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September 1, 2001Journal of Biological ChemistryOpen Access

Transport of Cyclic Nucleotides and Estradiol 17-β-d-Glucuronide by Multidrug Resistance Protein 4

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Authors

ZCZhe‐Sheng ChenKLKun Hee LeeGKGary D. Kruh

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Overview

In vitro study reveals ATP-dependent transport of cyclic nucleotides and estradiol glucuronide by MRP4, indicating a specialized role in cellular signaling and anticancer drug resistance.

Key Points

  • To identify the substrate selectivity, transport kinetics, and physiological roles of human multidrug resistance protein 4 (MRP4).
  • Generated insect cell membrane vesicles expressing human MRP4 via baculovirus infection.
  • Measured MgATP-dependent vesicular transport kinetics (Km and Vmax) for cyclic nucleotides and estradiol 17-beta-D-glucuronide (E217betaG).
  • Assessed the cellular drug resistance profile conferred by MRP4 against purine antimetabolite analogs.
  • MRP4 mediated MgATP-dependent transport of cGMP (Km = 9.7 ± 2.3 µM; Vmax = 2.0 ± 0.3 pmol/mg/min), cAMP (Km = 44.5 ± 5.8 µM; Vmax = 4.1 ± 0.4 pmol/mg/min), and E217betaG (Km = 30.3 ± 6.2 µM; Vmax = 102 ± 16 pmol/mg/min).
  • MRP4 expression conferred resistance to the anticancer purine nucleotide analogs 6-mercaptopurine and 6-thioguanine.

Cite This Study

Chen et al. (2001) studied this question.

synapsesocial.com/papers/6a714c49febe604dd709fda3https://doi.org/10.1074/jbc.m104833200
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