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  • Title: Modulation by (iso)flavonoids of the ATPase activity of the multidrug resistance protein.
    Author: Hooijberg JH, Broxterman HJ, Heijn M, Fles DL, Lankelma J, Pinedo HM.
    Journal: FEBS Lett; 1997 Aug 18; 413(2):344-8. PubMed ID: 9280310.
    Abstract:
    The multidrug resistance protein (MRP) is an ATP-dependent transport protein for organic anions, as well as neutral or positively charged anticancer agents. In this study we report that dinitrophenyl-S-glutathione increases ATPase activity in plasma membrane vesicles prepared from the MRP-overexpressing cell line GLC4/ADR. This ATPase stimulation parallels the uptake of DNP-SG in these vesicles. We also show that the (iso)flavonoids genistein, kaempferol and flavopiridol stimulate the ATPase activity of GLC4/ADR membranes, whereas genistin has no effect. The present data are consistent with the hypothesis that certain (iso)flavonoids affect MRP-mediated transport of anticancer drugs by a direct interaction with MRP.
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