Please use this identifier to cite or link to this item: https://doi.org/10.1016/j.ejmech.2019.111597
Title: Galloyl esters of trans-stilbenes are inhibitors of FASN with anticancer activity on non-small cell lung cancer cells
Authors: Tan, Yu-Jia
Ali, Azhar 
Tee, Sheng-Yang
Teo, Jun-Ting 
Xi, Yu
Go, Mei-Lin 
Lam, Yulin 
Keywords: Science & Technology
Life Sciences & Biomedicine
Chemistry, Medicinal
Pharmacology & Pharmacy
FASN inhibitors
Anticancer
Galloyl esters of trans-stilbenes
Non-small cell lung cancer
EGCG
FATTY-ACID SYNTHASE
EPIGALLOCATECHIN GALLATE
NATURAL INHIBITOR
OVEREXPRESSION
POLYPHENOLS
ACTIVATION
APOPTOSIS
PATHWAY
KINASE
GROWTH
Issue Date: 11-Mar-2020
Publisher: ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citation: Tan, Yu-Jia, Ali, Azhar, Tee, Sheng-Yang, Teo, Jun-Ting, Xi, Yu, Go, Mei-Lin, Lam, Yulin (2020-03-11). Galloyl esters of trans-stilbenes are inhibitors of FASN with anticancer activity on non-small cell lung cancer cells. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 182. ScholarBank@NUS Repository. https://doi.org/10.1016/j.ejmech.2019.111597
Abstract: Fatty acid synthase (FASN) is a lipogenic enzyme that is selectively upregulated in malignant cells. There is growing consensus on the oncogenicity of FASN-driven lipogenesis and the potential of FASN as a druggable target in cancer. Here, we report the synthesis and FASN inhibitory activities of two novel galloyl esters of trans-stilbene EC1 and EC5. Inhibition of FASN was accompanied by a loss in AKT activation and profound apoptosis in several non-small cell lung cancer (NSCLC) cells at the growth inhibitory concentrations of EC1 and EC5. Both FASN and phospho-AKT levels were concurrently downregulated. However, addition of a lipid concentrate to the treated cells reinstated cell viability and reversed the loss of FASN and AKT protein levels, thus recapitulating the causal relationship between FASN inhibition and the loss in cell viability.
Source Title: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
URI: https://scholarbank.nus.edu.sg/handle/10635/226660
ISSN: 0223-5234
1768-3254
DOI: 10.1016/j.ejmech.2019.111597
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