靶向ROS1酪氨酸激酶小分子抑制剂的研究进展
发布时间：2019-01-27 11:02
【摘要】：目的综述c-ros原癌基因1(c-ros oncogene 1,ROS1)酪氨酸激酶的结构和功能及其抑制剂的研究进展。方法查阅近年来国内外相关文献47篇,对其进行归纳总结和分析。结果 ROS1作为一个关键的跨膜受体蛋白酪氨酸激酶,控制细胞凋亡、生存、分化及增殖等多个细胞进程,对多种恶性肿瘤的治疗有重要作用,因此,开发ROS1抑制剂具有重要的价值。2015年4月,克唑替尼(crizotinib)被美国FDA授予突破性药物资格,用于ROS1阳性非小细胞肺癌的潜在治疗;随后2-氨基嘧啶类、4-芳氨基喹啉类等化合物相继被报道具有较强的ROS1激酶抑制活性,此外,一些选择性ROS1抑制剂(如化合物12)也被开发出来。结论尽管目前对ROS1选择性抑制剂研究较少,但ROS1抑制剂仍具有良好的开发前景。
[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.
【作者单位】： 沈阳药科大学基于靶点的药物设计与研究教育部重点实验室;
【基金】：国家自然科学基金资助项目(81673308)
【分类号】：R979.1
，
本文编号：2416199
[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.
【作者单位】： 沈阳药科大学基于靶点的药物设计与研究教育部重点实验室;
【基金】：国家自然科学基金资助项目(81673308)
【分类号】：R979.1
，
本文编号：2416199
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