期刊
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
卷 2011, 期 20-21, 页码 3685-3689出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201100304
关键词
Carbohydrates; Glycosylation; Glycopeptides; Antitumor agents; Solid-phase synthesis
资金
- National Natural Science Foundation of China [20825206, 21028004]
- Sino-German Center for Research Promotion [GZ561]
The tumor-associated mucin MUC1 over-expressed in most epithelial tumor tissues is considered a promising target for immunotherapy. The extracellular part of MUC1 contains a domain of numerous tandem repeats of the amino acid sequence HGVTSAPDTRPAPGSTAPPA, including five potential O-glycosylation sites. In this study, T9 and S15 have been chosen as the positions of glycosylation. The glycopeptides N-terminally equipped with a triethylene glycol spacer were synthesized by microwave-assisted Fmoc solid-phase peptide synthesis. After detachment from the resin and deprotection, the MUC1 glycopeptides were conjugated to bovine serum albumin (BSA). To evaluate the immunological properties, balb/c mice were immunized with these BSA vaccines.
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