OATP1B1 Plays an Important Role in the Transport and Treatment Efficacy of Sorafenib in Hepatocellular Carcinoma

Figure 2

Uptake of sorafenib in control and transgenic HepG2 and LO2 cells. HepG2, OATP1B1-HepG2, LO2, and OATP1B1-LO2 cells were incubated with different concentrations of sorafenib (5, 10, and 15 μM) for 10 min (a, b). Overexpression of OATP1B1 in HepG2 cells significantly increases the uptake of sorafenib compared with control of HepG2 cells (a). Gene mutations significantly decrease the intake of sorafenib in OATP1B11b-HepG2 cells (decrease by about 17.77% and 28.47%) and OATP1B115-HepG2 cells (decrease by about 42.24% and 28.47%) compared to those of OATP1B11a-GFP-HepG2 cells when treated with sorafenib concentrations of 10 and 15 μM, respectively (a). Similar to the patterns in OATP1B1-HepG2 cells, OATP1B1 overexpression in LO2 cells significantly increases sorafenib uptake of sorafenib compared with control of LO2 cells (b). Gene mutations also decrease the intake of sorafenib in OATP1B11b-GFP-LO2 cells (decrease by about 39.02% and 22.76%) and OATP1B115-GFP-LO2 cells (decrease by about 35.94% and 10.57%) compared to those of OATP1B11a-LO2 cells when treated with sorafenib. Concentrations of 10 and 15 μM, respectively (b). Interestingly, sorafenib uptake in HepG2 and OATP1B1-HepG2 cells are all significantly higher than in LO2 and OATP1B11a-LO2 cells (a, b). ; .

(a)

(b)