JAK抑制剂研究进展  

Research Progress of JAK Inhibitors

作　　者：闫森 杨兆祥 刘军锋 YAN Sen;YANG Zhao-xiang;LIU Jun-feng(School of Pharmacy,Kunming Medical University,Kunming 650100,China;Institute of Pharmaceutical Research of Kunming Pharmaceutical Group Co.,Ltd.,Kunming 650100,China)

机构地区：[1]昆明医科大学药学院,云南昆明650100 [2]昆药集团股份有限公司药物研究院,云南昆明650100

出　　处：《海峡药学》2022年第3期1-5,共5页Strait Pharmaceutical Journal

摘　　要：目的本文通过阐述JAK-STAT通路与疾病的关系,对JAK抑制剂的未来发展进行展望。方法通过对近年来在JAK抑制剂治疗类风湿性关节炎(RA)、骨髓增殖性肿瘤(Myelopro1iferative neoplasms,MPNs)、斑秃(AA)、特应性皮炎(AD)、溃疡性结肠炎等和研发与上市状况的阐述,以期为JAK抑制剂的发展提供参考。结果研究发现JAKs存在于哺乳动物体内,有4种不同的亚型:JAK1、JAK2、JAK3(存在于细胞质)、酪氨酸激酶2(TYK2);STAT存在于哺乳动物细胞中,有7种亚型:即STAT1、STAT2、STAT3、STAT4、STAT5a、STAT5b、STAT6;JAK-STAT通路中的功能蛋白的失调可导致多种疾病。结论JAK抑制剂的研究大多处于药理学研究阶段,没有好的药物剂型;如果JAK抑制剂研究未来能在新剂型方面有所突破,将为人类健康做出更大的贡献。OBJECTIVE This article describes the relationship between the JAK-STAT pathway and disease,and prospects the future development of JAK inhibitors.METHODS In recent years,JAK inhibitors have been used to treat rheumatoid arthritis(RA),myeloproliferative neoplasms(MPNs),alopecia areat(AA),atopic dermatitis(AD),ulcerative colitis,etc.The elaboration of the status of R&Dand marketing is expected to provide a reference for the development of JAK inhibitors.RESULTS Studies have found that JAKs exist in mammals,and there are 4 different subtypes:JAK1,JAK2,JAK3(existing in the cytoplasm),and tyrosine kinase 2(TYK2);STAT exists in mammalian cells,and there are 7 types Subtypes:namely STAT1,STAT2,STAT3,STAT4,STAT5 a,STAT5 b,STAT6;the imbalance of functional proteins in the JAK-STAT pathway can lead to a variety of diseases.CONCLUSION JAK inhibitors are mostly in the pharmacological research stage,not good Pharmaceutical formulations;if JAK inhibitor research can make breakthroughs in new formulations in the future,it will make greater contributions to human health.

关 键 词：Janus通路 JAK抑制剂 自身免疫性疾病 专利 药物新剂型 

分 类 号：R965[医药卫生—药理学]