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针对CDC25和HDAC的新型双抑制剂用于治疗三阴性乳腺癌
Bidyadhar Sethy1, Richa Upadhyay2, Iin Narwanti1,3
1School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan.
Apoptosis : an international journal on programmed cell death
|October 12, 2024
概括
研究人员开发了针对细胞分裂周期25 (CDC25) 和三阴性乳腺癌 (TNBC) 的基因组脱乙酶 (HDAC) 的双重抑制剂. 化合物18A对TNBC表现出强烈的选择性活性,提供了一个有前途的新治疗途径.
科学领域:
- 在瘤学瘤学.
- 药用化学 医学化学
- 分子生物学分子生物学
背景情况:
- 三阴性乳腺癌 (TNBC) 具有侵略性,治疗选择有限.
- 细胞分裂周期25 (CDC25) 和基因素脱乙酶 (HDACs) 与各种癌症有关.
- 针对CDC25和HDAC都是一种新的治疗策略.
研究的目的:
- 开发针对CDC25和HDAC的双重抑制剂,用于TNBC治疗.
- 为了合成和评估结合CDC25和HDAC药的新型化合物.
- 为了确定TNBC的强效和选择性抑制剂.
主要方法:
- 通过结合oline-5,8-dione和酸/胺基部分,合成双重的CDC25/HDAC抑制剂.
- 在体外评估化合物对TNBC,其他癌细胞和非恶性细胞的细胞毒性.
- 评估化合物对CDC25活性,CDK1脱,细胞循环进展,DNA损伤和亡的影响.
主要成果:
- 化合物18A对TNBC细胞表现出强有力的和选择性的细胞毒性,省略了非恶性细胞.
- 18A表现出与MS-275相似的HDAC抑制,并有效抑制了CDC25活性和CDK1脱化.
- 18A诱导的S和G2/M阶段停止,DNA损伤和TNBC细胞的亡.
结论:
- 双重的CDC25/HDAC抑制剂18A显示出作为TNBC的向治疗的显著潜力.
- 18A的进一步临床前开发对于TNBC治疗是有必要的.
- 对CDC25和HDACs的双抑制是针对TNBC的可行策略.
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