摘要/Abstract

摘要： AXL属于受体酪氨酸激酶中的TAM（TYRO3-AXL-MER）家族，在非小细胞肺癌、乳腺癌、卵巢癌等多种癌症中高表达，并介导上皮间质转化的发生，在肿瘤耐药中起重要作用；AXL还可以通过调节信号通路以及影响肿瘤微环境等来介导靶向治疗耐药的产生。临床上，AXL对于肿瘤患者的预后评价具有重要意义，以AXL为靶点的治疗有望成为一项治疗癌症的新策略。目前已有AXL多靶点小分子抑制剂被批准上市，还有多种特异性更高的抑制剂正处于临床或临床前研究阶段。该文着重介绍了AXL介导肿瘤耐药的机制，并总结不同AXL抑制剂的研究概况，从而为以AXL为靶点的抗肿瘤研究和治疗提供新思路。
关键词: AXL, 受体酪氨酸激酶, 肿瘤, 耐药, 上皮间质转化, 小分子抑制剂, 预后
Abstract:
AXL is a member of TAM (TYRO3-AXL-MER) family of receptor tyrosine kinases, which is overexpressed in many cancers, including non-small cell lung cancer, breast cancer and ovarian cancer. It can mediate the occurrence of epithelial-mesenchymal transition, and plays an important role in tumor drug resistance. In addition, AXL can also mediate the occurrence of targeted agents resistanceregulating the signaling pathway and influencing tumor microenviroment. As a result, AXL is an attractive candidate not only as a prognostic indicator in malignancy but also as a target for anti-cancer therapy. Several multi-target small molecule inhibitors against AXL have been approved, and varieties of inhibitors with higher specificity are in clinical or preclinical studies. This article focused on the role of AXL in tumor drug resistance and summarized the research profiles of different small molecule inhibitors against AXL to provide new ideas for anti-tumor research and therapy.
Key words: AXL, receptor tyrosine kinase, tumor, drug resistance, epithelial-mesenchymal transition, small molecule inhibitor, prognosis


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