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ABCG2 Transports Sulfated Conjugates of Steroids and Xenobiotics

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Suzuki, Michiko, Suzuki, Hiroshi, Sugimoto, Yoshikazu, Sugiyama, Yuichi·2003·Journal of Biological Chemistry

Abstract

The mechanism for the cellular extrusion of sulfated conjugates is still unknown. In the present study, we investigated whether human wild type ABCG2 transports estrone 3-sulfate (E1S) using membrane vesicles from cDNA-transfected mouse lymphoma cell line (P388 cells). The uptake of [3H]E1S into ABCG2-expressing membrane vesicles was stimulated by ATP, and the Km value for [3H]E1S was determined to be 16.6 microm. The ABCG2-mediated transport of [3H]E1S was potently inhibited by SN-38 and many sulfate conjugates but not by glucuronide and glutathione conjugates or other anionic compounds. Other sulfate conjugates such as [3H]dehydroepiandrosterone sulfate (DHEAS) and [35S]4-methylumbelliferone sulfate (Km = 12.9 microm) and [35S]6-hydroxy-5,7-dimethyl-2-methylamino-4-(3-pyridylmethyl)benzothiazole (E3040) sulfate (Km = 26.9 microm) were also transported by ABCG2. Although [3H]methotrexate, [3H]17beta-estradiol-17beta-D-glucuronide, [3H]2,4-dinitrophenyl-S-glutathione, and [14C]4-methylumbelliferone glucuronide were transported by ABCG2, this took place to a much lesser extent compared with [3H]E1S. It was suggested that ABCG2 preferentially transports sulfate conjugates and that E1S and DHEAS are the potential physiological substrates for this transporter.

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Metadata

Authors
Suzuki, M., Suzuki, H., Sugimoto, Y., & Sugiyama, Y.
Venue
Journal of Biological Chemistry
Publisher
Elsevier BV
Published
2003-06
Volume
278
Issue
25
Pages
22644-22649
ISSN
0021-9258 (ISSN-L)
OpenAlex
W1999004536
Cited by
341
References
1
FWCI
11.49
Type
journal article
Language
en
Open access
hybrid

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CoChat. (2026). Citation check: ABCG2 Transports Sulfated Conjugates of Steroids and Xenobiotics. https://app.cochat.ai/papers/10.1074/jbc.m212399200
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Suzuki, M., Suzuki, H., Sugimoto, Y., & Sugiyama, Y. (2003). ABCG2 Transports Sulfated Conjugates of Steroids and Xenobiotics. Journal of Biological Chemistry. https://doi.org/10.1074/jbc.m212399200

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