|
|||||
|
|
Design,synthesis and evaluation of monovalent ligands for the asialoglycoprotein receptor (ASGP-R) |
|
| Authors: | Daniela Stokmaier Oleg Khorev Brian Cutting Rita Born Daniel Ricklin Thomas OG Ernst Fabienne Böni Kathrin Schwingruber Martin Gentner Matthias Wittwer Morena Spreafico Angelo Vedani Said Rabbani Oliver Schwardt Beat Ernst |
| Institution: | Institute of Molecular Pharmacy, Pharmacenter, University of Basel, Klingelbergstrasse 50, CH-4056 Basel, Switzerland |
| 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: | |
| 本文献已被 ScienceDirect 等数据库收录！ | |