Department of Gastroenterology, Linyi People's Hospital, No. 27, Eastern Jiefang Road, Lanshan District, Linyi 276000, Shandong, China.
School of Pharmacy, Yantai University, 30 Qingquan Road, Yantai, 264005, Shandong, China.
Recent Pat Anticancer Drug Discov. 2020;15(3):228-238. doi: 10.2174/1574892815666200630102344.
BACKGROUND: Receptor Tyrosine Kinases (RTKs) play critical roles in a variety of cellular processes including growth, differentiation and angiogenesis, and in the development and progression of many types of cancer. Mesenchymal-Epithelial Transition Factor (c-Met) kinase is one of the types of RTKs and has become an attractive target for anti-tumor drug designing. c-Met inhibitors have a broad prospect in tumor prevention, chemotherapy, biotherapy, and especially in tumor resistance. OBJECTIVE: The purpose of this article is to review recent research progress of c-Met inhibitors reported in patents since 2015. METHODS: A comprehensive Scifinder and Web of Science literature review was conducted to identify all c-Met inhibitors published in patents since 2015. RESULTS: There are two kinds of c-Met inhibitors, one is from natural products, and the other one is of synthetic origin. Most of these c-Met inhibitors show potent in vivo and in vitro antitumor activities and have potential in the treatment of cancers. CONCLUSION: c-Met kinase inhibitors have emerged as an exciting new drug class for the treatment of all kinds of cancers, especially the Non-Small Cell Lung Cancer (NSCLC) with tumor resistance. More studies should be conducted on natural products to find novel c-Met kinase inhibitors.
背景:受体酪氨酸激酶(RTKs)在多种细胞过程中发挥着关键作用,包括生长、分化和血管生成,以及许多类型癌症的发生和发展。间质上皮转化因子(c-Met)激酶是 RTK 中的一种,已成为抗肿瘤药物设计的一个有吸引力的靶点。c-Met 抑制剂在肿瘤预防、化疗、生物治疗方面具有广阔的前景,特别是在肿瘤耐药方面。
目的:本文旨在综述 2015 年以来专利报道的 c-Met 抑制剂的最新研究进展。
方法:通过全面的 Scifinder 和 Web of Science 文献检索,确定了 2015 年以来专利中发表的所有 c-Met 抑制剂。
结果:c-Met 抑制剂有两种来源,一种来自天然产物,另一种来自合成。这些 c-Met 抑制剂大多数在体内和体外都表现出很强的抗肿瘤活性,在癌症治疗方面具有潜力。
结论:c-Met 激酶抑制剂已成为治疗各种癌症的一种令人兴奋的新药类别,特别是对具有肿瘤耐药性的非小细胞肺癌(NSCLC)。应进一步研究天然产物以寻找新型的 c-Met 激酶抑制剂。
Recent Pat Anticancer Drug Discov. 2020
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