靶向JAK治疗自身免疫病的小分子药物研究进展  

Research progress of small-molecule drugs targeting JAK in autoimmune diseases

作　　者：唐晓楠 张海婧[1] 王文杰[1] 吴练秋[1] TANG Xiao-nan;ZHANG Hai-jing;WANG Wen-jie;WU Lian-qiu(Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China)

机构地区：[1]中国医学科学院北京协和医学院药物研究所,北京100050

出　　处：《药学学报》2018年第10期1591-1597,共7页Acta Pharmaceutica Sinica

基　　金：北京市自然科学基金面上项目(7172139);中国医学科学院医学与健康科技创新工程项目(2016-12M-3-011)

摘　　要：自身免疫病是指机体对自身抗原发生免疫反应导致自体组织损伤所引起的一系列疾病,通常包括类风湿关节炎(RA)、系统性红斑狼疮(SLE)和银屑病等。JAKs(Januskinases)为一类非受体型酪氨酸激酶,是调控许多炎性细胞因子合成及释放所必需的信号转导介质,而这些炎性因子与自身免疫病的发生和发展密切相关。研究表明靶向JAK小分子抑制剂可通过调节炎性因子的信号转导通路而发挥其抗炎和免疫调节的药理学活性。本文对近年来在研及上市靶向JAK治疗自身免疫病的小分子药物进行梳理和归纳,旨在为该类药物的进一步研发提供参考。Autoimmune disease refers to a series of diseases caused by the body＇s immune response to autoantigens leading to autologous tissue damage. The examples include rheumatoid arthritis（RA）, systemic lupus erythematosus（SLE） and psoriasis, etc. Janus kinases（JAKs） are a class of non-receptor tyrosine kinases that are essential signaling mediators in the signal transduction and expression of the inflammatory cytokines, which are closely related to the occurrence and development of the autoimmune diseases. Studies have shown that the inhibitors targeting JAK can exert anti-inflammatory and immuno-modulatory pharmacological activities by modulation of the cell signaling pathways related to the inflammatory cytokines. In this paper, the literature about small-molecule drugs targeting JAK on autoimmune diseases in recent years are summarized to provide valuable information for the research and development of drugs.

关 键 词：JAK JAK/STAT 小分子药物 自身免疫病 

分 类 号：R967[医药卫生—药理学]