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
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