Recent advances in the development of STING inhibitors: an updated patent review

医学 专利分析 风险分析(工程) 重症监护医学 计算机科学 数据科学 工程类 航空航天工程
作者
Ancheng Shen,Mingjie Chen,Chen Qing-xuan,Zhiguo Liu,Ao Zhang
出处
期刊:Expert Opinion on Therapeutic Patents [Taylor & Francis]
卷期号:32 (11): 1131-1143 被引量:10
标识
DOI:10.1080/13543776.2022.2144220
摘要

STING is at the center of the cGAS-STING signaling and acts as the hub of the innate immune system. Hyper-activation of STING has been observed in various severe autoimmune diseases, such as AGS, SLE, and many other diseases including neurological and metabolic disorders. Therefore, STING has been considered as a promising target. In recent years, several STING inhibitors have been claimed in patents.Small-molecule STING inhibitors reported in patents (disclosed before May 2022 through the public database at https://worldwide.espacenet.com) were summarized in this review and the available structure-activity relationships (SARs) and molecular mechanisms of action were presented.Compared with STING agonists, the development of STING inhibitors is still in its infancy and no candidates have entered clinical investigation stage. Fortunately, patent applications are appearing at an increasing rate and a few of them have been validated in vivo, thus providing valuable insights for further structural optimization. More efforts are urgently needed since it is not clear yet that inhibitors targeting STING can solely exert sufficient therapeutic effects on autoimmune diseases, and the toxicity profile of such inhibitors is unknown as well. Therefore, it is extremely important to identify a selective and efficacious STING inhibitor for clinical evaluation to provide proof-of-concept for this approach.
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