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

doi:10.1016/S0014-5793(97)00940-X

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 journal › Article › peer-review

112 Scopus citations

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 language	English (US)
Pages (from-to)	344-348
Number of pages	5
Journal	FEBS Letters
Volume	413
Issue number	2
DOIs	https://doi.org/10.1016/S0014-5793(97)00940-X
State	Published - Aug 18 1997
Externally published	Yes

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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10.1016/S0014-5793(97)00940-X

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title = "Modulation by (iso)flavonoids of the ATPase activity of the multidrug resistance protein",

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.",

keywords = "(Iso)flavonoids, ATPase, Dinitrophenyl-S-glutathione, Flavopiridol, Multidrug resistance, Multidrug resistance protein",

author = "Hooijberg, {J. H.} and Broxterman, {H. J.} and M. Heijn and Fles, {D. L A} and J. Lankelma and Pinedo, {H. M.}",

year = "1997",

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language = "English (US)",

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AU - Hooijberg, J. H.

AU - Broxterman, H. J.

AU - Heijn, M.

AU - Fles, D. L A

AU - Lankelma, J.

AU - Pinedo, H. M.

PY - 1997/8/18

Y1 - 1997/8/18

N2 - 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.

AB - 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.

KW - (Iso)flavonoids

KW - ATPase

KW - Dinitrophenyl-S-glutathione

KW - Flavopiridol

KW - Multidrug resistance

KW - Multidrug resistance protein

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DO - 10.1016/S0014-5793(97)00940-X

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SN - 0014-5793

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JO - FEBS Letters

JF - FEBS Letters

IS - 2

ER -

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

Abstract

Keywords

ASJC Scopus subject areas

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