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

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

Research output: Contribution to journalArticle

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.

Original languageEnglish (US)
Pages (from-to)344-348
Number of pages5
JournalFEBS Letters
Volume413
Issue number2
DOIs
StatePublished - Aug 18 1997
Externally publishedYes

Keywords

  • (Iso)flavonoids
  • ATPase
  • Dinitrophenyl-S-glutathione
  • Flavopiridol
  • Multidrug resistance
  • Multidrug resistance protein

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

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  • Cite this

    Hooijberg, J. H., Broxterman, H. J., Heijn, M., Fles, D. L. A., Lankelma, J., & Pinedo, H. M. (1997). Modulation by (iso)flavonoids of the ATPase activity of the multidrug resistance protein. FEBS Letters, 413(2), 344-348. https://doi.org/10.1016/S0014-5793(97)00940-X