenobiotics'--with potentially harmful consequences. The cytochrome P450 (CYP) enzymes metabolize xenobiotics and thus are a primary defence against these compounds. Increased expression of specific CYP genes in response to particular xenobiotics is
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