本文選題：酪氨酸蛋白激酶　切入點(diǎn)：JAK-　出處：《藥學(xué)學(xué)報(bào)》2016年10期

【摘要】：JAK-3激酶(Janus kinase 3)作為酪氨酸蛋白激酶家族成員,在JAK-STAT(Janus kinase-signal transducer and activator of transcription)信號(hào)通路中起著非常重要的作用,研究證實(shí)JAK-3活性的調(diào)控在多種疾病的治療中起著關(guān)鍵作用,針對(duì)該激酶的抑制劑已經(jīng)有許多相關(guān)研究,并有多個(gè)JAK-3激酶抑制劑進(jìn)入臨床研究,表現(xiàn)出很好的JAK-3選擇性和抑制活性,其中tofacitinib等抑制劑已經(jīng)通過臨床試驗(yàn),被批準(zhǔn)用于類風(fēng)濕性關(guān)節(jié)炎的治療。很多JAK-3抑制劑表現(xiàn)出良好抑制活性的同時(shí),伴有一定的不良反應(yīng),有待于改進(jìn)。本文綜述了JAK-3激酶的結(jié)構(gòu)功能以及JAK-3激酶抑制劑的研究進(jìn)展,為后續(xù)研究提供參考。
[Abstract]:JAK-3 kinase Janus kinase 3, as a member of tyrosine protein kinase family, plays a very important role in the JAK-STAT(Janus kinase-signal transducer and activator of transcription.Study shows that the regulation of JAK-3 activity plays a key role in the treatment of many diseases. There have been many related studies on the inhibitors of this kinase, and many JAK-3 kinase inhibitors have entered clinical studies, showing good JAK-3 selectivity and inhibitory activity. Among them, tofacitinib and other inhibitors have passed the clinical trials. Approved for the treatment of rheumatoid arthritis. Many JAK-3 inhibitors exhibit good inhibitory activity with some adverse reactions. The structure and function of JAK-3 kinase and the research progress of JAK-3 kinase inhibitor are reviewed in this paper.
【作者單位】： 中國藥科大學(xué)藥物科學(xué)研究院;中國醫(yī)學(xué)科學(xué)院北京協(xié)和醫(yī)學(xué)院藥物研究所;
【基金】：國家自然科學(xué)基金資助項(xiàng)目(81573445;81172934)
【分類號(hào)】：R96
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本文編號(hào)：1689125