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Title: A small molecule that blocks fat synthesis by inhibiting the activation of SREBP
Authors: 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 (unconfirmed)
Author's alias: 上杉, 志成
Keywords: CHEMBIO
Issue Date: 28-Aug-2009
Publisher: Elsevier
Journal title: Chemistry & biology
Volume: 16
Issue: 8
Start page: 882
End page: 892
Abstract: 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.
Rights: © 2009 Elsevier
This is not the published version. Please cite only the published version.
DOI(Published Version): 10.1016/j.chembiol.2009.07.007
PubMed ID: 19716478
Appears in Collections:Journal Articles

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