LXR can sense excess cholesterol and mediate the expression of proteins that will increase cholesterol efflux. These transporter proteins include ABCA1 and ABCG1 which are ATP binding proteins that can facilitate the efflux of cholesterol to apoA-1 or HDL (respectively). FXR can sense bile acids and suppress genes involved in bile acid production. FXR activation can result in the upregulation of SHP, a transcription factor that will then suppress the expression of CYP7A1 and CYP8B1. CYP7A1 is the rate-limiting enzyme for the conversion of cholesterol to bile acids. HEPG2 cells, from a human cell line, were cultured and dose dependent titrations were done to determine the response of the cells to both LXR and FXR agonists through quantifying mRNA expression.

LXR and FXR response in human liver cells

245th National Meeting (2013)

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