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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.

DOI:10.1039/d5cb00196j
PMID:40896116
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12394912/
Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f576/12394912/b02a489ff226/d5cb00196j-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f576/12394912/f82f6dec15a5/d5cb00196j-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f576/12394912/18bc859b985c/d5cb00196j-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f576/12394912/84828a7ea642/d5cb00196j-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f576/12394912/6c4e8a910111/d5cb00196j-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f576/12394912/60231bc1d251/d5cb00196j-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f576/12394912/b02a489ff226/d5cb00196j-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f576/12394912/f82f6dec15a5/d5cb00196j-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f576/12394912/18bc859b985c/d5cb00196j-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f576/12394912/84828a7ea642/d5cb00196j-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f576/12394912/6c4e8a910111/d5cb00196j-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f576/12394912/60231bc1d251/d5cb00196j-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f576/12394912/b02a489ff226/d5cb00196j-f5.jpg

相似文献

1
Reductively activated CPP-PROTAC nanocomplexes enhance target degradation efficient cellular uptake.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。
RSC Chem Biol. 2025 Aug 25. doi: 10.1039/d5cb00196j.
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Acta Pharmacol Sin. 2024 Aug;45(8):1740-1751. doi: 10.1038/s41401-024-01266-z. Epub 2024 Apr 12.
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本文引用的文献

1
PROTAC Delivery Strategies for Overcoming Physicochemical Properties and Physiological Barriers in Targeted Protein Degradation.用于克服靶向蛋白质降解中物理化学性质和生理屏障的PROTAC递送策略
Pharmaceutics. 2025 Apr 9;17(4):501. doi: 10.3390/pharmaceutics17040501.
2
Advancements in delivery Systems for Proteolysis-Targeting Chimeras (PROTACs): Overcoming challenges and expanding biomedical applications.蛋白酶靶向嵌合体（PROTACs）递送系统的进展：克服挑战并拓展生物医学应用
J Control Release. 2025 Jun 10;382:113719. doi: 10.1016/j.jconrel.2025.113719. Epub 2025 Apr 21.
3
Conquering PROTAC molecular design and drugability.
攻克PROTAC分子设计与成药特性
Bioanalysis. 2025 Apr;17(7):455-470. doi: 10.1080/17576180.2025.2481021. Epub 2025 Mar 20.
4
Silica-based EGFR-degrading nano-PROTACs for efficient therapy of non-small cell lung cancer.用于非小细胞肺癌高效治疗的基于二氧化硅的表皮生长因子受体降解纳米蛋白降解靶向嵌合体
Eur J Pharm Biopharm. 2025 May;210:114699. doi: 10.1016/j.ejpb.2025.114699. Epub 2025 Mar 18.
5
Design and optimization strategies of PROTACs and its Application, Comparisons to other targeted protein degradation for multiple oncology therapies.PROTACs的设计与优化策略及其应用，与其他用于多种肿瘤治疗的靶向蛋白质降解方法的比较
Bioorg Chem. 2025 Jan;154:107984. doi: 10.1016/j.bioorg.2024.107984. Epub 2024 Nov 22.
6
Property-based optimisation of PROTACs.基于性质的PROTACs优化。
RSC Med Chem. 2024 Nov 7. doi: 10.1039/d4md00769g.
7
Recent insights of PROTAC developments in inflammation-mediated and autoimmune targets: a critical review.炎症介导和自身免疫靶点中PROTACs开发的最新见解：一项批判性综述。
RSC Med Chem. 2024 May 8;15(8):2585-2600. doi: 10.1039/d4md00142g. eCollection 2024 Aug 14.
8
Research Progress of Disulfide Bond Based Tumor Microenvironment Targeted Drug Delivery System.基于二硫键的肿瘤微环境靶向药物传递系统的研究进展。
Int J Nanomedicine. 2024 Jul 24;19:7547-7566. doi: 10.2147/IJN.S471734. eCollection 2024.
9
Lipid-mediated intracellular delivery of recombinant bioPROTACs for the rapid degradation of undruggable proteins.脂质介导的重组生物 PROTACs 的细胞内递送用于快速降解不可成药的蛋白质。
Nat Commun. 2024 Jul 10;15(1):5808. doi: 10.1038/s41467-024-50235-x.
10
Recent Advances in Targeted Cancer Therapy: Are PDCs the Next Generation of ADCs?靶向癌症治疗的最新进展：PDCs 是否是下一代 ADC 药物？
J Med Chem. 2024 Jul 25;67(14):11469-11487. doi: 10.1021/acs.jmedchem.4c00106. Epub 2024 Jul 9.