Targeting Stimulator of Interferon Genes (STING): A Medicinal Chemistry Perspective.,Journal of Medicinal Chemistry

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Targeting Stimulator of Interferon Genes (STING): A Medicinal Chemistry Perspective.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2019-12-20 , DOI: 10.1021/acs.jmedchem.9b01039
Han Zhang _{1,

2} , Qi-Dong You _{1,

2} , Xiao-Li Xu _{1,

2}

Affiliation

Stimulator of interferon genes (STING) is an adaptor protein that induces the secretion of type I interferons and proinflammatory cytokines and is triggered by cytosolic DNA of pathogen and host origins. Given that STING is a mediator in the immune system, pharmacological modulation of STING has shown viable therapeutic effects for pathogen infection, cancer, and inflammatory diseases. In the past decade, the substantial development in this field has encouraged the discovery of STING modulators. Here, we will summarize the current understanding of STING structure, survey the status quo of STING modulators, compare established bioassay methods, review the chemical structures and bioactivities of agonists and inhibitors, and propose suggestions and insights for the future exploitation of STING modulators.

中文翻译：

靶向干扰素基因刺激物（STING）：药物化学的观点。

干扰素基因刺激物（STING）是一种衔接蛋白，可诱导I型干扰素和促炎细胞因子的分泌，并由病原体和宿主来源的胞质DNA触发。鉴于STING是免疫系统的介质，STING的药理学调节已显示出对病原体感染，癌症和炎症性疾病的可行治疗作用。在过去的十年中，该领域的重大发展鼓励了STING调制器的发现。在这里，我们将总结当前对STING调节剂的了解，调查STING调节剂的现状，比较已建立的生物测定方法，回顾激动剂和抑制剂的化学结构和生物活性，并对STING调节剂的未来开发提出建议和见解。

更新日期：2019-12-10

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