Potent interaction of flavopiridol with MRP1

J.H. Hooijberg; H.J. Broxterman; G.L. Scheffer; C. Vrasdonk; M. Heijn; M.C. de Jong; R.J. Scheper; J. Lankelma; H.M. Pinedo

doi:10.1038/sj.bjc.6690687

Potent interaction of flavopiridol with MRP1

J.H. Hooijberg, H.J. Broxterman, G.L. Scheffer, C. Vrasdonk, M. Heijn, M.C. de Jong, R.J. Scheper, J. Lankelma, H.M. Pinedo

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Abstract

The multidrug resistance protein 1 (MRP1) is an ATP-dependent transport protein for organic anions, as well as neutral or positively charged anticancer agents. In this study we show that flavopiridol, a synthetic flavonoid currently studied in phase 1 trials for its anti-prolifetative characteristics, interacts with MRP1 in a potent way. Flavopiridol, as well as other (iso)flavonoids stimulate the ATPase activity of MRP1 in a dose-dependent way at low micromolar concentrations. A new specific monoclonal antibody against MRP1 (MIB6) inhibits the (iso)flavonoid-induced ATPase activity of plasma membrane vesicles prepared from the MRP1 overexpressing cell line GLC

Original language	English
Pages (from-to)	269-276
Journal	British Journal of Cancer
Volume	81
DOIs	https://doi.org/10.1038/sj.bjc.6690687
Publication status	Published - 1999

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title = "Potent interaction of flavopiridol with MRP1",

abstract = "The multidrug resistance protein 1 (MRP1) is an ATP-dependent transport protein for organic anions, as well as neutral or positively charged anticancer agents. In this study we show that flavopiridol, a synthetic flavonoid currently studied in phase 1 trials for its anti-prolifetative characteristics, interacts with MRP1 in a potent way. Flavopiridol, as well as other (iso)flavonoids stimulate the ATPase activity of MRP1 in a dose-dependent way at low micromolar concentrations. A new specific monoclonal antibody against MRP1 (MIB6) inhibits the (iso)flavonoid-induced ATPase activity of plasma membrane vesicles prepared from the MRP1 overexpressing cell line GLC",

author = "J.H. Hooijberg and H.J. Broxterman and G.L. Scheffer and C. Vrasdonk and M. Heijn and {de Jong}, M.C. and R.J. Scheper and J. Lankelma and H.M. Pinedo",

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doi = "10.1038/sj.bjc.6690687",

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T1 - Potent interaction of flavopiridol with MRP1

AU - Hooijberg, J.H.

AU - Broxterman, H.J.

AU - Scheffer, G.L.

AU - Vrasdonk, C.

AU - Heijn, M.

AU - de Jong, M.C.

AU - Scheper, R.J.

AU - Lankelma, J.

AU - Pinedo, H.M.

PY - 1999

Y1 - 1999

N2 - The multidrug resistance protein 1 (MRP1) is an ATP-dependent transport protein for organic anions, as well as neutral or positively charged anticancer agents. In this study we show that flavopiridol, a synthetic flavonoid currently studied in phase 1 trials for its anti-prolifetative characteristics, interacts with MRP1 in a potent way. Flavopiridol, as well as other (iso)flavonoids stimulate the ATPase activity of MRP1 in a dose-dependent way at low micromolar concentrations. A new specific monoclonal antibody against MRP1 (MIB6) inhibits the (iso)flavonoid-induced ATPase activity of plasma membrane vesicles prepared from the MRP1 overexpressing cell line GLC

AB - The multidrug resistance protein 1 (MRP1) is an ATP-dependent transport protein for organic anions, as well as neutral or positively charged anticancer agents. In this study we show that flavopiridol, a synthetic flavonoid currently studied in phase 1 trials for its anti-prolifetative characteristics, interacts with MRP1 in a potent way. Flavopiridol, as well as other (iso)flavonoids stimulate the ATPase activity of MRP1 in a dose-dependent way at low micromolar concentrations. A new specific monoclonal antibody against MRP1 (MIB6) inhibits the (iso)flavonoid-induced ATPase activity of plasma membrane vesicles prepared from the MRP1 overexpressing cell line GLC

U2 - 10.1038/sj.bjc.6690687

DO - 10.1038/sj.bjc.6690687

M3 - Article

SN - 0007-0920

VL - 81

SP - 269

EP - 276

JO - British Journal of Cancer

JF - British Journal of Cancer

ER -

Potent interaction of flavopiridol with MRP1

Abstract

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