ROS1型
癌症研究
肺癌
激酶
靶向治疗
间变性淋巴瘤激酶
化学
癌症
药物发现
腺癌
医学
内科学
生物化学
恶性胸腔积液
作者
Yingxue Li,Yanna Lv,Cheng Zhang,Bo Fu,Yue Liu,Jinxing Hu
标识
DOI:10.1016/j.ejmech.2023.115477
摘要
As a member of the insulin-receptor superfamily, ALK plays an important role in regulating the growth, proliferation, and survival of cells. ROS1 is highly homologous with ALK, and can also regulate normal physiological activities of cells. The overexpression of both is closely related to the development and metastasis of tumors. Therefore, ALK and ROS1 may serve as important therapeutic targets in non-small cell lung cancer (NSCLC). Clinically, many ALK inhibitors have shown powerful therapeutic efficacy in ALK and ROS1-positive NSCLC patients. However, after some time, patients inevitably develop drug resistance, leading to treatment failure. There are no significant drug breakthroughs in solving the problem of drug-resistant mutations. In this review, we summarize the chemical structural features of several novel dual ALK/ROS1 inhibitors, their inhibitory effect on ALK and ROS1 kinases, and future treatment strategies for patients with ALK and ROS1 inhibitor-resistant mutations.
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