Author/Authors :
Daniela Stokmaier، نويسنده , , Oleg Khorev، نويسنده , , Brian Cutting، نويسنده , , Rita Born، نويسنده , , Daniel Ricklin، نويسنده , , Thomas O.G. Ernst، نويسنده , , Fabienne B?ni، نويسنده , , Kathrin Schwingruber، نويسنده , , Martin Gentner، نويسنده , , Matthias Wittwer، نويسنده , , Morena Spreafico، نويسنده , , Angelo Vedani، نويسنده , , Said Rabbani، نويسنده , , Oliver Schwardt، نويسنده , , Beat Ernst، نويسنده ,
Abstract :
A series of novel aryl-substituted triazolyl d-galactosamine derivatives was synthesized as ligands for the carbohydrate recognition domain of the major subunit H1 (H1-CRD) of the human asialoglycoprotein receptor (ASGP-R). The compounds were biologically evaluated with a newly developed competitive binding assay, surface plasmon resonance and by a competitive NMR binding experiment. With compound 1b, a new ligand with a twofold improved affinity to the best so far known d-GalNAc was identified. This small, drug-like ligand can be used as targeting device for drug delivery to hepatocytes.
Keywords :
Asialoglycoprotein receptor (ASGP-R) , Competitive NMR binding experiments , Triazolyl d-galactosamine derivatives , Competitive binding assay
