【摘要】：目的綜述c-ros原癌基因1(c-ros oncogene 1,ROS1)酪氨酸激酶的結(jié)構和功能及其抑制劑的研究進展。方法查閱近年來國內(nèi)外相關文獻47篇,對其進行歸納總結(jié)和分析。結(jié)果 ROS1作為一個關鍵的跨膜受體蛋白酪氨酸激酶,控制細胞凋亡、生存、分化及增殖等多個細胞進程,對多種惡性腫瘤的治療有重要作用,因此,開發(fā)ROS1抑制劑具有重要的價值。2015年4月,克唑替尼(crizotinib)被美國FDA授予突破性藥物資格,用于ROS1陽性非小細胞肺癌的潛在治療;隨后2-氨基嘧啶類、4-芳氨基喹啉類等化合物相繼被報道具有較強的ROS1激酶抑制活性,此外,一些選擇性ROS1抑制劑(如化合物12)也被開發(fā)出來。結(jié)論盡管目前對ROS1選擇性抑制劑研究較少,但ROS1抑制劑仍具有良好的開發(fā)前景。
[Abstract]:Objective to review the structure and function of c-ros proto-oncogene 1 (c-ros oncogene 1 rosl) tyrosine kinase and its inhibitors. Methods 47 literatures were reviewed, summarized and analyzed in recent years. Results as a key transmembrane receptor protein tyrosine kinase, ROS1 controls cell apoptosis, survival, differentiation and proliferation, and plays an important role in the treatment of various malignant tumors. The development of ROS1 inhibitors is of great value. In April 2015, (crizotinib) was awarded a breakthrough drug qualification by the United States FDA for the potential treatment of ROS1 positive non-small cell lung cancer (NSCLC). Subsequently, 2-aminopyrimidine, 4-arylaminoquinoline and other compounds have been reported to have strong ROS1 kinase inhibitory activity, in addition, some selective ROS1 inhibitors (such as compound 12) have also been developed. Conclusion although there are few studies on ROS1 selective inhibitors at present, ROS1 inhibitors still have a good prospect.
【作者單位】： 沈陽藥科大學基于靶點的藥物設計與研究教育部重點實驗室;
【基金】：國家自然科學基金資助項目(81673308)
【分類號】：R979.1
，

本文編號：2416199