小分子Janus激酶抑制剂的研究进展  

Research progress of small-molecule Janus kinase inhibitors

作　　者：李梦丽 卢诚 万慧阳 王玉斌[1] LI Meng-li;LU Cheng;WAN Hui-yang;WANG Yu-bin(School of Pharmacy,Nanjing University of Technology,Nanjing 210009,China)

机构地区：[1]南京工业大学药学院,南京210009

出　　处：《中国新药杂志》2021年第23期2178-2188,共11页Chinese Journal of New Drugs

摘　　要：Janus激酶(JAKs)是一类非受体型酪氨酸激酶,在过去近20年里,小分子Janus激酶抑制剂逐渐进入大众视野并受到研究者广泛的重视。JAKs可通过其与下游的信号传导及转录激活因子形成的JAK-STAT信号通路调节细胞增殖、分化、凋亡以及血管生成和免疫,其抑制剂可用于自身免疫性疾病、炎症反应以及恶性肿瘤等的防治。目前已经有近10种小分子Janus激酶抑制剂获得上市资格,还有一些抑制剂正处于临床研究阶段。本文就Janus激酶的结构、JAK-STAT信号通路以及近年来在研及已上市的JAKs抑制剂的研发进展及临床应用进行综述,旨在为该类抑制剂的研发提供有益的参考。Janus kinases(JAKs) are a class of non-receptor tyrosine kinases. In the past two decades, small-molecule Janus kinases inhibitors have gradually entered the public vision and received extensive attention from researchers. JAKs can regulate cell proliferation, differentiation, apoptosis, angiogenesis and immunity through JAK-STAT signal pathway formed by Janus kinases and their downstream signal transducers and activators of transcription. The inhibitors of JAKs can be used for prevention and treatment of autoimmune diseases, inflammatory reactions and malignant tumors. At present, nearly ten small-molecule Janus kinases inhibitors have been approved for marketing, and some others are in clinical research stage. This review summarizes the structure of Janus kinase, JAK-STAT signaling pathway, research and development progress and clinical application of JAKs inhibitors in recent years, providing useful reference for the further research and development of this class of inhibitors.

关 键 词：JANUS激酶 JAK-STAT通路 JAKs抑制剂 研究进展 

分 类 号：R967[医药卫生—药理学]