Discovery of IDO1 Inhibitors: From Bench to Bedside.
Discovery of IDO1 Inhibitors: From Bench to Bedside.
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DOI：
10.1158/0008-5472.can-17-2285
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发表时间：
2017-12-15
期刊：
影响因子：
11.2
通讯作者：
Muller AJ
中科院分区：
文献类型：
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作者：
Prendergast GC;Malachowski WP;DuHadaway JB;Muller AJ
吲哚胺2，3-双加氧酶-1(IDO1)的小分子抑制剂正在成为肿瘤实验药物的先锋。在这里，这一新药类别的先驱们提供了关于IDO1作为癌症治疗靶点的临床前验证以及一系列机械上不同的化合物-吲哚昔洛特、爱卡托司坦和Navoximod的发现和开发的床边回顾，这些化合物最初是作为IDO抑制剂在临床试验中进行评估的。作为拓宽治疗窗口的免疫代谢佐剂，IDO抑制剂不仅可以利用免疫肿瘤学方法，还可以利用化疗和放射治疗作为肿瘤临床治疗的标准。
Small molecule inhibitors of indoleamine 2,3-dioxygenase-1 (IDO1) are emerging at the vanguard of experimental agents in oncology. Here pioneers of this new drug class provide a bench-to-bedside review on preclinical validation of IDO1 as a cancer therapeutic target and on the discovery and development of a set of mechanistically distinct compounds – indoximod, epacadostat and navoximod – that were first to be evaluated as IDO inhibitors in clinical trials. As ‘immunometabolic adjuvants’ to widen therapeutic windows, IDO inhibitors may leverage not only immuno-oncology modalities but also chemotherapy and radiotherapy as standards of care in the oncology clinic.