The First Clinical College, Guangdong Medical University, Zhanjiang 524023, China.
Animal Experiment Center of Guangdong Medical University, Zhanjiang, 524023, China.
Biomed Pharmacother. 2020 Dec;132:110945. doi: 10.1016/j.biopha.2020.110945. Epub 2020 Nov 1.
Cyclic guanosine monophosphate-adenosine monophosphate synthase (cGAS) -stimulator of interferon genes (STING) signaling pathway is the primary immune response pathway in the cytoplasm. Pharmacological regulation of the STING pathway has good characteristics in both structure and function, which plays a significant role in the immunotherapy of autoimmune diseases, autoinflammatory diseases, and cancer. In this review, we summarized the activation of STING signaling pathway, the STING-related diseases, the development principle and the latest progress of inhibitors and agonists targeting STING. Our review demonstrates that STING signal pathway is a promising drug target, providing effective clues and correct guidance for the discovery of novel small molecule inhibitors/agonists that targeted STING for cancer, autoimmune, and inflammatory diseases.
环鸟苷酸-腺苷酸合成酶(cGAS)-干扰素基因刺激物(STING)信号通路是细胞质中的主要免疫反应途径。STING 通路的药理学调节在结构和功能上都具有良好的特征,在自身免疫性疾病、自身炎症性疾病和癌症的免疫治疗中发挥着重要作用。在这篇综述中,我们总结了 STING 信号通路的激活、STING 相关疾病、抑制剂和激动剂的开发原理及最新进展。我们的综述表明,STING 信号通路是一个很有前途的药物靶点,为发现针对癌症、自身免疫和炎症性疾病的新型 STING 靶向小分子抑制剂/激动剂提供了有效的线索和正确的指导。