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タイトル: A small molecule that blocks fat synthesis by inhibiting the activation of SREBP
著者: Kamisuki, Shinji
Mao, Qian
Abu-Elheiga, Lutfi
Gu, Ziwei
Kugimiya, Akira
Kwon, Youngjoo
Shinohara, Tokuyuki
Kawazoe, Yoshinori
Sato, Shin-ichi  KAKEN_id
Asakura, Koko
Choo, Hea-Young Park
Sakai, Juro
Wakil, Salih J
Uesugi, Motonari  kyouindb  KAKEN_id  orcid https://orcid.org/0000-0002-8515-445X (unconfirmed)
著者名の別形: 上杉, 志成
キーワード: CHEMBIO
CELLBIO
発行日: 28-Aug-2009
出版者: Elsevier
誌名: Chemistry & biology
巻: 16
号: 8
開始ページ: 882
終了ページ: 892
抄録: Sterol regulatory element binding proteins (SREBPs) are transcription factors that activate transcription of the genes involved in cholesterol and fatty acid biosynthesis. In the present study, we show that a small synthetic molecule we previously discovered to block adipogenesis is an inhibitor of the SREBP activation. The diarylthiazole derivative, now called fatostatin, impairs the activation process of SREBPs, thereby decreasing the transcription of lipogenic genes in cells. Our analysis suggests that fatostatin inhibits the ER-Golgi translocation of SREBPs through binding to their escort protein, the SREBP cleavage-activating protein (SCAP), at a distinct site from the sterol-binding domain. Fatostatin blocked increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice, even under uncontrolled food intake. Fatostatin may serve as a tool for gaining further insights into the regulation of SREBP.
著作権等: © 2009 Elsevier
This is not the published version. Please cite only the published version.
この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。
URI: http://hdl.handle.net/2433/112665
DOI(出版社版): 10.1016/j.chembiol.2009.07.007
PubMed ID: 19716478
出現コレクション:学術雑誌掲載論文等

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