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Issue 11, 2013
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Small-molecule inhibitors of SREBP activation – potential for new treatment of metabolic disorders

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Abstract

Sterol regulatory element-binding proteins (SREBPs) are transcriptional factors that control lipid and cholesterol metabolism. Activation of SREBPs in response to a decrease in cellular sterols results in acceleration of the synthesis of fatty acids, triglycerides, and cholesterol. Aberrant SREBP activity has been linked to metabolic disease states, such as obesity, fatty liver, insulin resistance, hyperlipidemia, and atherosclerosis. Thus, inhibition of SREBP activation is a potential therapeutic approach to treating metabolic disorders. This review focuses on direct or indirect small-molecule inhibitors of SREBP activation.

Graphical abstract: Small-molecule inhibitors of SREBP activation – potential for new treatment of metabolic disorders

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Publication details

The article was received on 20 Jun 2013, accepted on 15 Aug 2013 and first published on 19 Aug 2013


Article type: Review Article
DOI: 10.1039/C3MD00177F
Citation: Med. Chem. Commun., 2013,4, 1422-1433
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    Small-molecule inhibitors of SREBP activation – potential for new treatment of metabolic disorders

    M. Watanabe and M. Uesugi, Med. Chem. Commun., 2013, 4, 1422
    DOI: 10.1039/C3MD00177F

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