Article
Simultaneous substitution of phenylalanine-305 and aspartate-318 of rat pregnane X receptor with the corresponding human residues abolishes the ability to transactivate the CYP3A23 promoter.
The Journal of pharmacology and experimental therapeutics - 1 Feb 2005
Song Xiulong, Li Yuxin, Liu Jirong, Mukundan Madhu, Yan Bingfang
Abstract excerpt
The pregnane X receptor (PXR) is a key regulator on the expression of genes involved in the elimination of chemicals. As one of the most divergent members in the nuclear receptor family, PXR is activated in a highly species-dependent manner by certain chemicals. Pregnenolone 16alpha-carbonitrile (PCN), a glucocorticoid antagonist, efficaciously activates rodent but not human PXR. This study was undertaken to...
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