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. Author manuscript; available in PMC: 2012 Jul 14.
Published in final edited form as: J Med Chem. 2011 Jun 8;54(13):4548–4558. doi: 10.1021/jm2001629

Figure 4. Selectivity of OCT2 inhibitors for the polymorphic transporter, OCT2-A270S and other organic cation transporters.

Figure 4

(A) Correlation analyses between OCT2 inhibition and inhibition of OCT2-A270S, the hepatic homologue OCT1, and the apical organic cation transporters MATE1 and MATE2-K. The prototypical organic cation transport inhibitor cimetidine is indicated by the arrows. (B) Venn diagram showing the overlapping inhibitors for OCT2, OCT1, MATE1 and MATE2-K. (C) Selectivity of inhibition for putative clinical inhibitors of OCT2. The concentration dependent inhibition of ASP+ uptake is shown for HEK293 cells stably expressing OCT2-Reference (closed circles), OCT2-A270S (open circles), MATE1 (upward pointing triangles), MATE2-K (downward pointing triangles) and OCT1 (open squares). Data are presented as mean ± s.d. (three separate samples from one representative experiment).