Central Laboratory, Linyi Central Hospital, No.17 Jiankang Road, Linyi 276400, China.
State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, No.163 Xianlin Road, Nanjing 210023, China.
Curr Top Med Chem. 2019;19(15):1338-1349. doi: 10.2174/1568026619666190620155613.
Axl, a Receptor Tyrosine Kinase (RTK) belonging to the TAM (Axl, Mer, Tyro3) family, participates in many signal transduction cascades after mostly being stimulated by Growth arrestspecific 6(Gas6). Axl is widely expressed in many organs, such as macrophages, endothelial cells, heart, liver and skeletal muscle. Over-expression and activation of Axl are associated with promoting chemotherapy resistance, cell proliferation, invasion and metastasis in many human cancers, such as breast, lung, and pancreatic cancers. Therefore, the research and development of Axl inhibitors is of great significance to strengthen the means of cancer treatment, especially to solve the problem of drug resistance. Axl inhibitors have attracted more and more researchers' attention in recent years. This review discusses the research progress of Axl inhibitors in recent years.
Axl 是受体酪氨酸激酶(RTK)家族中的一员,属于 TAM(Axl、Mer、Tyro3)家族,主要在受到生长停滞特异性 6(Gas6)刺激后参与许多信号转导级联反应。Axl 在许多器官中广泛表达,如巨噬细胞、内皮细胞、心脏、肝脏和骨骼肌。Axl 的过度表达和激活与促进许多人类癌症(如乳腺癌、肺癌和胰腺癌)中的化疗耐药性、细胞增殖、侵袭和转移有关。因此,研究和开发 Axl 抑制剂对于加强癌症治疗手段具有重要意义,特别是解决耐药性问题。近年来,Axl 抑制剂引起了越来越多研究人员的关注。本文讨论了近年来 Axl 抑制剂的研究进展。