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The research progress of indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitors
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Xin-yuan ZHANG, Guo-nan CUI, Bai-ling XU*
Acta Pharmaceutica Sinica | 2018, 53(11) : 1784 - 1796
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Acta Pharmaceutica Sinica | 2018, 53(11): 1784-1796
• REVIEWS •
The research progress of indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitors
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Xin-yuan ZHANG, Guo-nan CUI, Bai-ling XU*
Affiliations
  • Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2018-11-12 doi: 10.16438/j.0513-4870.2018-0673
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Indoleamine 2, 3-dioxygenase 1 (IDO1) is a key enzyme of L-tryptophan metabolic oxidation pathway, in which the L-tryptophan is transformed into N-formyl kynurenine by oxidative cleavage. IDO1 is considered as a potential target for the development of cancer immunotherapeutic molecules. Up to now, at least 10 drug candidates have been advanced into clinical research. In this review, the binding mode and structure-activity relationships of the representative IDO1 small molecule inhibitors were summarized according the characteristics of chemical structures. Hopefully, this review could provide some insights for further development of novel IDO1 inhibitors.

indoleamine 2, 3-dioxygenase 1  /  IDO1 inhibitors  /  structure-activity relationship  /  binding mode  /  tumor immunotherapy
Xin-yuan ZHANG, Guo-nan CUI, Bai-ling XU. The research progress of indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitors[J]. Acta Pharmaceutica Sinica, 2018 , 53 (11) : 1784 -1796 . DOI: 10.16438/j.0513-4870.2018-0673
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Article Info
doi: 10.16438/j.0513-4870.2018-0673
  • Receive Date：2018-07-24
  • Online Date：2026-01-15
  • Published：2018-11-12
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History
  • Received：2018-07-24
  • Revised：2018-09-21
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    Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and 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
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Genus		 种数
Number of
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Percentage of total
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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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