Source:http://linkedlifedata.com/resource/pubmed/id/20347305
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
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pubmed:dateCreated |
2010-4-20
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pubmed:abstractText |
Cucurbitane-type triterpenes, cucurbitacins B and E, were reported to exhibit cytotoxic effects in several cell lines mediated by JAK/STAT3 signaling. However, neither compound inhibited phosphorylation of STAT3 in human leukemia (U937) cells at low concentrations. We therefore synthesized a biotin-linked cucurbitacin E to isolate target proteins based on affinity for the molecule. As a result, cofilin, which regulates the depolymerization of actin, was isolated and suggested to be a target. Cucurbitacins E and I inhibited the phosphorylation of cofilin in a concentration-dependent manner, and their effective concentrations having the same range as the concentrations at which they had cytotoxic effects in U937 cells. In addition, the fibrous-/globular-actin ratio was decreased after treatment with cucurbitacin E in HT1080 cells. These findings suggested that the inhibition of cofilin's phosphorylation increased the severing activity of cofilin, and then the depolymerization of actin was enhanced after treatment with cucurbitacin E at lower concentrations.
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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/Actins,
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Cofilin 1,
http://linkedlifedata.com/resource/pubmed/chemical/STAT3 Transcription Factor,
http://linkedlifedata.com/resource/pubmed/chemical/STAT3 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Triterpenes,
http://linkedlifedata.com/resource/pubmed/chemical/cucurbitacin B,
http://linkedlifedata.com/resource/pubmed/chemical/cucurbitacin E,
http://linkedlifedata.com/resource/pubmed/chemical/cucurbitacin I
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:copyrightInfo |
2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2994-7
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pubmed:meshHeading |
pubmed-meshheading:20347305-Actins,
pubmed-meshheading:20347305-Antineoplastic Agents,
pubmed-meshheading:20347305-Cell Line, Tumor,
pubmed-meshheading:20347305-Cofilin 1,
pubmed-meshheading:20347305-Humans,
pubmed-meshheading:20347305-Phosphorylation,
pubmed-meshheading:20347305-STAT3 Transcription Factor,
pubmed-meshheading:20347305-Triterpenes,
pubmed-meshheading:20347305-U937 Cells
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pubmed:year |
2010
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pubmed:articleTitle |
Cucurbitacin E as a new inhibitor of cofilin phosphorylation in human leukemia U937 cells.
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pubmed:affiliation |
Department of Pharmacognosy, Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto 607-8412, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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