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Study of substance transport via membrane transporters
 Halamová, Zuzana ; Smutná, Lucie (advisor) ; Maixnerová, Jana (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Student: Zuzana Halamová Supervisor: PharmDr. Lucie Smutná, PhD. Title of diploma thesis: Study of substance transport via membrane transporters Wide range of specialized transport proteins expressed mainly in the kidney proximal tubule ensures the excretion of endogenous and exogenous substances. OCT2 (organic cation transporter 2) is localized on the basolateral membrane of the kidney proximal tubule, the transporter transports broad spectrum of structurally different substances. Drug-drug interactions may occur at the level of this transporter due to its broad substrate specificity. Within this diploma thesis the accumulation of the radiolabeled antiviral agent [3 H]lamivudine and the model hOCT2 substrate [3 H]MPP+ was evaluated using accumulation and transport studies. The canine kidney cells MDCKII or human cell line HeLa were used as model cell lines. Mentioned cell lines expressed the human OCT2 transporter stably or transiently. The antibacterial chemotherapy agent trimethoprim was used as competitive inhibitor of OCT2 transporter. The results indicate the lamivudine accumulation in the cells with OCT2 is low compared to accumulation of MPP+ . Accumulation studies showed that lamivudine had a...
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