European Journal of Medicinal Chemistry (2019)
Update date:2022-08-15
Topics:
Tan, Yu-Jia
Ali
Tee, Sheng-Yang
Teo, Jun-Ting
Xi, Yu
Go, Mei-Lin
Lam
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.
View MoreShanghai Norky Pharmaceutical Co., LTD.
website:http://www.norkypharm.com
Contact:86-21-61075300
Address:1165 Jiangning Road, Office 1502, Shanghai, China
Shijiazhuang Haitian Amino Acid Co., Ltd.
Contact:+86-311-88908111
Address:Shijiazhuang Hebei province,China
Jiangxi Hessence Chemicals Co., Ltd.
Contact:+86 796 3511924
Address:Chengxi Industrial Park, Jishui County, Jiangxi Province 331600 China.
Contact:86 311 85902108 / 85902109
Address:room 1001-1005 ,huanghe Road ,shijiazhuang ,China
Zhejiang Chemicals Import & Export Corporation
Contact:86-571-87043088
Address:No.37,Qingchun Road,Hangzhou,China
Doi:10.1021/ja00206a040
(1989)Doi:10.1002/ejoc.200900951
(2009)Doi:10.1021/jm00174a017
(1990)Doi:10.1021/ic1006082
(2010)Doi:10.1080/17415991003682617
(2010)Doi:10.1002/ejoc.200901224
(2010)