Literature DB >> 9280310

Modulation by (iso)flavonoids of the ATPase activity of the multidrug resistance protein.

J H Hooijberg1, H J Broxterman, M Heijn, D L Fles, J Lankelma, H M Pinedo.   

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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Year:  1997        PMID: 9280310     DOI: 10.1016/s0014-5793(97)00940-x

Source DB:  PubMed          Journal:  FEBS Lett        ISSN: 0014-5793            Impact factor:   4.124


  8 in total

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6.  Potent interaction of flavopiridol with MRP1.

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7.  Perturbation of the lipid phase of a membrane is not involved in the modulation of MRP1 transport activity by flavonoids.

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  8 in total

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