鲁索利替尼
贾纳斯激酶
托法替尼
酪氨酸激酶2
激酶
JAK-STAT信号通路
酪氨酸激酶
医学
药理学
癌症研究
生物
受体
免疫学
内科学
骨髓纤维化
生物化学
类风湿性关节炎
生长因子
骨髓
血小板源性生长因子受体
作者
Ahmed M. Shawky,Faisal A. Almalki,Ashraf N. Abdalla,Ahmed H. Abdelazeem,Ahmed M. Gouda
出处
期刊:Pharmaceutics
[MDPI AG]
日期:2022-05-06
卷期号:14 (5): 1001-1001
被引量:71
标识
DOI:10.3390/pharmaceutics14051001
摘要
Janus kinase (JAK) is a family of cytoplasmic non-receptor tyrosine kinases that includes four members, namely JAK1, JAK2, JAK3, and TYK2. The JAKs transduce cytokine signaling through the JAK-STAT pathway, which regulates the transcription of several genes involved in inflammatory, immune, and cancer conditions. Targeting the JAK family kinases with small-molecule inhibitors has proved to be effective in the treatment of different types of diseases. In the current review, eleven of the JAK inhibitors that received approval for clinical use have been discussed. These drugs are abrocitinib, baricitinib, delgocitinib, fedratinib, filgotinib, oclacitinib, pacritinib, peficitinib, ruxolitinib, tofacitinib, and upadacitinib. The aim of the current review was to provide an integrated overview of the chemical and pharmacological data of the globally approved JAK inhibitors. The synthetic routes of the eleven drugs were described. In addition, their inhibitory activities against different kinases and their pharmacological uses have also been explained. Moreover, their crystal structures with different kinases were summarized, with a primary focus on their binding modes and interactions. The proposed metabolic pathways and metabolites of these drugs were also illustrated. To sum up, the data in the current review could help in the design of new JAK inhibitors with potential therapeutic benefits in inflammatory and autoimmune diseases.
科研通智能强力驱动
Strongly Powered by AbleSci AI