Anti-Protein-Adsorption Nano-Proteolysis Targeting Chimeras as a Potent Platform for Efficient Programmed Cell Death Ligand 1 Degradation

下调和上调 蛋白质水解 化学 细胞生物学 免疫系统 黑色素瘤 免疫检查点 HEK 293细胞 抑制器 泛素 效应器 蛋白质降解 配体(生物化学) 程序性细胞死亡 泛素连接酶 细胞 癌症研究 生物物理学 封锁 细胞存活 计算生物学 内吞作用 纳米技术 降级(电信) 两亲性 自噬 免疫疗法 内化
作者
Xiang Lu,Shihui Song,Furui Qiu,Hongling Zhang,Jinjin Shi,Binghua Wang
出处
期刊:ACS Nano [American Chemical Society]
卷期号:20 (7): 6110-6124
标识
DOI:10.1021/acsnano.5c19999
摘要

Immune checkpoint blockade (ICB) therapies targeting the PD-1/PD-L1 axis have shown clinical promise, yet most patients do not achieve durable responses due to adaptive PD-L1 upregulation and recycling. While nanoparticle-based proteolysis targeting chimeras (PROTACs) offer a strategy for direct PD-L1 degradation, their therapeutic potential remains largely untapped because of a fundamental barrier: the inevitable formation of a nonspecific protein corona that severely limits target engagement. Here, we introduce a corona-free nano-PROTACs platform (CF-nPTs) that overcomes this obstacle. By integrating DSPE-PCB─a zwitterionic antifouling amphiphile with exceptional resistance to protein adsorption─into micellar nano-PROTACs, we construct a nano-PROTACs system capable of maintaining an ultraclean surface in biological fluids. Compared with previously reported Au, liposomal, and micellar based nano-PROTACs platforms, the CF-nPTs effectively resisted nonspecific protein adsorption, markedly enhanced the corecruitment of PD-L1 and E3 ligase, and enabled highly efficient proteasome-mediated PD-L1 degradation. Additionally, the corona-free architecture also promoted robust lymph-node targeting, further amplifying immunotherapeutic efficacy. As a result, CF-nPTs achieved pronounced tumor regression, extended survival, and strong immune activation in both subcutaneous melanoma and lymph-node-metastasis models. Collectively, this study identifies protein-corona resistance as a key determinant of nano-PROTACs performance and establishes CF-nPTs as a promising platform for efficient target protein degradation.
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