托法替尼
Janus激酶3
贾纳斯激酶
化学
免疫系统
类风湿性关节炎
免疫抑制
药理学
信号转导
免疫学
生物化学
医学
白细胞介素12
体外
细胞毒性T细胞
作者
Gebhard Thoma,Peter Drückes,Hans‐Günter Zerwes
标识
DOI:10.1016/j.bmcl.2014.08.046
摘要
Jak3, together with Jak1, is involved in signal transduction initiated by cytokines signaling through the common gamma chain which are important in immune homeostasis and immune pathologies. Based on genetic evidence Jak3 has been considered to be an attractive target for immunosuppression. The Jak inhibitor tofacitinib (CP-690,550) which is an approved drug for rheumatoid arthritis was originally introduced as a selective Jak3 inhibitor, however, it also inhibits Jak1 and Jak2. The search for new selective Jak3 inhibitors has yielded several compounds whose profiles will be reviewed here. Implications on Jak3 as a therapeutic target are also discussed.
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