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吲哚胺2,3-双加氧酶1抑制剂的研究进展

程雨兰, 门金霞, 周金培, 张惠斌

程雨兰, 门金霞, 周金培, 张惠斌. 吲哚胺2,3-双加氧酶1抑制剂的研究进展[J]. 中国药科大学学报, 2017, 48(3): 361-370. DOI: 10.11665/j.issn.1000-5048.20170318
引用本文: 程雨兰, 门金霞, 周金培, 张惠斌. 吲哚胺2,3-双加氧酶1抑制剂的研究进展[J]. 中国药科大学学报, 2017, 48(3): 361-370. DOI: 10.11665/j.issn.1000-5048.20170318
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CHENG Yulan, MEN Jinxia, ZHOU Jinpei, ZHANG Huibin. Advances in indoleamine 2, 3-dioxygenase 1 inhibitors[J]. Journal of China Pharmaceutical University, 2017, 48(3): 361-370. DOI: 10.11665/j.issn.1000-5048.20170318
Citation: CHENG Yulan, MEN Jinxia, ZHOU Jinpei, ZHANG Huibin. Advances in indoleamine 2, 3-dioxygenase 1 inhibitors[J]. Journal of China Pharmaceutical University, 2017, 48(3): 361-370. DOI: 10.11665/j.issn.1000-5048.20170318
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吲哚胺2,3-双加氧酶1抑制剂的研究进展

  • 中国药科大学药物化学教研室

Advances in indoleamine 2, 3-dioxygenase 1 inhibitors

摘要

    摘要
  • 摘要: 吲哚胺2，3-双加氧酶1(indoleamine 2，3-dioxygenase 1，IDO1)是介导色氨酸沿犬尿氨酸途径分解代谢的限速酶。IDO1在肿瘤细胞和抗原呈递细胞(antigen presenting cells，APC)中存在过度表达现象，通过色氨酸的消耗及其代谢产物的聚积抑制局部免疫应答，使肿瘤细胞逃避免疫系统的监测，这与多数肿瘤治疗的不良预后有关。因此，IDO1是肿瘤免疫疗法的重要靶点。目前有多种骨架的IDO1抑制剂正在研究当中，其中3个已经进入了临床研究阶段。本文介绍了IDO1在肿瘤免疫耐受中的作用，并按结构分类，综述了IDO1抑制剂的研究进展。
    Abstract: Indoleamine 2, 3-dioxygenase 1(IDO1)is the rate-limiting enzyme which catalyses the metabolism of L-tryptophan(L-Trp)in the kynurenine pathway. It is overexpressed in many tumor cells and antigen presenting cells. This enzyme inhibits local immune response and supports tumor cells to evade immune surveillance by depleting L-Trp and producing kynurenine metabolites, thus, it is an important target for cancer immunotherapy. There are several IDO1 inhibitors with different scarfold under investigation, three of which have already entered clinical stage. The role of IDO1 in tumor immune tolerance and the research progress on IDO1 inhibitors in recent years are summarized in this paper.
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  • 刊出日期:  2017-06-24

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