Interrupting cyclic dinucleotide-cGAS-STING axis with small molecules.,RSC Medicinal Chemistry

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Interrupting cyclic dinucleotide-cGAS-STING axis with small molecules.
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2019-08-15 , DOI: 10.1039/c8md00555a
Herman O Sintim _{1,

2,

3} , Clinton G Mikek ₁ , Modi Wang ₁ , Moloud A Sooreshjani ₁

Affiliation

The cyclic dinucleotide-cGAS-STING axis plays important roles in host immunity. Activation of this signaling pathway, via cytosolic sensing of bacterial-derived c-di-GMP/c-di-AMP or host-derived cGAMP, leads to the production of inflammatory interferons and cytokines that help resolve infection. Small molecule activators of the cGAS-STING axis have the potential to augment immune response against various pathogens or cancer. The aberrant activation of this pathway, due to gain-of-function mutations in any of the proteins that are part of the signaling axis, could lead to various autoimmune diseases. Inhibiting various nodes of the cGAS-STING axis could provide relief to patients with autoimmune diseases. Many excellent reviews on the cGAS-STING axis have been published recently, and these have mainly focused on the molecular details of the cGAS-STING pathway. This review however focuses on small molecules that can be used to modulate various aspects of the cGAS-STING pathway, as well as other parallel inflammatory pathways.

中文翻译：

用小分子中断环状二核苷酸-cGAS-STING 轴。

环状二核苷酸-cGAS-STING轴在宿主免疫中发挥重要作用。通过细菌来源的 c-di-GMP/c-di-AMP 或宿主来源的 cGAMP 的胞质传感，该信号通路的激活导致炎症干扰素和细胞因子的产生，从而帮助解决感染。 cGAS-STING 轴的小分子激活剂有可能增强针对各种病原体或癌症的免疫反应。由于作为信号轴一部分的任何蛋白质的功能获得性突变，该通路的异常激活可能导致各种自身免疫性疾病。抑制 cGAS-STING 轴的各个节点可以缓解自身免疫性疾病患者的症状。最近发表了许多关于 cGAS-STING 轴的优秀评论，这些评论主要集中在 cGAS-STING 通路的分子细节上。然而，本综述重点关注可用于调节 cGAS-STING 通路以及其他平行炎症通路各个方面的小分子。

更新日期：2019-12-13

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