Regulation of the Organic Anion Transporting Polypeptide 1B3 (OATP1B3) by Sex Hormones.

The mechanisms of regulation of the organic anion transporting polypeptide OATP1B3 by sex hormones were studied using HepG2 cells. Estradiol, progesterone, and testosterone were added to cells at concentrations of 1, 10, 100 μM for 24 h. The relative content of OATP1B3 was evaluated by Western blotting. Estradiol at concentrations of 10 and 100 μM increased the level of OATP1B3 acting through the farnesoid X-receptor, testosterone at concentrations of 1, 10, and 100 μM increased the expression of the transporter protein due to its effect on the liver X-receptor subtype α (LXRα), and progesterone did not affect the expression of OATP1B3.