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The Structures and Bioactivities of Fatty Acid Synthase Inhibitors

文献类型： 外文期刊

作者： Jiang, Hezhong 1 ; Gan, Tian 1 ; Zhang, Jiasui 1 ; Ma, Qingyun 2 ; Liang, Yan 3 ; Zhao, Youxing 2 ;

作者机构： 1.Southwest Jiaotong Univ, Sch Life Sci & Engn, Chengdu 610031, Sichuan, Peoples R China

2.Chinese Acad Trop Agr Sci, Inst Trop Biosci & Biotechnol, Haikou 571101, Hainan, Peoples R China

3.Capital Univ Phys Educ & Sports, Sch Kinesiol & Hlth, Beijing 100191, Peoples R China

关键词： Fatty acid synthase (FAS); inhibitors; structures; inhibitory activities; structure-activity relationships (SAR); anti-obesity; anti-cancer

期刊名称：CURRENT MEDICINAL CHEMISTRY （ 影响因子：4.53； 五年影响因子：4.676 ）

ISSN： 0929-8673

年卷期： 2019 年 26 卷 39 期

页码：

收录情况： SCI

摘要： Background: Fatty Acid Synthase (FAS or FASN) is a vital enzyme which catalyzes the de novo synthesis of long chain fatty acids. A number of studies have recently been reported that FAS was combined targets for the discovery of anti-obesity and anti-cancer drugs. Great interest has been developed in finding novel FAS inhibitors, and result in more than 200 inhibitors being reported. Methods: The reported research literature about the FAS inhibitors was collected and analyzedsised through major databases including Web of Science, and PubMed. Then the chemical stractures, FAS inhibitory activities, and Structure-Activity Relationships (SAR) were summarized focused on all these reported FAS inhibitors. Results: The 248 FAS inhibitors, which were reported during the past 20 years, could be divided into thiolactone, butyrolactone and butyrolactam, polyphenols, alkaloids, terpenoids, and other structures, in view of their structure characteristics. And the SAR of high inhibitory structures of each type was proposed in this paper. Conclusion: A series of synthetic quinolinone derivatives show strongest inhibitory activity in the reported FAS inhibitors. Natural polyphenols, existing in food and herbs, show more adaptive in medicine exploration because of their safety and efficiency. Moreover, screening the FAS inhibitors from microorganism and marine natural products could be the hot research directions in the future.

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