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- Title
Multivalent Design of Apoptosis-Inducing Bid-BH3 Peptide-Oligosaccharides Boosts the Intracellular Activity at Identical Overall Peptide Concentrations.
- Authors
Richter, Martin; Chakrabarti, Alokta; Ruttekolk, Ivo R.; Wiesner, Burkhard; Beyermann, Michael; Brock, Roland; Rademann, Jörg
- Abstract
Multivalent peptide-oligosaccharide 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.
- Publication
Chemistry - A European Journal, 2012, Vol 18, Issue 52, p16708
- ISSN
0947-6539
- Publication type
Article
- DOI
10.1002/chem.201202276