Polymere Selectinliganden als komplexe Glykomimetika: von Selectinbindung bis zur Modifizierung der Makrophagenmigration

6533b862fe1ef96bd12c7597

RESEARCH PRODUCT

Polymere Selectinliganden als komplexe Glykomimetika: von Selectinbindung bis zur Modifizierung der Makrophagenmigration

Lydia Braun Frank Tacke Matthias Bartneck Nicole Mohr Jens Dernedde Figen Beceren-braun Horst Kunz Zhuojun Wu Rudolf Zentel Kai E. Moog Matthias Barz Elisa A. Liehn Twan Lammers

subject

010405 organic chemistry General Medicine 010402 general chemistry 01 natural sciences 0104 chemical sciences

description

Bei neuartigen polymeren Inhibitoren der Zelladhasion wird das Selectin-bindende Tetrasaccharid Sialyl-LewisX (SLeX) multivalent auf einem biokompatiblen Poly(2-hydroxypropyl)methacrylamid (PHPMA) entweder alleine (P1) oder in Kombination mit O-sulfatierten Tyramin-Seitenketten (P2) prasentiert. Zum Vergleich wurden entsprechende polymere Glykomimetika hergestellt, in denen die entscheidenden Fucose-, Galactose und Sialinsaure-Seitenketten statistisch verteilt im PHPMA-Ruckgrat (P3 oder P4 (O-sulfatiertes Tyramin) vorliegen. Alle Polymere haben den gleichen Polymerisationsgrad, da sie vom selben Ausgangspolymer abstammen. Assays fur die Bindung an Selectine, aktivierte Endothelzellen und Makrophagen zeigen, dass PHPMA mit SLeX exzellent an E-, L- und P-Selectine bindet. Das Mimetikum P4 kann allerdings vergleichbare Bindungsaffinitaten bei In-vitro-Messungen erzielen und inhibiert uberraschenderweise signifikant die Migration von Makrophagen; dies eroffnet neue Perspektiven fur die Therapie schwerer Entzundungen.

year	journal	country	edition	language
2016-12-22	Angewandte Chemie

https://doi.org/10.1002/ange.201610395

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