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作为乳腺癌有效抗瘤策略的基于双阿普塔默的SETDB1 PROTACs

Yanxuan Guo¹, Yingge Lv¹, Shuyu Huang¹

¹The Province and Ministry Co-Sponsored Collaborative Innovation Center for Medical Epigenetics, State Key Laboratory of Experimental Hematology, Key Laboratory of Breast Cancer Prevention and Therapy (Tianjin Medical University), Ministry of Education, Key Laboratory of Immune Microenvironment and Disease (Tianjin Medical University), Ministry of Education, Department of Biochemistry and Molecular Biology, School of Basic Medical Sciences, Tianjin Medical University, Tianjin, China.

Advanced science (Weinheim, Baden-Wurttemberg, Germany)

|January 7, 2026

概括

新的基于双体的PROTAC向表观遗传调节器SETDB1,这是乳腺癌的关键驱动因素. 这些PROTACs降解SETDB1,抑制癌症生长并增强免疫反应.

科学领域:

生物化学生物化学
分子生物学分子生物学
在瘤学瘤学.

背景情况:

蛋白质溶解T向化马体 (PROTACs) 是一种针对瘤原蛋白的新型治疗策略.
SET域分叉的基因组 lysine 甲基转移酶 1 (SETDB1) 是一个关键的表观遗传调节器,参与乳腺癌的进展,耐药性和免疫逃避.

研究的目的:

开发和描述针对乳腺癌治疗的SETDB1的基于双体的PROTACs.
评估这些PROTACs在抑制乳腺癌细胞增殖,迁移和耐药性以及调节瘤免疫微环境方面的有效性.

主要方法:

通过指数式丰富对联体的系统进化 (SELEX) 用于识别针对SETDB1.1.的高亲和性ssDNA吸收体.
该SETDB1体与AS1411体结合,产生单链 (AP-SETDB1-S6A) 和部分双链 (AP-SETDB1-D2) 的PROTACs.
通过细胞增殖,迁移,药物敏感化,T细胞细胞毒性和体内瘤生长试验来评估PROTAC活性.

主要成果:

AP-SETDB1-S6A和AP-SETDB1-D2都表现出良好的血清稳定性,并通过招募MDM2有效诱导乳腺癌细胞中SETDB1的蛋白酶依赖性降解.
这些PROTAC显著抑制了乳腺癌细胞的增殖和迁移,并重新敏感化了对他莫西芬耐药的细胞.
该PROTACs增强了CD8+T细胞介导的细胞毒性对乳腺癌细胞和抑制瘤生长在体内.

结论:

针对SETDB1的基于双体的PROTACs为乳腺癌提供了一个有前途的治疗方法.
这些新型药物表现出强大的抗癌活性,包括克服药物耐药性和调节免疫反应,突出其临床转化潜力.

关键词:

这就是PROTAC.在SETDB1中,我们可以使用SETDB1.一个aptamer的应用程序.乳腺癌乳腺癌乳腺癌

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