华东师范大学学报（自然科学版）Issue(3)：196-211,16.DOI:10.3969/j.issn.1000-5641.2018.03.021
靶向吲哚胺2,3-双加氧酶(IDO)的肿瘤免疫治疗小分子抑制剂研发进展
Progress in development of small molecule inhibitors targeting indoleamine 2,3-dioxygenase
摘要
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.关键词
吲哚胺2,3-双加氧酶/IDO抑制剂/免疫调节/癌症治疗Key words
indoleamine 2, 3-dioxygenase/IDO inhibitors/immune system regulation/cancer treatment分类
农业科技引用本文复制引用
陈瑞,方艳芬,章雄文..靶向吲哚胺2,3-双加氧酶(IDO)的肿瘤免疫治疗小分子抑制剂研发进展[J].华东师范大学学报（自然科学版）,2018,(3):196-211,16.基金项目
上海市科委项目(14431902700,16DZ2280100),国家自然科学基金青年基金资助项目(81402953),中国博士后基金(2015T80416). （14431902700,16DZ2280100）
