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Advances in research on USP7-mediated regulation of protein homeostasis and associated antitumor strategies
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Xing LI1, Shu-fen HE1, Jun-jie QIN1, Hui ZHOU1, Yi MOU1, Juan SONG1, Xin ZHANG1, Yong-jun ZANG2, *, Xiao-an WEN3, *
Acta Pharmaceutica Sinica | 2025, 60(11) : 3355 - 3370
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Acta Pharmaceutica Sinica | 2025, 60(11): 3355-3370
• Special Reports: Recent advances in targeted protein degradation therapeutics •
Advances in research on USP7-mediated regulation of protein homeostasis and associated antitumor strategies
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Xing LI1, Shu-fen HE1, Jun-jie QIN1, Hui ZHOU1, Yi MOU1, Juan SONG1, Xin ZHANG1, Yong-jun ZANG2, *, Xiao-an WEN3, *
Affiliations
  • 1School of Pharmacy, Taizhou University, Taizhou 225300, China
  • 2School of Biology and Pharmaceutical Engineering, West Anhui University, Lu′an 237012, China
  • 3State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China
Published: 2025-11-12 doi: 10.16438/j.0513-4870.2025-0899
Outline
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Proteostasis is a core biological process through which cells maintain the stability and functional integrity of the proteome via a multi-level quality control network. As a key molecule in the ubiquitination regulatory pathway, the deubiquitinase USP7 can drive tumorigenesis and progression by altering the ubiquitination status of substrate proteins when its expression is aberrant or activity is dysregulated, thus emerging as a critical target in precision cancer therapy. This article systematically outlines the structural features of USP7, its role in regulating substrate protein homeostasis, and its biological functions in tumor development. It focuses on recent advances in USP7-based anti-tumor strategies, including the development of small-molecule inhibitors, applications of proteolysis-targeting chimeras (PROTACs) technology, and exploration of novel approaches such as deubiquitinase-targeting chimeras (DUBTACs). This review provides a systematic theoretical framework and cutting-edge research directions for the development of USP7-targeted anti-tumor drugs.

protein homeostasis regulation  /  USP7  /  tumor therapy  /  inhibitor  /  proteolysis-targeting chimera  /  deubiquitinase-targeting chimera
李幸, 何姝芬, 覃俊杰, 周慧, 牟伊, 宋娟, 张鑫, 臧永军, 温小安. USP7的蛋白稳态调控作用及其抗肿瘤策略研究进展. 药学学报, 2025 , 60 (11) : 3355 -3370 . DOI: 10.16438/j.0513-4870.2025-0899
Xing LI, Shu-fen HE, Jun-jie QIN, Hui ZHOU, Yi MOU, Juan SONG, Xin ZHANG, Yong-jun ZANG, Xiao-an WEN. Advances in research on USP7-mediated regulation of protein homeostasis and associated antitumor strategies[J]. Acta Pharmaceutica Sinica, 2025 , 60 (11) : 3355 -3370 . DOI: 10.16438/j.0513-4870.2025-0899
Appendix
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Year 2025 volume 60 Issue 11
320
164
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Article Info
doi: 10.16438/j.0513-4870.2025-0899
  • Receive Date：2025-07-31
  • Online Date：2026-09-20
  • Published：2025-11-12
Article Data
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History
  • Received：2025-07-31
  • Revised：2025-09-10
Affiliations
    1School of Pharmacy, Taizhou University, Taizhou 225300, China
    2School of Biology and Pharmaceutical Engineering, West Anhui University, Lu′an 237012, China
    3State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China
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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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