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<p>Osteosarcoma, a malignant bone tumor, faces significant treatment challenges. Enhancer of zeste homolog 2 (EZH2) shows aberrant expression in various tumors including osteosarcoma, which is identified as a potential therapeutic target. The anti-cancer efficacy of EZH2 inhibitor GSK126 has attracted attention, yet its impact on osteosarcoma cells was not fully understood. The study investigated the effects of GSK126 on osteosarcoma cells, particularly in apoptosis, autophagy, and cell motility. Our findings revealed that GSK126 induced apoptosis and autophagy, evidenced by increased markers like cleaved caspase-3 and LC3-II, and decreased cellular migration, through downregulation of the <Emphasis Type="Underline">F</Emphasis>use <Emphasis Type="Underline">B</Emphasis>inding <Emphasis Type="Underline">P</Emphasis>rotein 1 (FBP1)/C-Myc axis. These findings suggest GSK126 as a promising therapeutic against osteosarcoma, offering a dual action of promoting cell death and hindering migration.</p>

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Unveiling the effects of GSK126 on osteosarcoma cells implications for apoptosis, autophagy, and cellular migration

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年2月27日

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  • Xifeng Xiong,
  • Yulin Liu,
  • Yanli Du,
  • Xudong Lai,
  • Chunming Si,
  • Haixiong Miao

摘要

Osteosarcoma, a malignant bone tumor, faces significant treatment challenges. Enhancer of zeste homolog 2 (EZH2) shows aberrant expression in various tumors including osteosarcoma, which is identified as a potential therapeutic target. The anti-cancer efficacy of EZH2 inhibitor GSK126 has attracted attention, yet its impact on osteosarcoma cells was not fully understood. The study investigated the effects of GSK126 on osteosarcoma cells, particularly in apoptosis, autophagy, and cell motility. Our findings revealed that GSK126 induced apoptosis and autophagy, evidenced by increased markers like cleaved caspase-3 and LC3-II, and decreased cellular migration, through downregulation of the Fuse Binding Protein 1 (FBP1)/C-Myc axis. These findings suggest GSK126 as a promising therapeutic against osteosarcoma, offering a dual action of promoting cell death and hindering migration.