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TYK2抑制剂的研究进展
Research Progress in TYK2 Inhibitors
【摘要】 TYK2(酪氨酸激酶2)作为Janus激酶家族的一员,在IL-12、IL-23和I型IFN等细胞因子的调控中扮演着重要的角色。鉴于JAK抑制剂选择性不高而产生不良反应等问题,靶向TYK2蛋白抑制剂的研发正逐步受到科研工作者的重视。本文从TYK2蛋白的结构特征出发,先后介绍了靶向TYK2激酶结构域(JH1)的底物竞争性抑制剂和靶向假激酶结构域(JH2)的变构抑制剂以及TYK2降解剂,为以后TYK2抑制剂的研究提供新的参考。
【Abstract】 TYK2(tyrosine kinase 2), as a member of the Janus kinase family, plays an important role in the regulation of cytokines such as IL-12, IL-23, and type I IFN. Due to the low selectivity and adverse reactions of JAK inhibitors, the development of targeted TYK2 protein inhibitors is gradually receiving attention from researchers. Starting from the structural characteristics of TYK2 protein, this article introduces substrate competitive inhibitors targeting the TYK2 kinase domain(JH1), conformational inhibitors targeting the pseudokinase domain(JH2), and TYK2 degradation agents, providing new references for future research on TYK2 inhibitors.
【Key words】 Tyrosine kinase 2; kinase domain; pseudokinase domain; inhibitors; degradation agent;
- 【文献出处】 广东化工 ,Guangdong Chemical Industry , 编辑部邮箱 ,2024年10期
- 【分类号】R979.5
- 【下载频次】35