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Advances in developing small molecule inhibitors of ubiquitin-specific protease 1
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Jia-hao XU1, 3, 4, Hong-rui LI2, 3, 4, Rui-xian BA2, 3, 4, Tong-chao LIU3, *, Bing XIONG3, 4, *
Acta Pharmaceutica Sinica | 2024, 59(4) : 866 - 885
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Acta Pharmaceutica Sinica | 2024, 59(4): 866-885
• Reviews •
Advances in developing small molecule inhibitors of ubiquitin-specific protease 1
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Jia-hao XU1, 3, 4, Hong-rui LI2, 3, 4, Rui-xian BA2, 3, 4, Tong-chao LIU3, *, Bing XIONG3, 4, *
Affiliations
  • 1. School of Pharmacy, Jiangxi University of Chinese Medicine, Nanchang 330004, China
  • 2. Shenyang Pharmaceutical University, Shenyang 110016, China
  • 3. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
  • 4. Yangtze Delta Drug Advanced Research Institute, Nantong 226133, China
Published: 2024-04-12 doi: 10.16438/j.0513-4870.2023-1076
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Ubiquitin-specific protease 1 (USP1) is one of the deubiquitinating enzymes which has received increasing attention in cancer research. USP1 is overexpressed in many types of cancer cells, and has been found to control tumorigenesis and progression by regulating various proteins associated with tumors, such as SIK2, GSK-3β, and Bcl-2. Knockdown or pharmacological inhibition of USP1 can effectively suppress tumors and is also expected to address the issues of cisplatin and poly ADP-ribose polymerase (PARP) inhibitor resistance. This review describes the structure and function of USP1 and the relationship between USP1 targets and tumors and systematically summarizes the structure-activity relationships of small molecule USP1 inhibitors disclosed from 2013 to 2023. Finally, this review discusses the challenges and opportunities in developing small molecule USP1 inhibitors.

ubiquitin-specific protease 1  /  small molecule inhibitor  /  synthetic lethality  /  drug resistance  /  structure-activity relationship
Jia-hao XU, Hong-rui LI, Rui-xian BA, Tong-chao LIU, Bing XIONG. Advances in developing small molecule inhibitors of ubiquitin-specific protease 1[J]. Acta Pharmaceutica Sinica, 2024 , 59 (4) : 866 -885 . DOI: 10.16438/j.0513-4870.2023-1076
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Article Info
doi: 10.16438/j.0513-4870.2023-1076
  • Receive Date：2023-09-16
  • Online Date：2025-11-28
  • Published：2024-04-12
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History
  • Received：2023-09-16
  • Revised：2024-01-04
Funding
Affiliations
    1. School of Pharmacy, Jiangxi University of Chinese Medicine, Nanchang 330004, China
    2. Shenyang Pharmaceutical University, Shenyang 110016, China
    3. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
    4. Yangtze Delta Drug Advanced Research Institute, Nantong 226133, China
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表12种不同金属材料的力学参数
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Family		 属数
Number of
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Number of
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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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