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Identification of an IDO1 inhibitor prodrug that specifically targets tumor tissue
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Hao FENG1, Qian-qian DU2, Zhi-qiang FENG2, *, Yan LI2, Zhong-cheng LIU1, Xiao-ling XU3
Acta Pharmaceutica Sinica | 2020, 55(5) : 958 - 966
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Acta Pharmaceutica Sinica | 2020, 55(5): 958-966
• Original Articles •
Identification of an IDO1 inhibitor prodrug that specifically targets tumor tissue
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Hao FENG1, Qian-qian DU2, Zhi-qiang FENG2, *, Yan LI2, Zhong-cheng LIU1, Xiao-ling XU3
Affiliations
  • 1. College of Pharmacy, Hebei University, Baoding 071002, China
  • 2. Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
  • 3. Heze Municipal Hospital, Heze 274000, China
Published: 2020-05-12 doi: 10.16438/j.0513-4870.2020-0016
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Hypoxia-activated prodrugs that specifically target tumor tissues were designed by attaching the nitro-aromatic ring carrier molecules that can be degraded in the hypoxic microenvironment of the tumor to the hydroxyamidine group of IDO1 inhibitor compound B and epacadostat. Eleven prodrug compounds were synthesized and their structures were confirmed by 1H NMR and HR-MS. Compounds F-1 and F-6, which had a higher stability and drug release rate, were identified by an in vitro stability assay, nitroreductase reduction assay, MTT assay, and an in vivo tumor tissue hypoxia degradation assay, and then evaluated for anti-tumor efficacy in vivo. The results showed that prodrug F-1 inhibited tumor growth by 67.41%, which was significantly higher than 42.31% for the starting drug group. It appeared that the inhibition of IDO1 in the tumor tissue was different from the overall inhibition of IDO1 in vivo. Animal treatment procedures were carried out with the approval of the Animal Care and Use Committee of the Chinese Academy of Medical Sciences and Peking Union Medical College.

immunotherapy  /  IDO inhibitor  /  prodrug  /  hypoxia
Hao FENG, Qian-qian DU, Zhi-qiang FENG, Yan LI, Zhong-cheng LIU, Xiao-ling XU. Identification of an IDO1 inhibitor prodrug that specifically targets tumor tissue[J]. Acta Pharmaceutica Sinica, 2020 , 55 (5) : 958 -966 . DOI: 10.16438/j.0513-4870.2020-0016
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Article Info
doi: 10.16438/j.0513-4870.2020-0016
  • Receive Date：2020-01-07
  • Online Date：2026-01-21
  • Published：2020-05-12
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  • Received：2020-01-07
  • Revised：2020-02-10
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Affiliations
    1. College of Pharmacy, Hebei University, Baoding 071002, China
    2. Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    3. Heze Municipal Hospital, Heze 274000, 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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