Source:http://linkedlifedata.com/resource/pubmed/id/12711022
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
2-3
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| pubmed:dateCreated |
2003-4-24
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| pubmed:abstractText |
The endogenous oestrogen metabolite, 2-methoxyoestradiol (2-MeOE2) inhibits the growth of breast cancer cells and is also a potent anti-angiogenic agent. We have previously shown that the 3-sulphamoylated derivatives of 2-methoxyoestrogens are more potent than the non-sulphamoylated compounds. In this study, we have compared the abilities of 2-methoxyoestradiol-bis-sulphamate (2-MeOE2bisMATE) and 2-MeOE2 to inhibit the growth of MCF-7 breast cancer cells. Both compounds inhibited cell growth with the IC(50) for 2-MeOE2bisMATE (0.4 microM) being six-fold lower than that for 2-MeOE2 (2.5 microM). Oestrogen sulphamates are potent inhibitors of steroid sulphatase (STS) activity. 2-MeOE2bisMATE was found to retain its STS inhibitory activity and in a placental microsome assay system it was equipotent with oestrone-3-O-sulphamate (EMATE). An in vivo study was also carried out to compare the potency of 2-MeOE2bisMATE with that of EMATE and the non-steroidal STS inhibitor, 667 coumarin sulphamate (667 COUMATE). After a single oral dose (10mg/kg) some recovery of STS activity was detected by day 3 (10%) with activity partially restored (55%) by day 7 after administration of 667 COUMATE. For the other two steroidal compounds, STS activity remained almost completely inactivated for up to 5 days with complete restoration of activity occurring by day 15. The anti-proliferative and STS inhibitory properties of 2-MeOE2bisMATE suggest that it has considerable potential for development as a novel anti-cancer drug.
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/2-methoxyestradiol,
http://linkedlifedata.com/resource/pubmed/chemical/667 coumate,
http://linkedlifedata.com/resource/pubmed/chemical/Arylsulfatases,
http://linkedlifedata.com/resource/pubmed/chemical/Coumarins,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Estradiol,
http://linkedlifedata.com/resource/pubmed/chemical/Steryl-Sulfatase,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfonamides,
http://linkedlifedata.com/resource/pubmed/chemical/coumarin
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| pubmed:status |
MEDLINE
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| pubmed:month |
Feb
|
| pubmed:issn |
0960-0760
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| pubmed:author | |
| pubmed:issnType |
Print
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| pubmed:volume |
84
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
351-8
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| pubmed:dateRevised |
2006-11-15
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| pubmed:meshHeading |
pubmed-meshheading:12711022-Animals,
pubmed-meshheading:12711022-Arylsulfatases,
pubmed-meshheading:12711022-Cell Division,
pubmed-meshheading:12711022-Coumarins,
pubmed-meshheading:12711022-Dose-Response Relationship, Drug,
pubmed-meshheading:12711022-Enzyme Inhibitors,
pubmed-meshheading:12711022-Estradiol,
pubmed-meshheading:12711022-Female,
pubmed-meshheading:12711022-Humans,
pubmed-meshheading:12711022-Inhibitory Concentration 50,
pubmed-meshheading:12711022-Microsomes,
pubmed-meshheading:12711022-Models, Chemical,
pubmed-meshheading:12711022-Placenta,
pubmed-meshheading:12711022-Rats,
pubmed-meshheading:12711022-Rats, Wistar,
pubmed-meshheading:12711022-Steryl-Sulfatase,
pubmed-meshheading:12711022-Sulfonamides,
pubmed-meshheading:12711022-Time Factors,
pubmed-meshheading:12711022-Tumor Cells, Cultured
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| pubmed:year |
2003
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| pubmed:articleTitle |
Inhibition of MCF-7 breast cancer cell proliferation and in vivo steroid sulphatase activity by 2-methoxyoestradiol-bis-sulphamate.
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| pubmed:affiliation |
Endocrinology and Metabolic Medicine, Faculty of Medicine and Sterix Ltd., Imperial College, St. Mary's Hospital, London W2 1NY, UK. b.malini@ic.ac.uk
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| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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