TABLE 1

Inhibitory effects of statins on the ATP-dependent upta ke of [³H]estrone-3-sulfate by human BCRP- and mouse Bcrp-expressing membrane vesicles

The ATP-dependent uptake of [³H]estrone-3-sulfate (0.1 μM) for 1 min by human BCRP (hBCRP) and mouse Bcrp (mBcrp) was determined in the presence and absence of unlabeled statins at the designated concentrations. The values are expressed as a percentage of the ATP-dependent uptake of [³H]estrone-3-sulfate in the absence of any unlabeled compounds. The ATP-dependent uptake was obtained by subtracting the transport velocity in the presence of AMP from that in the presence of ATP. The K_i values were determined by fitting the data using the non-least s quares method. The values are expressed as mean ± computer-calculated S.D. (n = 3).