靶向KRAS G12突变肿瘤药物的作用机制及研究进展
Mechanism of Action and Research Progress of Drugs Targeting KRAS G12-Mutant Tumors
DOI: 10.12677/wjcr.2025.152011, PDF,    科研立项经费支持
作者: 郑金蓉, 郎靖瑜, 毛 佳, 孟秋韵, 孟渝维, 张世谱, 卿 晨*：昆明医科大学药学院暨云南省天然药物药理重点实验室，云南 昆明
关键词: KRAS突变；靶向治疗；共价抑制剂；临床研究；KRAS Mutation； Targeted Therapy； Covalent Inhibitors； Clinical Research
摘要: Kirsten大鼠肉瘤病毒癌基因同源物(KRAS)是人类癌症中常见的突变癌基因，KRAS G12突变是KRAS最常见的突变类型。突变导致KRAS蛋白在细胞信号转导中持续活化，促进肿瘤的生长与转移。尽管KRAS在过去被视作不可成药的靶点，但近年来已有多款KRAS G12C靶向药物上市或进入临床研究阶段。本文对各类KRAS G12抑制剂的代表化合物、作用机制及生物活性的研究进展进行综述，旨在为KRAS G12小分子抑制剂抗肿瘤药物的开发提供思路和参考。
Abstract: The Kirsten rat sarcoma viral oncogene homolog (KRAS) is a frequently mutated oncogene in human cancers, with the KRAS G12 mutation being the most common type of KRAS mutation. This mutation leads to the continuous activation of the KRAS protein in cellular signal transduction, promoting tumor growth and metastasis. Although KRAS was historically considered an undruggable target, several KRAS G12C-targeted drugs have been approved or entered clinical research stages in recent years. This article reviews the representative compounds, mechanisms of action, and research progress on the biological activities of various KRAS G12 inhibitors, aiming to provide insights and references for the development of small-molecule inhibitors targeting KRAS G12 in anti-tumor drug discovery.
文章引用：郑金蓉, 郎靖瑜, 毛佳, 孟秋韵, 孟渝维, 张世谱, 卿晨. 靶向KRAS G12突变肿瘤药物的作用机制及研究进展[J]. 世界肿瘤研究, 2025, 15(2): 77-89. https://doi.org/10.12677/wjcr.2025.152011

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