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Issue 4, 2015
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Bioorthogonal oxime ligation mediated in vivo cancer targeting

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Abstract

Current cancer targeting relying on specific biological interaction between the cell surface antigen and respective antibody or its analogue has proven to be effective in the treatment of different cancers; however, this strategy has its own limitations, such as the heterogeneity of cancer cells and immunogenicity of the biomacromolecule binding ligands. Bioorthogonal chemical conjugation has emerged as an attractive alternative to biological interaction for in vivo cancer targeting. Here, we report an in vivo cancer targeting strategy mediated by bioorthogonal oxime ligation. An oxyamine group, the artificial target, is introduced onto 4T1 murine breast cancer cells through liposome delivery and fusion. Poly(ethylene glycol)-polylactide (PEG-PLA) nanoparticles (NPs) are surface-functionalized with aldehyde groups as targeting ligands. The improved in vivo cancer targeting of PEG-PLA NPs is achieved through specific and efficient chemical reaction between the oxyamine and aldehyde groups.

Graphical abstract: Bioorthogonal oxime ligation mediated in vivo cancer targeting

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Publication details

The article was received on 07 Jan 2015, accepted on 11 Jan 2015 and first published on 02 Feb 2015


Article type: Edge Article
DOI: 10.1039/C5SC00063G
Citation: Chem. Sci., 2015,6, 2182-2186
  • Open access: Creative Commons BY-NC license
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    Bioorthogonal oxime ligation mediated in vivo cancer targeting

    L. Tang, Q. Yin, Y. Xu, Q. Zhou, K. Cai, J. Yen, L. W. Dobrucki and J. Cheng, Chem. Sci., 2015, 6, 2182
    DOI: 10.1039/C5SC00063G

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