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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, 44(4): 313-附页2.
Citation: 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, 44(4): 313-附页2.

Advances in Research on Tranylcyprominebased Covalent Inhibitors of Lysine-Specific Demethylase 1

  • Histone lysine-specific demethylase 1 (LSD1), which is highly expressed in various tumor cells, plays an important role in functionally regulating methylation degrees of H3K4 and H3K9. 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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