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基于聚炔桥连红光 AIE 生色团的生物正交 AIE 点用于肿瘤代谢标记和靶向成像。

Bio-orthogonal AIE Dots Based on Polyyne-Bridged Red-emissive AIEgen for Tumor Metabolic Labeling and Targeted Imaging.

机构信息

HKUST Shenzhen Research Institute, No. 9 Yuexing First RD, South Area, Hi-Tech Park, Nanshan, Shenzhen, 518057, China.

Department of Chemistry, Hong Kong Branch of Chinese National Engineering Research Centre for Tissue Restoration and Reconstruction, Institute for Advanced Study, Institute of Molecular Functional Materials, State Key Laboratory of Molecular Neuroscience, Division of Life Science, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China.

出版信息

Chem Asian J. 2019 Mar 15;14(6):770-774. doi: 10.1002/asia.201801609. Epub 2018 Dec 21.

DOI:10.1002/asia.201801609
PMID:30536637
Abstract

In this work, we aim to develop cancer cell-targeting AIE dots based on a polyyne-bridged red-emissive AIEgen, 2TPE-4E, through the combination of metabolic engineering and bio-orthogonal reactions. Azide groups on a tumor were efficiently produced by intravenous injection of Ac4ManNAz and glycol-metabolic engineering. These bio-orthogonal azide groups could facilitate the specific targeting of DBCO-AIE dots to the tumor cells undergoing metal-free click reaction in vivo. The efficiency of this targeting strategy could be further improved with the development of new bio-orthogonal chemical groups with higher reactivity and a large amount of AIEgens could be delivered to the tumor for diagnosis.

摘要

在这项工作中,我们旨在通过代谢工程和生物正交反应的结合,基于聚炔桥联的红色发光 AIE 物 2TPE-4E,开发基于癌细胞靶向的 AIE 点。通过静脉注射 Ac4ManNAz 和糖代谢工程,在肿瘤上高效产生叠氮基团。这些生物正交叠氮基团可以促进 DBCO-AIE 点在体内无金属点击反应下特异性靶向肿瘤细胞。通过开发具有更高反应活性的新生物正交化学基团,可以进一步提高这种靶向策略的效率,并且可以将大量 AIE 物递送到肿瘤中进行诊断。

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