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Advances on clinical research of histone demethylase LSD1 inhibitors
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Yu-ting SHI, Xin-yu YANG, Bin YU*, Yi-hui SONG*
Acta Pharmaceutica Sinica | 2022, 57(10) : 2949 - 2959
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Acta Pharmaceutica Sinica | 2022, 57(10): 2949-2959
Special Reports Ⅰ: New Targets, New Strategies for Drug Discovery and Advances in Antiviral Drug Research
Advances on clinical research of histone demethylase LSD1 inhibitors
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Yu-ting SHI, Xin-yu YANG, Bin YU*, Yi-hui SONG*
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  • School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China
Published: 2022-10-12 doi: 10.16438/j.0513-4870.2022-0688
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Lysine-specific demethylase 1 (LSD1) plays vital roles in cell stemness, differentiation, cell motility, metabolic control and epithelial-mesenchymal transition, which is closely associated with tumorigenesis processes including cell proliferation, invasive, metastasis and poor prognosis. Besides, LSD1 also contributes to the occurrence of other diseases such as neurodegenerative diseases and viral infections. Since 2013, the irreversible inhibitors including tranylcypromine, ORY-1001, ORY-2001, GSK-2879552, IMG-7289, INCB059872, TAK-418, LH-1802 and reversible inhibitors including CC-90011 and SP-2577 have been approved for clinical assessment. This review comprehensively summarizes the clinical research of LSD1 drug candidates and briefly discusses the prospects, opportunities and challenges of LSD1-targeted drug discovery, aiming to provide a landscape for the related drug development.

epigenetics  /  histone demethylase  /  lysine-specific demethylase 1 inhibitor  /  clinical trial  /  drug discovery
Yu-ting SHI, Xin-yu YANG, Bin YU, Yi-hui SONG. Advances on clinical research of histone demethylase LSD1 inhibitors[J]. Acta Pharmaceutica Sinica, 2022 , 57 (10) : 2949 -2959 . DOI: 10.16438/j.0513-4870.2022-0688
Year 2022 volume 57 Issue 10
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doi: 10.16438/j.0513-4870.2022-0688
  • Receive Date:2022-06-02
  • Online Date:2025-12-24
  • Published:2022-10-12
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  • Received:2022-06-02
  • Revised:2022-07-04
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    School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
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Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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