1196658-75-9Relevant academic research and scientific papers
Design, synthesis and evaluation of monovalent ligands for the asialoglycoprotein receptor (ASGP-R)
Stokmaier, Daniela,Khorev, Oleg,Cutting, Brian,Born, Rita,Ricklin, Daniel,Ernst, Thomas O.G.,Boeni, Fabienne,Schwingruber, Kathrin,Gentner, Martin,Wittwer, Matthias,Spreafico, Morena,Vedani, Angelo,Rabbani, Said,Schwardt, Oliver,Ernst, Beat
experimental part, p. 7254 - 7264 (2010/03/24)
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.
