論文 - 詳細
| RRC ID | 43149 |
|---|---|
| 著者 | Sugimoto Y, Naniwa Y, Nakamura T, Kato H, Yamamoto M, Tanabe H, Inoue K, Imaizumi A. |
| タイトル | A novel acetyl-CoA carboxylase inhibitor reduces de novo fatty acid synthesis in HepG2 cells and rat primary hepatocytes. |
| ジャーナル | Arch Biochem Biophys |
| Abstract |
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. |
| 巻・号 | 468(1) |
| ページ | 44-8 |
| 公開日 | 2007-12-1 |
| DOI | 10.1016/j.abb.2007.09.012 |
| PII | S0003-9861(07)00470-5 |
| PMID | 17950240 |
| MeSH | Acetyl Coenzyme A / antagonists & inhibitors* Acetyl Coenzyme A / metabolism* Animals Benzofurans / administration & dosage* Cell Line Enzyme Inhibitors / administration & dosage Fatty Acids / metabolism* Hepatoblastoma / metabolism* Hepatocytes / drug effects Hepatocytes / metabolism* Humans Liver Neoplasms / metabolism* Pyrones / administration & dosage* Rats |
| IF | 3.391 |
| 引用数 | 15 |
| WOS 分野 | BIOPHYSICS BIOCHEMISTRY & MOLECULAR BIOLOGY |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 各媒体での言及数の合計 | 0 |
| リソース情報 | |
| ヒト・動物細胞 | |