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Issue 24, 2018
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2-Aminoimidazole facilitates efficient gene delivery in a low molecular weight poly(amidoamine) dendrimer

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Abstract

Functional groups have shown great potential in gene delivery. However, a number of the reported functional groups can only overcome one certain physiological barrier, resulting in limited transfection efficiencies. Based on the structure–activity relationships of both imidazolyl and guanidyl, we designed a novel multifunctional group, 2-aminoimidazole (AM), for gene delivery. On modifying with the AM group, the transfection efficiency of low molecular weight poly(amidoamine) (G2) was 200 times greater than the parent dendrimer in vitro. In contrast, the transfection efficiency of G2 showed a decreasing trend when it was grafted with imidazole. Assays revealed that the AM group played multiple roles in gene delivery, including condensing DNA into monodisperse nanoparticles of 80–90 nm in diameter, achieving nearly ten times higher cellular-uptake efficacy, and enhancing the abilities of endosome/lysosome escape and nuclear localization. What's more, AM showed low toxicity. These results demonstrate that the AM group could be a promising tool in non-viral gene delivery.

Graphical abstract: 2-Aminoimidazole facilitates efficient gene delivery in a low molecular weight poly(amidoamine) dendrimer

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Publication details

The article was received on 23 Apr 2018, accepted on 21 May 2018 and first published on 22 May 2018


Article type: Paper
DOI: 10.1039/C8OB00953H
Citation: Org. Biomol. Chem., 2018,16, 4464-4470
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    2-Aminoimidazole facilitates efficient gene delivery in a low molecular weight poly(amidoamine) dendrimer

    J. Wang, X. Hu, D. Wang, C. Xie, W. Lu, J. Song, R. Wang, C. Gao and M. Liu, Org. Biomol. Chem., 2018, 16, 4464
    DOI: 10.1039/C8OB00953H

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