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Bioactive modulators targeting STING adaptor in cGAS-STING pathway.
Drug Discovery Today ( IF 6.5 ) Pub Date : 2019-11-20 , DOI: 10.1016/j.drudis.2019.11.007
Xi Feng 1 , Dongyu Liu 1 , Zhiyu Li 1 , Jinlei Bian 1
Affiliation  

The cyclic GMP-AMP synthase (cGAS)-stimulator of interferon genes (STING)-pathway triggers innate immune responses by recognizing cytosolic DNA. Recent studies revealed that STING adaptor associates with various diseases, and several modulators targeting STING have been identified including three agonists that have entered clinical trials for treating cancer over the past 2 years. In particular, the efficacy of STING agonists and/or antagonists suggests adaptor STING as a potential therapeutic target for diverse diseases. Herein, we summarize the latest advances in understanding STING functioning and provide an overview of recent STING modulator discoveries, including structural details and the potential therapeutic applications of these modulators.

中文翻译:

在cGAS-STING途径中靶向STING衔接子的生物活性调节剂。

干扰素基因的环GMP-AMP合酶(cGAS)刺激物(STING)途径通过识别胞质DNA触发先天免疫应答。最近的研究表明,STING衔接子与多种疾病有关,并且已经确定了几种靶向STING的调节剂,包括在过去2年中已进入治疗癌症的三项激动剂的临床试验。特别地,STING激动剂和/或拮抗剂的功效表明衔接子STING作为多种疾病的潜在治疗靶标。本文中,我们总结了了解STING功能的最新进展,并概述了STING调节剂的最新发现,包括这些调节剂的结构细节和潜在的治疗应用。
更新日期:2019-11-21
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