Article
Molecular determinants of steroid inhibition for the mouse constitutive androstane receptor.
Journal of medicinal chemistry - 23 Oct 2003
Jyrkkärinne Johanna, Mäkinen Janne, Gynther Jukka, Savolainen Heidi, Poso Antti, Honkakoski Paavo
Abstract excerpt
The constitutive androstane receptor (CAR) regulates drug and steroid metabolism through binding to cytochrome P450 2B, 2C, and 3A gene enhancers. Uniquely among nuclear receptors, mouse CAR (mCAR) can be suppressed by androstenol and activated by structurally diverse drugs, pesticides, and environmental pollutants. To gain insight into presently ill-defined structural requirements of mCAR ligands, we employed a...
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