Journal of East China Normal University(Natural Sc ›› 2018, Vol. 2018 ›› Issue (3): 196-211.doi: 10.3969/j.issn.1000-5641.2018.03.021

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Progress in development of small molecule inhibitors targeting indoleamine 2,3-dioxygenase

CHEN Rui, FANG Yan-fen, ZHANG Xiong-wen   

  1. School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, 200062, China
  • Received:2017-07-06 Online:2018-05-25 Published:2018-05-29

Abstract: In the development of cancer, cancer cells can employ a number of mechanisms to escape detection by the immune system. Indoleamine 2, 3-dioxygenase (IDO) is a type of enzyme in immune cells, which catalyzes the metabolism of tryptophan through the kynurenine pathway. Inflammation induced by cancer development can result in overexpression of IDO in protuberance cells and tumor cells in the tumor microenvironment,causing sustained consumption of tryptophan, inhibition of tryptophan-sensitive T cells functional activity, and a decrease in local immune activity in tumor tissues. Inhibition of IDO activity and its expression could effectively activate the immune system to kill tumor cells. Therefore, IDO has become a new target in cancer immunotherapy. Currently, four IDO inhibitors, namely Epacadostat, Indoximod, GDC-0919 and BMS-986205, are in the clinical research stage as potential new anti-cancer molecule immunotherapy drugs. At the same time, new IDO inhibitors such as PF-06840003 and RG70099 are also being investigated. In this article, the pogress of research on IDO and the development of IDO inhibitors as a new anti-cancer drug for tumor immunotherapy is reviewed.

Key words: indoleamine 2,3-dioxygenase, IDO inhibitors, immune system regulation, cancer treatment

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