还原激活的CPP-PROTAC纳米复合物增强了靶点降解及高效的细胞摄取。
Reductively activated CPP-PROTAC nanocomplexes enhance target degradation efficient cellular uptake.
作者信息
Miyamoto Maho, Saito Kosuke, Yokoo Hidetomo, Demizu Yosuke
机构信息
Graduate School of Medical Life Science, Yokohama City University 1-7-29 Yokohama 230-0045 Japan.
Division of Organic Chemistry, National Institute of Health Sciences 3-25-26 Tonomachi Kawasaki 210-9501 Japan
出版信息
RSC Chem Biol. 2025 Aug 25. doi: 10.1039/d5cb00196j.
We developed a nanoparticle based on a cell-penetrating peptide-PROTAC conjugate with a disulfide linker, , and dextran sulfate, enhancing cellular uptake and BRD4 degradation. This delivery platform significantly improves PROTAC bioavailability and offers a promising strategy to overcome membrane permeability challenges for targeted protein degradation.
我们开发了一种基于细胞穿透肽-蛋白酶体靶向嵌合体（PROTAC）共轭物、二硫键连接子以及硫酸葡聚糖的纳米颗粒，可增强细胞摄取和BRD4降解。该递送平台显著提高了PROTAC的生物利用度，并为克服靶向蛋白质降解的膜通透性挑战提供了一种有前景的策略。
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