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New 4‐Amino‐1,2,3‐Triazole Inhibitors of Indoleamine 2,3‐Dioxygenase Form a Long‐Lived Complex with the Enzyme and Display Exquisite Cellular Potency
ChemBioChem ( IF 2.6 ) Pub Date : 2018-01-31 , DOI: 10.1002/cbic.201700560
Julie Anne Christine Alexandre 1 , Michael Kenneth Swan 1 , Mike John Latchem 1 , Dean Boyall 1 , John Robert Pollard 1 , Stuart Wynn Hughes 1 , James Westcott 1
Affiliation  

Pocket sized: Indoleamine 2,3‐dioxygenase 1 (IDO1) is an immunosuppressive enzyme employed by cancers to evade the immune system response, and as such is an exciting target for drug discovery. Kinetic, biochemical and structural studies reveal the surprising mechanisms by which a series of IDO1 inhibitors attain potency in cells.
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中文翻译:

吲哚胺 2,3-双加氧酶的新型 4-氨基-1,2,3-三唑抑制剂与酶形成长寿复合物并显示出精致的细胞效力

袖珍型:吲哚胺 2,3-双加氧酶 1 (IDO1) 是一种被癌症用来逃避免疫系统反应的免疫抑制酶,因此是药物发现的一个令人兴奋的目标。动力学、生化和结构研究揭示了一系列 IDO1 抑制剂在细胞中发挥效力的惊人机制。
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更新日期:2018-01-31
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