Hezhong Jiang, Tian Gan, Jiasui Zhang, Qingyun Ma, Yan Liang* and Youxing Zhao* Pages 7081 - 7101 ( 21 )
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.Fatty acid synthase (FAS), inhibitors, structures, inhibitory activities, structure-activity relationships (SAR), anti-obesity, anti-cancer.
School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou 571101, School of Kinesiology and Health, Capital University of Physical Education and Sports, Beijing 100191, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou 571101