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  • Title: Differential effect of phenothiazines on MRP1 and P-glycoprotein activity.
    Author: Wesołowska O, Molnar J, Ocsovszki I, Michalak K.
    Journal: In Vivo; 2009; 23(6):943-7. PubMed ID: 20023237.
    Abstract:
    BACKGROUND: Overexpression of ATP-binding cassette (ABC) transporters such as P-glycoprotein (P-gp), multidrug resistance-associated protein 1 (MRP1) or breast cancer resistance protein (BCRP) accounts for majority of cases of multidrug resistance (MDR) of cancer cells. MATERIALS AND METHODS: In the present work, the interactions of seven commercially available phenothiazine derivatives, known P-glycoprotein inhibitors, with this transporter and MRP1 were compared. By flow cytometry, it was shown that all the drugs increased the accumulation of rhodamine 123 in the P-gp-overexpressing lymphoma cell line L5178 MDR. On the other hand, phenothiazine derivatives stimulated MRP1-mediated efflux of fluorescent probe (BCPCF) out of human erythrocytes. RESULTS: In this way, these phenothiazine derivatives were identified as a group of atypical MDR modulators that differently interact with P-gp (as inhibitors) and MRP1 (as stimulators). CONCLUSION: This observation clearly shows that the activity of all new modulators should be tested for their effects towards different ABC transporters as a standard procedure.
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