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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Chakrabarti, Alokta Beyermann, Michael Richter, Martin Brock, Roland Rademann, Jörg Wiesner, Burkhard Ruttekolk, Ivo R. |
| Description | Author Affiliation: Richter M ( Leibniz Institut für Molekulare Pharmakologie, Berlin, Germany.) |
| 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. |
| ISSN | 09476539 |
| e-ISSN | 15213765 |
| Journal | Chemistry - A European Journal |
| Issue Number | 52 |
| Volume Number | 18 |
| Language | English |
| Publisher | Wiley-VCH;ChemPubSoc Europe |
| Publisher Date | 2012-12-21 |
| Publisher Place | Germany |
| Access Restriction | Open |
| Subject Keyword | Apoptosis Drug Effects BH3 Interacting Domain Death Agonist Protein Chemistry Dextrans Peptide Fragments Proto-Oncogene Proteins Cell Membrane Metabolism Chemical Synthesis Pharmacology Dose-Response Relationship, Drug Electroporation HeLa Cells Jurkat Cells Maleimides Microscopy, Confocal Oligopeptides Administration & Dosage Spectrometry, Fluorescence Research Support, Non-U.S. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Organic Chemistry Catalysis |
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