Source:http://linkedlifedata.com/resource/pubmed/id/17950240
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
2007-11-20
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pubmed:abstractText |
To identify the novel inhibitor of de novo lipogenesis in hepatocytes, we screened for inhibitory activity of triglyceride (TG) synthesis using [14C]acetate in the human hepatoma cell line, HepG2. Using this assay system we discovered the novel compound, benzofuranyl alpha-pyrone (TEI-B00422). TEI-B00422 also inhibited the incorporation of acetate into the triglyceride (TG) fraction in rat primary hepatocytes. In HepG2 cells, the incorporation of oleate into TG was unaffected. TEI-B00422 inhibited rat hepatic acetyl-CoA carboxylase (ACC), K(i)=3.3 microM, in a competitive manner with respect to acety-CoA but not fatty acid synthase and acyl-CoA transferase/diacylglycerol. Thus, these results suggest that the inhibition of TG synthesis by TEI-B00422 is based on the inhibitory action of ACC. The structure of TEI-B00422 is totally different from the known inhibitors of ACC and may be useful in the development of therapeutic agents to combat a number of metabolic disorders.
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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/Acetyl Coenzyme A,
http://linkedlifedata.com/resource/pubmed/chemical/Benzofurans,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Fatty Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrones
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
1096-0384
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
468
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
44-8
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pubmed:meshHeading |
pubmed-meshheading:17950240-Acetyl Coenzyme A,
pubmed-meshheading:17950240-Animals,
pubmed-meshheading:17950240-Benzofurans,
pubmed-meshheading:17950240-Cell Line,
pubmed-meshheading:17950240-Enzyme Inhibitors,
pubmed-meshheading:17950240-Fatty Acids,
pubmed-meshheading:17950240-Hepatoblastoma,
pubmed-meshheading:17950240-Hepatocytes,
pubmed-meshheading:17950240-Humans,
pubmed-meshheading:17950240-Liver Neoplasms,
pubmed-meshheading:17950240-Pyrones,
pubmed-meshheading:17950240-Rats
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pubmed:year |
2007
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pubmed:articleTitle |
A novel acetyl-CoA carboxylase inhibitor reduces de novo fatty acid synthesis in HepG2 cells and rat primary hepatocytes.
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pubmed:affiliation |
Teijin Pharma Limited, Pharmaceutical Discovery Research Laboratories, Institute for Bio-medical Research, 4-3-2, Asahigaoka, Hino Tokyo 191-8512, Japan. y.sugimoto@teijin.co.jp
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pubmed:publicationType |
Journal Article
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