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新型KRAS突变体抑制剂抗胰腺癌的作用研究

罗桂芳 陈攀 刘晓雨 胡舒洁 杨小平

肿瘤药学2025,Vol.15Issue(2):169-177,9.
肿瘤药学2025,Vol.15Issue(2):169-177,9.DOI:10.3969/j.issn.2095-1264.2025.02.04

新型KRAS突变体抑制剂抗胰腺癌的作用研究

Study on the effects of novel KRAS mutant inhibitors on pancreatic cancer

罗桂芳 1陈攀 2刘晓雨 3胡舒洁 3杨小平2

作者信息

  • 1. 湖南师范大学医学部 小分子靶向药物研究与创制湖南省重点实验室,湖南 长沙,410013||湖南九典制药股份有限公司,湖南 长沙,410205
  • 2. 湖南师范大学医学部 小分子靶向药物研究与创制湖南省重点实验室,湖南 长沙,410013
  • 3. 湖南九典制药股份有限公司,湖南 长沙,410205
  • 折叠

摘要

Abstract

Objective To delineate the effects of the novel KRAS mutant inhibitor JQC series compounds(JQC-001 to JQC-006)on pancreatic cancer.Methods The inhibitory effects of JQC compounds on the proliferation of KRAS-mutant tumor cells(DU 145,A549,PANC-1,HCT-116)were evaluated using the MTT assay.RT-qPCR was performed to assess the impact of JQC-005 on KRAS mRNA expression in PANC-1 cells.A PANC-1 xenograft nude mouse model was estab-lished to evaluate the in vivo antitumor activity of JQC-005.Results With the exception of JQC-004,the remaining JQC se-ries compounds(JQC-001,JQC-002,JQC-003,JQC-005,JQC-006)were found to inhibit the proliferation of human pros-tate cancer DU 145 cells,human non-small cell lung cancer A549 cells,human pancreatic cancer PANC-1 cells,and hu-man colon cancer HCT-116 cells in a dose-dependent manner.JQC-005 significantly down-regulated the expression of KRAS mRNA in PANC-1 cells,and markedly suppressed tumor growth in the PANC-1 xenograft nude mouse model.Con-clusion The JQC series compounds,particularly JQC-005,exhibit significant anti-pancreatic cancer effects,potentially mediated through regulation of KRAS mutant activity.

关键词

JQC系列化合物/胰腺癌/KRAS突变体/新型KRAS突变体抑制剂

Key words

JQC series compounds/Pancreatic cancer/KRAS mutant/Novel KRAS mutant inhibitors

分类

医药卫生

引用本文复制引用

罗桂芳,陈攀,刘晓雨,胡舒洁,杨小平..新型KRAS突变体抑制剂抗胰腺癌的作用研究[J].肿瘤药学,2025,15(2):169-177,9.

基金项目

湖南师范大学生殖健康与转化医学研究团队资助项目(2023JC101). (2023JC101)

肿瘤药学

2095-1264

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