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Advances in the study of tumorigenesis and progression mechanism of LSD1 and its targeting strategies
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Shu-yuan DAI, Lang CHEN, Xiao-xi LÜ, Shuang SHANG*, Fang HUA*
Acta Pharmaceutica Sinica | 2026, 61(5) : 1435 - 1449
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Acta Pharmaceutica Sinica | 2026, 61(5): 1435-1449
• Reviews •
Advances in the study of tumorigenesis and progression mechanism of LSD1 and its targeting strategies
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Shu-yuan DAI, Lang CHEN, Xiao-xi LÜ, Shuang SHANG*, Fang HUA*
Affiliations
  • State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, State Key Laboratory of Digestive Health, CAMS Key Laboratory of Molecular Mechanism and Target Discovery of Metabolic Disorder and Tumorigenesis, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
Published: 2026-05-12 doi: 10.16438/j.0513-4870.2026-0002
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Lysine-specific demethylase 1 (LSD1) is a member of the flavin adenine dinucleotide (FAD)-dependent monoamine oxidase family and is highly expressed in various tumor cells. LSD1 plays a crucial role in tumor progression by participating in multiple processes such as tumor cell proliferation, invasion, differentiation, and immune cell killing. Studies have shown that LSD1 exerts its oncogenic functions not only by demethylating histone and non-histone substrates but also through demethylase activity-independent protein-protein interactions, thereby diversifying its mechanisms of action. With the increasing depth of research into the tumor-promoting mechanisms of LSD1, targeting LSD1 for cancer therapy has become a major focus in the field. This review summarizes the oncogenic functions of LSD1 through its interactions with different proteins and provides an overview of LSD1 inhibitors that have entered clinical stages. A comprehensive understanding of the roles of LSD1 in tumors will offer theoretical support for developing more effective and specific LSD1 inhibitors, thereby guiding future directions for enhanced anti-tumor therapies targeting LSD1.

lysine-specific demethylase 1  /  tumor  /  histone  /  protein-protein interaction  /  tumor immune microenvironment
戴舒远, 陈朗, 吕晓希, 尚爽, 花芳. LSD1促进肿瘤发生发展的机制和靶向治疗研究进展. 药学学报, 2026 , 61 (5) : 1435 -1449 . DOI: 10.16438/j.0513-4870.2026-0002
Shu-yuan DAI, Lang CHEN, Xiao-xi LÜ, Shuang SHANG, Fang HUA. Advances in the study of tumorigenesis and progression mechanism of LSD1 and its targeting strategies[J]. Acta Pharmaceutica Sinica, 2026 , 61 (5) : 1435 -1449 . DOI: 10.16438/j.0513-4870.2026-0002
Year 2026 volume 61 Issue 5
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Article Info
doi: 10.16438/j.0513-4870.2026-0002
  • Receive Date:2025-12-31
  • Online Date:2026-09-21
  • Published:2026-05-12
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  • Received:2025-12-31
  • Revised:2026-02-09
Affiliations
    State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, State Key Laboratory of Digestive Health, CAMS Key Laboratory of Molecular Mechanism and Target Discovery of Metabolic Disorder and Tumorigenesis, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
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表12种不同金属材料的力学参数
科
Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)
属
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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