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Research progress of anticancer drugs targeting inosine-5′-monophosphate dehydrogenase
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Xiao-qian LIU1, 2, Zi-yao HUANG2, Ya-xi YANG3, Chao CHEN2, 3, *, Bing ZHOU1, 2, 3, *
Acta Pharmaceutica Sinica | 2026, 61(9) : 3343 - 3354
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Acta Pharmaceutica Sinica | 2026, 61(9): 3343-3354
• Reviews •
Research progress of anticancer drugs targeting inosine-5′-monophosphate dehydrogenase
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Xiao-qian LIU1, 2, Zi-yao HUANG2, Ya-xi YANG3, Chao CHEN2, 3, *, Bing ZHOU1, 2, 3, *
Affiliations
  • 1School of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250117, China
  • 2Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai 264117, China
  • 3State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
Published: 2026-09-12 doi: 10.16438/j.0513-4870.2025-1597
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Maintaining intracellular purine nucleotide homeostasis is critical for sustaining normal cellular physiology. Inosine-5′-monophosphate dehydrogenase (IMPDH) acts as the rate-limiting enzyme in the de novo purine nucleotide biosynthesis (DNPNB) pathway, directly regulating intracellular guanine nucleotide synthesis levels. In rapidly proliferating tumor cells, IMPDH is aberrantly activated to meet heightened nucleic acid demands, rendering it a promising target for cancer therapy. Despite the advancement of several candidates — including tiazofurin — into clinical trials, no IMPDH-targeted antitumor drugs have been approved for marketing, highlighting the need for more rigorous and systematic investigation in this field. This review summarizes the structural and functional properties of IMPDH and the progress in developing IMPDH-targeting anticancer drugs, with the aim of providing insights for future research.

nucleotide metabolism  /  de novo synthesis pathway  /  inosine-5′-monophosphate  /  inhibitor  /  cancer therapy
刘晓倩, 黄紫瑶, 杨亚玺, 陈超, 周兵. 靶向肌苷5′-单磷酸脱氢酶的抗肿瘤药物研究进展. 药学学报, 2026 , 61 (9) : 3343 -3354 . DOI: 10.16438/j.0513-4870.2025-1597
Xiao-qian LIU, Zi-yao HUANG, Ya-xi YANG, Chao CHEN, Bing ZHOU. Research progress of anticancer drugs targeting inosine-5′-monophosphate dehydrogenase[J]. Acta Pharmaceutica Sinica, 2026 , 61 (9) : 3343 -3354 . DOI: 10.16438/j.0513-4870.2025-1597
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Year 2026 volume 61 Issue 9
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doi: 10.16438/j.0513-4870.2025-1597
  • Receive Date：2026-01-20
  • Online Date：2026-10-22
  • Published：2026-09-12
Article Data
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History
  • Received：2026-01-20
  • Revised：2026-03-20
Affiliations
    1School of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250117, China
    2Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai 264117, China
    3State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, 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
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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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