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

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Title:	Multivalent Design of Apoptosis-Inducing Bid-BH3 Peptide-Oligosaccharides Boosts the Intracellular Activity at Identical Overall Peptide Concentrations
Author(s):	Richter, M.; Chakrabarti, A.; Ruttekolk, I.R.R. ; Wiesner, B.; Beyermann, M.; Brock, R.E. ; Rademann, J.
Publication year:	2012
Source:	Chemistry : a European Journal, vol. 18, iss. 52, (2012), pp. 16708-16715
ISSN:	0947-6539
DOI:	https://doi.org/10.1002/chem.201202276
Publication type:	Article / Letter to editor
Please use this identifier to cite or link to this item : http://hdl.handle.net/2066/108756
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Subject:	NCMLS 2: Immune Regulation
Organization:	Biochemistry (UMC)
Journal title:	Chemistry : a European Journal
Volume:	vol. 18
Issue:	iss. 52
Page start:	p. 16708
Page end:	p. 16715
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.