Discovery of novel small molecule inhibitors of lysine methyltransferase G9a and their mechanism in leukemia cell lines
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- 作者：Shukkoor M. Kondengadena ; 1 ; Liu-fei Luob ; 1 ; Kenneth Huanga ; Mengyuan Zhua ; Lanlan Zanga ; c ; Eudoxie Batabaa ; Runling Wangc ; Cheng Luod ; Binghe Wanga ; Keqin Kathy Lia ; b ; kli10@gsu.edu" class="auth_mail" title="E-mail the corresponding author ; Peng George Wanga ; pwang11@gsu.edu" class="auth_mail" title="E-mail the corresponding author
- 关键词：Lysine methyltransferase ; G9a inhibitor ; Leukemia ; MALDI-TOF assay
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：21 October 2016
- 年：2016
- 卷：122
- 期：Complete
- 页码：382-393
- 全文大小：2045 K
文摘
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Performed Structure based virtual screening on SPECS database for G9a inhibitors.
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4 novel, nonquinazoline small molecules were discovered as G9a inhibitors.
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DCG066 having the best activity.
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Binding studies indicate same characteristics as other H3 mimetics.
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DCG066 inhibits cancer cell proliferation, blocks cell cycle and induces apoptosis.
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