| 赖氨酸特异性去甲基酶1反苯环丙胺类不可逆抑制剂的研究进展 |
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| 引用本文： | 高琦冰,刘超亿,孙旭东,马超亚,王志正,郑甲信,丁丽娜.赖氨酸特异性去甲基酶1反苯环丙胺类不可逆抑制剂的研究进展[J].药学进展,2020(4):313-320,I0003,I0004. |
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| 作者姓名： | 高琦冰 刘超亿 孙旭东 马超亚 王志正 郑甲信 丁丽娜 |
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| 作者单位： | 郑州大学药学院药物关键制备技术教育部重点实验室 |
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| 基金项目： | 国家自然科学基金青年项目(No.21403200);国家自然科学基金重点项目(No.81430085)。 |
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| 摘 要： | 组蛋白赖氨酸特异性去甲基酶1(LSD1)在调节组蛋白H3K4、H3K9的甲基化状态中起重要作用,在多种肿瘤细胞中高表达,已成为一种新型抗肿瘤靶点。目前为止,已报道的LSD1抑制剂中对反苯环丙胺(TCP)类抑制剂的研究相对更为深入。综述TCP类抑制剂的作用机制、与辅酶黄素腺嘌呤二核苷酸(FAD)结合模式及设计优化的研究进展。
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| 关 键 词： | 组蛋白赖氨酸特异性去甲基酶1 反苯环丙胺类抑制剂 抑制机制 结合模式 |
Advances in Research on Tranylcyprominebased Covalent Inhibitors of Lysine-Specific Demethylase 1 |
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| GAO Qibing,LIU Chaoyi,SUN Xudong,MA Chaoya,WANG Zhizheng,ZHENG Jiaxin,DING Lina.Advances in Research on Tranylcyprominebased Covalent Inhibitors of Lysine-Specific Demethylase 1[J].Progress in Pharmaceutical Sciences,2020(4):313-320,I0003,I0004. |
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| Authors: | GAO Qibing LIU Chaoyi SUN Xudong MA Chaoya WANG Zhizheng ZHENG Jiaxin DING Lina |
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| Institution: | (College of Pharmacy,Key Laboratory of Advanced Drug Preparation Technologies of the Ministry of Education,Zhengzhou University,Zhengzhou 450001,China) |
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| Abstract: | Histone lysine-specific demethylase 1(LSD1), which is highly expressed in various tumor cells, plays an important role in functionally regulating methylation degrees of H3 K4 and H3 K9. Therefore, it has already been known as a new anti-tumor target. Up to now, deeper researches have been focused on tranylcypromine(TCP)-based inhibitors in all kinds of LSD1 inhibitors. This review aims at TCP’s mechanism of inhibition, the modes of combination with coenzyme flavin adenine dinucleotide( FAD) and optimization of its design. |
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| Keywords: | histone lysine-specific demethylase 1 tranylcypromine-based inhibitor inhibition mechanism binding mode |
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