Structure-based design of ester compounds to inhibit MLL complex catalytic activity by targeting mixed lineage leukemia 1 (MLL1)-WDR5 interaction
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- 作者：Dong-Dong Lia ; Zhi-Hui Wanga ; Wei-Lin Chena ; Yi-Yue Xiea ; Qi-Dong Youa ; b ; youqidong@gmail.com" class="auth_mail" title="E-mail the corresponding author ; Xiao-Ke Guoa ; b ; kexin95@126.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：MLL1&ndash ; WDR5 interaction ; Histone methyltransferase ; Ester compounds ; Leukemia ; Docking
- 刊名：Bioorganic & Medicinal Chemistry
- 出版年：2016
- 出版时间：15 November 2016
- 年：2016
- 卷：24
- 期：22
- 页码：6109-6118
- 全文大小：1375 K
文摘
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A series of ester compounds were designed and synthetized to disturb MLL1–WDR5 interaction.
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WL-5 and WL-15 effectively inhibited MLL1-dependent H3K4 methylation in vitro.
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Representative ester compounds selectively inhibited the proliferation of MV4-11 cells.
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Docking study was applied to elucidate the binding model of ester compounds.