Discovery and Development of Janus Kinase (JAK) Inhibitors for Inflammatory Diseases
Discovery and Development of Janus Kinase (JAK) Inhibitors for Inflammatory Diseases
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DOI：
10.1021/jm401490p
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发表时间：
2014-06-26
影响因子：
7.3
通讯作者：
Telliez, Jean-Baptiste
中科院分区：
文献类型：
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作者：
Clark, James D.;Flanagan, Mark E.;Telliez, Jean-Baptiste
Janus激酶（JAK）是细胞内酪氨酸激酶家族，在多种细胞因子的信号传导中发挥重要作用，这些细胞因子与炎症性疾病的发病机制有关。因此，JAK近年来作为治疗靶标受到制药和生物技术行业的极大关注。在这里，我们提供了JAK途径，JAK酶的结构，功能和激活的综述，然后详细介绍了目前临床上或批准用于这些适应症的JAK抑制剂。最后，提供了一个观点，在过去十年的研究与JAK抑制剂的炎症适应症已经教沿着的想法，未来可能会举行的方面，解决的机会和挑战仍然存在。
The Janus kinases (JAKs) are a family of intracellular tyrosine kinases that play an essential role in the signaling of numerous cytokines that have been implicated in the pathogenesis of inflammatory diseases. As a consequence, the JAKs have received significant attention in recent years from the pharmaceutical and biotechnology industries as therapeutic targets. Here, we provide a review of the JAK pathways, the structure, function, and activation of the JAK enzymes followed by a detailed look at the JAK inhibitors currently in the clinic or approved for these indications. Finally, a perspective is provided on what the past decade of research with JAK inhibitors for inflammatory indications has taught along with thoughts on what the future may hold in terms of addressing the opportunities and challenges that remain.