期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 18, 期 52, 页码 16708-16715出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201202276
关键词
apoptosis; cancer; oligosaccharides; peptides; polymers; protein-protein interactions
资金
- DFG [Ra895-4-6, SFB 765, FOR 806, BR2443-5]
- Fonds der Chemischen Industrie
Multivalent peptideoligosaccharide conjugates were prepared and used to investigate the multivalency effect concerning the activity of Bid-BH3 peptides in live cells. Dextran oligosaccharides were carboxyethylated selectively in the 2-position of the carbohydrate units and activated for the ligation of N-terminally cysteinylated peptides. Ligation through maleimide coupling was found to be superior to the native chemical ligation protocol. Monomeric Bid-BH3 peptides were virtually inactive, whereas pentameric peptide conjugates induced apoptosis up to 20-fold stronger at identical peptide concentrations. Comparison of lowly multivalent and highly multivalent peptide dextrans proved a multivalency effect in life cells which was specific for the BH3 peptide sequence.
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