| Literature DB >> 19762243 |
Daniela Stokmaier1, Oleg Khorev, Brian Cutting, Rita Born, Daniel Ricklin, Thomas O G Ernst, Fabienne Böni, Kathrin Schwingruber, Martin Gentner, Matthias Wittwer, Morena Spreafico, Angelo Vedani, Said Rabbani, Oliver Schwardt, Beat Ernst.
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.Entities:
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Year: 2009 PMID： 19762243 DOI： 10.1016/j.bmc.2009.08.049
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641