Department of Chemistry, Pohang University of Science and Technology, Pohang 37673, South Korea.
ACS Appl Bio Mater. 2024 Jun 17;7(6):3991-3996. doi: 10.1021/acsabm.4c00342. Epub 2024 Jun 5.
Mitigating the adverse effects of anticancer agents requires innovative prodrug engineering. In this study, we showcase the potential of our -quinone methide-based trigger-release-conjugation platform as a versatile tool for constructing advanced prodrug systems. Using this platform, we achieved the light-triggered release of an anticancer drug mechlorethamine, targeting mitochondrial DNA. The entire process was adeptly tracked through the emission of fluorescence signals, revealing notable effects across various cancer cell lines compared to a normal cell line. Exploring alternative cancer-associated triggers, including enzymes, and incorporating cancer/tumor-specific targeting elements could lead to effective prodrugs with reduced cytotoxicity.
减轻抗癌药物的不良反应需要创新的前药工程。在这项研究中，我们展示了我们基于 - 醌甲叉的触发释放偶联平台作为构建先进前药系统的多功能工具的潜力。使用这个平台，我们实现了抗癌药物盐酸氮芥的光触发释放，靶向线粒体 DNA。整个过程通过荧光信号的发射进行了巧妙的跟踪，与正常细胞系相比，在各种癌细胞系中都显示出了显著的效果。探索替代的癌症相关触发因素，包括酶，并结合癌症/肿瘤特异性靶向元件，可以开发出具有降低细胞毒性的有效前药。
