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

IF 2.9 4区 医学 Q3 ENDOCRINOLOGY & METABOLISM Discover. Oncology Pub Date : 2025-02-27 DOI:10.1007/s12672-025-02010-7
Xifeng Xiong, Yulin Liu, Yanli Du, Xudong Lai, Chunming Si, Haixiong Miao
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Abstract

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.

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揭示GSK126对骨肉瘤细胞凋亡、自噬和细胞迁移的影响。
骨肉瘤是一种恶性骨肿瘤,其治疗面临着重大挑战。zeste同源物增强子2 (Enhancer of zeste homolog 2, EZH2)在包括骨肉瘤在内的多种肿瘤中异常表达,被认为是潜在的治疗靶点。EZH2抑制剂GSK126的抗癌功效备受关注,但其对骨肉瘤细胞的影响尚不完全清楚。本研究探讨了GSK126对骨肉瘤细胞的影响,特别是对细胞凋亡、自噬和细胞运动的影响。我们的研究结果表明,GSK126通过下调融合结合蛋白1 (FBP1)/C-Myc轴,诱导细胞凋亡和自噬,如cleaved caspase-3和LC3-II等标志物的增加,以及细胞迁移的减少。这些发现表明GSK126具有促进细胞死亡和阻碍迁移的双重作用,是一种很有希望的骨肉瘤治疗药物。
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来源期刊
Discover. Oncology
Discover. Oncology Medicine-Endocrinology, Diabetes and Metabolism
CiteScore
2.40
自引率
9.10%
发文量
122
审稿时长
5 weeks
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