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Glycopeptide Nanoconjugates Based on Multilayer Self-Assembly as an Antitumor Vaccine

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† Department of Chemistry, Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology (Ministry of Education),Tsinghua University, Beijing 100084, P. R. China
‡ National Engineering Research Center for Carbohydrate Synthesis, Jiangxi Normal University, Nanchang 330022, P. R. China
*E-mail: [email protected]
Cite this: Bioconjugate Chem. 2015, 26, 8, 1439–1442
Publication Date (Web):June 24, 2015
https://doi.org/10.1021/acs.bioconjchem.5b00150
Copyright © 2015 American Chemical Society
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    Abstract

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    Antitumor vaccine, which is promising for tumor therapy, has been extensively studied. Some encouraging results of chemically synthetic vaccine designs based on the tumor-associated antigen mucin 1 have been achieved. However, some shortcomings such as low efficiency and difficult purification restrict their clinical application. To overcome these difficulties, we designed a novel antitumor vaccine of glycopeptide nanoconjugates based on the multilayer self-assembly through the interaction of positive and negative charges. This vaccine formed the spherical structure and effectively activated the macrophage in vitro. Besides, it also induced high titer of antibodies against mucin 1 glycopeptide. The induced antibodies could highly bind to the tumor cells and effectively kill them by activation of the complement dependent cytotoxicity complex. This novel strategy provides a new way for the development of simple and effective antitumor vaccine.

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    Detailed experimental methods, supplementary figures, synthesis, and identification of carbohydrate and peptides. The Supporting Information is available free of charge on the ACS Publications website at DOI: 10.1021/acs.bioconjchem.5b00150.

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