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间变性淋巴瘤激酶抑制剂的研究进展

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间变性淋巴瘤激酶(ALK)基因与棘皮动物微管相关类蛋白4(EML4)基因由于染色体易位而发生融合,形成具有强大致癌作用的融合基因EML4-ALK,促使细胞发生癌变,占非小细胞肺癌(NSCLC)患者的3%~7%.随着肿瘤分子靶向治疗的研究进展,已有多种ALK酪氨酸激酶抑制剂(ALK-TKI)逐渐应用于EML4-ALK阳性的NSCLC患者,较传统化疗显示出更好的疗效.因此ALK小分子抑制剂的开发已成为研究热点.本文对近年的小分子ALK抑制剂及其抗肿瘤应用等部分研究文献进行综述.
Research progress in anaplastic lymphoma kinase inhibitors
The anaplastic lymphoma kinase(ALK)gene is fused with the echinoderm microtubule-associated protein like 4(EML4)gene due to a chromosomal translocation,resulting in the formation of the potent oncogenic EML4-ALK fusion gene.The EML4-ALK fusion gene is a potent oncogenic gene that contributes to cellular carcinogenesis,which accounts for 3%~7%of non-small cell lung cancer(NSCLC).With the progress in tumor molecular targeted therapy,many ALK tyrosine kinase inhibitors(ALK-TKI)have been gradually used for EML4-ALK-positive NSCLC patients,showing better efficacy than that of traditional chemotherapy.Therefore,the development of ALK small molecule inhibitors has become a research hotspot.This paper reviewed some literatures on small molecule ALK inhibitors and their anticancer application in recent years.

mesenchymal lymphoma kinasesmall molecule inhibitortumornon-small cell lung cancer

李湘静、郑鹏武、朱五福

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江西科技师范大学药学院,南昌 330013

间变性淋巴瘤激酶 小分子抑制剂 肿瘤 非小细胞肺癌

国家自然科学基金项目

82060629

2024

中南药学
湖南省药学会

中南药学

CSTPCD
影响因子:0.736
ISSN:1672-2981
年,卷(期):2024.22(10)