TYK2抑制剂的研究进展
Research Progress in TYK2 Inhibitors
施欣雨 1李志裕 1毕小玲1
作者信息
- 1. 中国药科大学,江苏 南京 210009
- 折叠
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.
关键词
酪氨酸激酶2/激酶结构域/假激酶结构域/抑制剂/降解剂Key words
Tyrosine kinase 2/kinase domain/pseudokinase domain/inhibitors/degradation agent引用本文复制引用
出版年
2024
NETL
NSTL
万方数据