Junhong Yang, Guangcheng Yue, Zhiguo Fan, Ning Zhang, Shiwei Nie, Jing Li, Yuanyuan Ji
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Gene set enrichment analysis (GSEA) analyzed signaling pathways enriched by the NEK2 gene in LUAD. Dual luciferase and CHIP experiments were conducted to verify the binding relationship between NEK2 and FOXA1. Comet assay was utilized to analyze the level of DNA damage in LUAD cells. Western blot (WB) measured the expression levels of DNA damage-related proteins (γ-H2AX, p-ATM). The experimental results showed that FOXA1 and NEK2 were highly expressed in LUAD tissues and cells. GSEA analysis showed that NEK2 was enriched in DNA damage-related pathways, and silencing NEK2 could reduce the vitality of LUAD cisplatin-resistant cells, lower the IC<sub>50</sub> value of cells to cisplatin, and increase their DNA damage levels. FOXA1 can target the promoter region that binds to NEK2, and it can activate NEK2 through transcription to promote DNA damage repair and cisplatin resistance in cisplatin-resistant LUAD cells. This study confirms that FOXA1 can target NEK2 to promote DNA damage repair and cisplatin resistance in LUAD cells, providing a new valuable therapeutic target for the treatment of LUAD and the control of chemotherapy drug resistance.</p>\n </section>\n </div>","PeriodicalId":11291,"journal":{"name":"Drug Development Research","volume":"86 2","pages":""},"PeriodicalIF":3.5000,"publicationDate":"2025-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"FOXA1 Targets NEK2 to Mediate Cisplatin Resistance in Lung Adenocarcinoma Cells by Activating DNA Damage Repair\",\"authors\":\"Junhong Yang, Guangcheng Yue, Zhiguo Fan, Ning Zhang, Shiwei Nie, Jing Li, Yuanyuan Ji\",\"doi\":\"10.1002/ddr.70087\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div>\\n \\n \\n <section>\\n <p>Lung adenocarcinoma (LUAD) is one of the main causes of death in cancer patients, as its hidden course is difficult to uncover, resulting in many patients being diagnosed as advanced. 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引用次数: 0
摘要
肺腺癌(LUAD)是癌症患者死亡的主要原因之一,由于其隐藏的过程难以发现,导致许多患者被诊断为晚期。晚期LUAD患者容易对顺铂产生耐药性。本研究旨在探讨NEK2对LUAD细胞顺铂耐药的潜在分子调控机制。利用生物信息学方法分析NEK2和FOXA1在LUAD组织中的表达水平。采用qRT-PCR方法检测LUAD细胞中NEK2和FOXA1 mRNA的表达水平。CCK8检测并计算各组细胞的细胞活力和IC50值。基因集富集分析(GSEA)分析了NEK2基因在LUAD中富集的信号通路。通过双荧光素酶和CHIP实验验证NEK2与FOXA1的结合关系。采用彗星法分析LUAD细胞的DNA损伤水平。Western blot (WB)检测DNA损伤相关蛋白(γ-H2AX, p-ATM)的表达水平。实验结果显示,FOXA1和NEK2在LUAD组织和细胞中高表达。GSEA分析显示NEK2富集于DNA损伤相关通路,沉默NEK2可降低LUAD顺铂耐药细胞的活力,降低细胞对顺铂的IC50值,增加其DNA损伤水平。FOXA1可以靶向与NEK2结合的启动子区域,通过转录激活NEK2,促进顺铂耐药LUAD细胞DNA损伤修复和顺铂耐药。本研究证实FOXA1可以靶向NEK2促进LUAD细胞的DNA损伤修复和顺铂耐药,为LUAD的治疗和化疗耐药的控制提供了新的有价值的治疗靶点。
FOXA1 Targets NEK2 to Mediate Cisplatin Resistance in Lung Adenocarcinoma Cells by Activating DNA Damage Repair
Lung adenocarcinoma (LUAD) is one of the main causes of death in cancer patients, as its hidden course is difficult to uncover, resulting in many patients being diagnosed as advanced. Late-stage LUAD patients are prone to develop resistance to cisplatin. This study aims to explore the potential molecular regulatory mechanism of NEK2 on cisplatin resistance in LUAD cells. The expression levels of NEK2 and FOXA1 in LUAD tissues were analyzed based on bioinformatics methods. qRT-PCR analysis was carried out to measure the mRNA expression levels of NEK2 and FOXA1 in LUAD cells. CCK8 detected and calculated cell viability and IC50 values for each group of cells. Gene set enrichment analysis (GSEA) analyzed signaling pathways enriched by the NEK2 gene in LUAD. Dual luciferase and CHIP experiments were conducted to verify the binding relationship between NEK2 and FOXA1. Comet assay was utilized to analyze the level of DNA damage in LUAD cells. Western blot (WB) measured the expression levels of DNA damage-related proteins (γ-H2AX, p-ATM). The experimental results showed that FOXA1 and NEK2 were highly expressed in LUAD tissues and cells. GSEA analysis showed that NEK2 was enriched in DNA damage-related pathways, and silencing NEK2 could reduce the vitality of LUAD cisplatin-resistant cells, lower the IC50 value of cells to cisplatin, and increase their DNA damage levels. FOXA1 can target the promoter region that binds to NEK2, and it can activate NEK2 through transcription to promote DNA damage repair and cisplatin resistance in cisplatin-resistant LUAD cells. This study confirms that FOXA1 can target NEK2 to promote DNA damage repair and cisplatin resistance in LUAD cells, providing a new valuable therapeutic target for the treatment of LUAD and the control of chemotherapy drug resistance.
期刊介绍:
Drug Development Research focuses on research topics related to the discovery and development of new therapeutic entities. The journal publishes original research articles on medicinal chemistry, pharmacology, biotechnology and biopharmaceuticals, toxicology, and drug delivery, formulation, and pharmacokinetics. The journal welcomes manuscripts on new compounds and technologies in all areas focused on human therapeutics, as well as global management, health care policy, and regulatory issues involving the drug discovery and development process. In addition to full-length articles, Drug Development Research publishes Brief Reports on important and timely new research findings, as well as in-depth review articles. The journal also features periodic special thematic issues devoted to specific compound classes, new technologies, and broad aspects of drug discovery and development.