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使用小分子抑制剂选择性向BCL6是一种潜在的卵巢癌治疗策略

Min Wu¹, Jiuqing Xie¹, Yajing Xing¹

¹East China Normal University, Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, 500 Dong Chuan Rd, Shanghai 200241, China.

International journal of biological sciences

|January 3, 2024

概括

一种名为WK369的新药向B细胞淋巴瘤6 (BCL6) 以有效治疗卵巢癌. 这种新型抑制剂对抗抗西斯胺抗性瘤有前途,并在临床前模型中提高了生存率.

科学领域:

在瘤学瘤学.
分子生物学分子生物学
药物发现药物发现药物发现

背景情况:

卵巢癌的死亡率很高,五年生存率很低 (<35%).
乙细胞淋巴瘤6 (BCL6) 与卵巢癌的预后不佳和对西斯普拉丁的耐药性有关.
需要针对BCL6的新型治疗策略.

研究的目的:

研究向BCL6在卵巢癌治疗中的潜力.
开发和评估一种新的BCL6小分子抑制剂,名为WK369.9.
为了阐明WK369.9的抗癌机制.

主要方法:

开发了一种新的BCL6小分子抑制剂,WK369.9.
在体外和体内评估WK369的抗卵巢癌活性,包括对细胞周期,细胞亡,生长和转移的影响.
涉及BCL6-BTB域结合,SMRT相互作用阻断和下游信号通路分析 (p53,ATR,CDKN1A,AKT,MEK/ERK) 的机制研究.

主要成果:

WK369表现出显著的抗卵巢癌生物活性,诱导细胞循环停止和亡.
在没有明显的毒性的情况下,WK369在体外和体内抑制了瘤生长和转移.
在小鼠中,WK369延长了生存时间,并显示对抗抗西斯普拉丁的卵巢癌细胞系的有效性.
在机械上,WK369阻断了BCL6-SMRT相互作用,重新激活了p53,ATR和CDKN1A,并抑制了BCL6-AKT和BCL6-MEK/ERK信号传输.

结论:

向BCL6代表了对卵巢癌的有希望的治疗策略.
WK369表现出强大的抗瘤作用,并具有作为卵巢癌的候选治疗剂的潜力,包括对西斯普拉丁耐药的病例.

关键词:

在 BCL6 中.BTB 域名 BTB 域名转移转移转移转移卵巢癌是发生在卵巢中的癌症.

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