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核小体——靶向肿瘤细胞核。

Nuclisome--targeting the tumor cell nucleus.

作者信息

Gedda Lars, Edwards Katarina

机构信息

Department of Radiology, Oncology and Radiation Sciences, Unit of Biomedical Radiation Sciences, Rudbeck Laboratory, Uppsala University, 751 85 Uppsala, Sweden.

出版信息

Tumour Biol. 2012 Jun;33(3):661-7. doi: 10.1007/s13277-012-0341-3.

Abstract

The Nuclisome concept builds on a novel two-step targeting strategy with the aim to deliver short-range Auger-electron-emitting radionuclides to nuclear DNA of tumor cells. The concept is based on the use of Nuclisome-particles, i.e., tumor-targeted PEG-stabilized liposomes loaded with a unique DNA-intercalating compound that enables specific and effective delivery of radionuclides to DNA. The specific and potent two-step targeting leads to eradication of tumor cells while toxicity to normal organs is reduced to a minimum. Results of in vitro and in vivo studies point towards the Nuclisome concept as a promising strategy for the treatment of small tumor masses and, in particular, for the elimination of spread single cells and micrometastases.

摘要

核小体概念基于一种新颖的两步靶向策略,旨在将发射俄歇电子的短程放射性核素递送至肿瘤细胞的核DNA。该概念基于核小体颗粒的使用,即负载有独特DNA嵌入化合物的肿瘤靶向聚乙二醇稳定脂质体,该化合物能够将放射性核素特异性且有效地递送至DNA。这种特异性且强效的两步靶向可导致肿瘤细胞的根除,同时将对正常器官的毒性降至最低。体外和体内研究结果表明,核小体概念是治疗小肿瘤块,特别是消除扩散的单个细胞和微转移的一种有前景的策略。

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