Formation of DNA adducts by chemically reactive substrate is one of the main factors leading to carcinogenesis. Methylpyrenes are converted to sulfooxymethylpyrenes in the liver, and are transported via the blood to kidneys, where they lead to DNA adducts. In a recent study, Bakiya et. al. demonstrated the interaction of organic anion transporter 1 and 3 (OAT1, OAT3) with 1-sulfooxymethylpyrene(1-SMP),2-SMP and 4-SMP. In the present study we examined the interaction of OAT4, which is located at the luminal side of renal proximal tubule cells and in placenta, with 1-SMP, 2-SMP 4-SMP and a-1- sulfooxyethylpyrenes (a-1-SEP) and W-1-SEP. OAT4 mediated [3H]estrone sulfate (ES) uptake was inhibited by 1-SMP, 2-SMP 4-SMP and W-1-SEP in a concentration dependent manner, but not by a-1-SEP. The calculated IC50 value for 2-SMP, 4-SMP and W-1-SEP for OAT4 mediated ES uptake were 3.3 ± 0.2 mM, 5.1 ± 1.3 mM and 3.6 ± 0.3 mM, respectively. Additionally, we measured uptake of 4-SMP by HPLC. OAT4 expressing cells showed a 2.6 fold higher accumulation of 4-SMP than control cells, which was abolished by probenecid. These data document that the uptake of sulfooxymethlpyrenes is facilitated by basolateral as well as luminal Organic Anion Transporters of proximal tubule cells and hence, could be an important factor in renal carcinogenesis.