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小分子 TBK1 抑制剂的最新进展:专利回顾(2015-2020)。

Recent progress in small molecule TBK1 inhibitors: a patent review (2015- 2020).

机构信息

Functional Genomics, Cellzome GmbH, GlaxoSmithKline, Heidelberg, Germany.

出版信息

Expert Opin Ther Pat. 2021 Sep;31(9):785-794. doi: 10.1080/13543776.2021.1904893. Epub 2021 Mar 31.

Abstract

: TANK-binding kinase 1 (TBK1) is a key mediator of innate immunity processes and studies have reported on its role in inflammatory and autoimmune diseases. Moreover, several studies have also described the important role of TBK1 in cancer and metabolic disorders. Therefore, there is increasing interest in this noncanonical IKK serine/threonine kinase family member as a drug target in both the scientific community and the pharmaceutical industry as indicated by the growing number of patents reporting on these efforts.: This review covers the patent literature from 2015 to 2020 issued by the World, US and European patent offices on novel TBK1 small molecule inhibitors as well as patents claiming new applications of TBK1 inhibitors.: The high complexity TBK1 biology greatly increases the challenge of pursuing it as a drug target. The recent discovery of several small molecule inhibitors, particularly those with high selectivity, will enable further exploration of TBK1s biological role and its validation as a drug target.

摘要

: TANK 结合激酶 1(TBK1)是先天免疫过程的关键介质,已有研究报道其在炎症和自身免疫性疾病中的作用。此外,一些研究还描述了 TBK1 在癌症和代谢紊乱中的重要作用。因此,越来越多的人对这种非典型的 IKK 丝氨酸/苏氨酸激酶家族成员感兴趣,将其作为药物靶点,这一点在科学界和制药行业都有体现,越来越多的专利报告了这方面的努力。: 本文综述了 2015 年至 2020 年世界、美国和欧洲专利局公布的新型 TBK1 小分子抑制剂的专利文献,以及声称 TBK1 抑制剂新应用的专利。: TBK1 生物学的高度复杂性极大地增加了将其作为药物靶点的挑战。最近发现的几种小分子抑制剂,特别是那些具有高选择性的抑制剂,将能够进一步探索 TBK1 的生物学作用及其作为药物靶点的验证。

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