Synthesis and Evaluation of Nonsulfated and Sulfated Glycopolymers as L- and P-selectin Inhibitors

Selectins are carbohydrate-binding proteins and responsible for leukocyte extravasation in inflammation. Here we demonstrate the potential of synthetic glycocompounds as inhibitors for the selectin-ligand interaction. Pentaerythritol derivatives showed distinct selectin-binding properties with IC 50...

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Published inJournal of carbohydrate chemistry Vol. 30; no. 4-6; pp. 347 - 360
Main Authors Dernedde, Jens, Papp, Ilona, Enders, Sven, Wedepohl, Stefanie, Paulus, Florian, Haag, Rainer
Format Journal Article
LanguageEnglish
Published Philadelphia Taylor & Francis Group 01.05.2011
Taylor & Francis Ltd
Subjects
Carbohydrate ligands
Carbohydrates
Hyperbranched polyglycerol
Selectin inhibitors
Sulfation
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Summary:Selectins are carbohydrate-binding proteins and responsible for leukocyte extravasation in inflammation. Here we demonstrate the potential of synthetic glycocompounds as inhibitors for the selectin-ligand interaction. Pentaerythritol derivatives showed distinct selectin-binding properties with IC 50 values up to 1.5 μM. Multivalent hyperbranched polyglycerol (hPG) derivatives did not lead to a substantial increase in inhibition, but a more than 1000-fold enhancement was realized when sulfated glyco-hPGs were tested. IC 50 values in the high picomolar to low nanomolar range were obtained for selectin inhibition, which highlights the relevance of sulfate groups that seem to dominate the binding mode.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
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ISSN:0732-8303
1532-2327
DOI:10.1080/07328303.2011.608227