Design and synthesis of emodin derivatives as novel inhibitors of ATP-citrate lyase

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• 作者：Steffi K. Koerner^a ; Jun-ichi Hanai^b ; ^c ; Sha Bai^a ; Finith E. Jernigan^a ; Miwa Oki^b ; Chieko Komaba^b ; Emi Shuto^b ; Vikas P. Sukhatme^b ; ^c ; ^d ; ^{vsukhatm@bidmc.harvard.edu} ; Lijun Sun^a ; ^{lsun1@bidmc.harvard.edu}
• 关键词：Emodin anthraquinones and anthracenone ; ATP citrate lyase inhibitor ; Lipogenesis ; Cancer stem cell
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：920-928
• 全文大小：1604 K
• 卷排序：126

文摘

Emodin anthraquinones inhibited the enzymatic activity ATP-citrate lyase (ACL), a key player in cancer cell metabolism. Lead compound 1d inhibited A549 lung cancer cell proliferation and reduced the stemness of A549 cells. Docking suggested that anthraquinone inhibitors occupied an allosteric site adjacent to the citrate-binding domain of ACL.