Multivalent Design of Apoptosis-Inducing Bid-BH3 Peptide–Oligosaccharides Boosts the Intracellular Activity at Identical Overall Peptide Concentrations

M. Richter, A. Chakrabarti, I. R. Ruttekolk, B. Wiesner, M. Beyermann, R. Brock, J. Rademann – 2012

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.

Titel
Multivalent Design of Apoptosis-Inducing Bid-BH3 Peptide–Oligosaccharides Boosts the Intracellular Activity at Identical Overall Peptide Concentrations
Verfasser
M. Richter, A. Chakrabarti, I. R. Ruttekolk, B. Wiesner, M. Beyermann, R. Brock, J. Rademann
Datum
2012
Kennung
DOI: 10.1002/chem.201202276
Quelle/n
Zitierweise
Chem. Eur. J. 2012, 18, 16708-16715
Art
Text
dfg_logo