Research progress of JAK-3 kinase and its inhibitors
10.16438/j.0513-4870.2016-0087
- VernacularTitle:JAK-3激酶及其抑制剂的研究进展
- Author:
Yuan YIN
1
;
Tian-tai ZHANG
2
;
Da-yong ZHANG
1
Author Information
1. Institute of Pharmaceutical Science, China Pharmaceutical University, Nanjing 210009, China
2. Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
- Publication Type:REVIEWS
- Keywords:
tyrosine protein kinase;
JAK-3;
kinase inhibitor;
rheumatoid arthritis
- From:
Acta Pharmaceutica Sinica
2016;51(10):1520-
- CountryChina
- Language:Chinese
-
Abstract:
JAK-3, a member of the Janus kinase family, is a protein tyrosine kinase, which plays an important role in the JAK-STAT signaling pathway. Previous studies showed that regulation of JAK-3's activity plays a crucial role in the treatment of diseases such as rheumatoid arthritis. Many reports have been published with a focus on selective JAK-3 inhibitors, some of which showed excellent JAK-3 selectivity and inhibitory activities. Among the JAK-3 inhibitors reported, tofacitinib has satisfactory therapeutic benefits in the clinical trials, and has been approved for treatment of patients with rheumatoid arthritis. However, some JAK-3 inhibitors exhibited moderate to severe side effects, which need to be controlled by drug improvement. In order to pave the way for improvement of current JAK-3 inhibitors and development of new JAK-3 inhibitors, we provide an outline of the structure of JAK-3 and strategies in development of its inhibitors.
