Proteins in Response to Environmental Stress. Regulation of Cytochrome P-450 (CYP) Genes by Nuclear Receptors.
- 1 January 2002
- journal article
- abstracts
- Published by Japanese Society for Hygiene in Nippon Eiseigaku Zasshi (Japanese Journal of Hygiene)
- Vol. 56 (4) , 622-628
- https://doi.org/10.1265/jjh.56.622
Abstract
Many xenobiotics are metabolized and detoxified by cytochrome P-450s (CYP). The xenobiotics metabolizing CYPs are induced by various kinds of receptors. To induce CYP1A1, the Ah receptor requires a ligand for its activation as a transcription factor. On the other hand, benzimidazole compounds can induce CYP1A1 without binding to the Ah receptor as a ligand (ligand-independent pathway). In response to phenobarbital (PB) and other PB-type inducers, the nuclear receptor CAR (the NR-constitutive active receptor) translocates to the nucleus, forms a dimer with the retinoid X receptor (RXR), and activates the PB-responsive enhancer module (PBREM) in the PB-inducible CYP2B genes. For human CYP3A4 genes, pregnane X receptor (PXR) binds to the xenobiotic-responsive enhancer module (XREM) and upon induction by rifampicin, a PXR:RXR heterodimer could transactivate XREM.Keywords
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