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. 2017 May 11;14(6):2147–2157. doi: 10.1021/acs.molpharmaceut.7b00308

Figure 2.

Figure 2

Expression and function of renal drug transporters upon cetuximab pretreatment. Cells were pretreated with cetuximab (CTX) before gene and protein expression was determined. The activity of renal drug transporter was evaluated using fluorescent substrates (OAT1, fluorescein; BCRP, Hoechst33342; P-gp, calcein and MRP4; GS-MF, respectively). Changes in transport activity are depicted in fluorescent intensity expressed in arbitrary units (a.u). CTX effectively reduced the expression and activity of OAT1 (A, B) and BCRP (C, D), while increasing the expression and activity of P-gp (E, F) and MRP4 (G, H). Protein expression was determined for OAT1 (60 kDa) and BCRP (72 kDa) (A, C lower panel), Na,K-ATPase was used as loading control (112 kDa). Data are presented as mean values ± SEM, n = 3. Statistical analysis was performed via unpaired Student’s t test. ∗, p < 0.05 and ∗∗∗, p < 0.01 compared to control (+EGF condition).