دورية أكاديمية
A small molecule that blocks fat synthesis by inhibiting the activation of SREBP
| العنوان: | A small molecule that blocks fat synthesis by inhibiting the activation of SREBP |
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| المؤلفون: | Kamisuki, Shinji, Mao, Qian, Abu-Elheiga, Lutfi, Gu, Ziwei, Kugimiya, Akira, Kwon, Youngjoo, Shinohara, Tokuyuki, Kawazoe, Yoshinori, Sato, Shin-ichi, Asakura, Koko, Choo, Hea-Young Park, Sakai, Juro, Wakil, Salih J, Uesugi, Motonari |
| المساهمون: | 上杉, 志成, 70534478, 10402926 |
| بيانات النشر: | Elsevier |
| سنة النشر: | 2009 |
| المجموعة: | Kyoto University Research Information Repository (KURENAI) / 京都大学学術情報リポジトリ |
| مصطلحات موضوعية: | CHEMBIO, CELLBIO, Animals, Blood Glucose/metabolism, Body Weight, CHO Cells, Cricetinae, Cricetulus, Fatty Acids/biosynthesis, Fatty Acids/metabolism, Humans, Intracellular Signaling Peptides and Proteins/metabolism, Membrane Proteins/metabolism, Mice, Obese, Protein Binding, Protein Structure, Tertiary, Pyridines/chemistry, Pyridines/pharmacology, Sterol Regulatory Element Binding Proteins/antagonists & inhibitors, Sterol Regulatory Element Binding Proteins/chemistry, Sterol Regulatory Element Binding Proteins/metabolism, Thiazoles/chemistry, Thiazoles/pharmacology, Transcription, Genetic |
| الوصف: | 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. |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | application/pdf |
| اللغة: | English |
| تدمد: | 1879-1301 19716478 |
| العلاقة: | http://hdl.handle.net/2433/112665Test; AA11072585; Chemistry & biology; 16; 882; 892 |
| الإتاحة: | http://hdl.handle.net/2433/112665Test |
| حقوق: | © 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。 |
| رقم الانضمام: | edsbas.B548939B |
| قاعدة البيانات: | BASE |
Full Text Finder | تدمد: | 18791301 19716478 |
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