Transport of Ethinylestradiol Glucuronide and Ethinylestradiol Sulfate by the Multidrug Resistance Proteins MRP1, MRP2, and MRP3

@article{Chu2004TransportOE,
  title={Transport of Ethinylestradiol Glucuronide and Ethinylestradiol Sulfate by the Multidrug Resistance Proteins MRP1, MRP2, and MRP3},
  author={Xiao-yan Chu and S W Huskey and Matthew P. Braun and Bal{\'a}zs Sarkadi and D. C. Evans and Raymond Evers},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2004},
  volume={309},
  pages={156 - 164}
}
  • X. Chu, S. Huskey, +3 authors R. Evers
  • Published 1 April 2004
  • Biology, Medicine
  • Journal of Pharmacology and Experimental Therapeutics
Ethinylestradiol (EE) is one of the key constituents of oral contraceptives. Major metabolites of EE in humans are the glucuronide and sulfate conjugates, EE-3-O-glucuronide (EE-G) and EE-3-O-sulfate (EE-S). In the present study, transport of EE-G and EE-S by the human multidrug resistance proteins MRP1, MRP2, and MRP3 was investigated using inside-out membrane vesicles, isolated from Sf9 cells expressing human MRP1, MRP2, or MRP3. Vesicular uptake studies showed that EE-G was not a substrate… 
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ESTRADIOL 3-GLUCURONIDE IS TRANSPORTED BY THE MULTIDRUG RESISTANCE-ASSOCIATED PROTEIN 2 BUT DOES NOT ACTIVATE THE ALLOSTERIC SITE BOUND BY ESTRADIOL 17-GLUCURONIDE
TLDR
E217G binds not only to an Mrp2 transport site, but also to an allosteric site that activatesMrp2 with positive cooperativity, thus activating its own transport and potentially that of other Mrp 2 substrates, such as E23G.
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