Trivalent, Gal/GalNAc-containing ligands designed for the asialoglycoprotein receptor

O Khorev, D Stokmaier, O Schwardt, B Cutting… - Bioorganic & medicinal …, 2008 - Elsevier
A series of novel, fluorescent ligands designed to bind with high affinity and specificity to the
asialoglycoprotein receptor (ASGP-R) has been synthesized and tested on human liver …

Efficient liver targeting by polyvalent display of a compact ligand for the asialoglycoprotein receptor

CA Sanhueza, MM Baksh, B Thuma… - Journal of the …, 2017 - ACS Publications
A compact and stable bicyclic bridged ketal was developed as a ligand for the
asialoglycoprotein receptor (ASGPR). This compound showed excellent ligand efficiency …

Design, synthesis and evaluation of monovalent ligands for the asialoglycoprotein receptor (ASGP-R)

D Stokmaier, O Khorev, B Cutting, R Born… - Bioorganic & medicinal …, 2009 - Elsevier
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 …

Glycomimetic ligands for the human asialoglycoprotein receptor

SK Mamidyala, S Dutta, BA Chrunyk… - Journal of the …, 2012 - ACS Publications
The asialoglycoprotein receptor (ASGPR) is a high-capacity galactose-binding receptor
expressed on hepatocytes that binds its native substrates with low affinity. More potent …

Ligands of the asialoglycoprotein receptor for targeted gene delivery, part 1: Synthesis of and binding studies with biotinylated cluster glycosides containing N …

U Westerlind, J Westman, E Törnquist, CIE Smith… - Glycoconjugate …, 2004 - Springer
In order to develop the non-viral Bioplex vector system for targeted delivery of genes to
hepatocytes, we have evaluated the structure-function relationship for a number of synthetic …

Well-defined multivalent ligands for hepatocytes targeting via asialoglycoprotein receptor

X Huang, JC Leroux, B Castagner - Bioconjugate chemistry, 2017 - ACS Publications
Targeted delivery of therapeutic agents to hepatocytes is a particularly attractive strategy for
the treatment of hepatocellular carcinoma and other liver diseases. The asialoglycoprotein …

[HTML][HTML] Determination of the upper size limit for uptake and processing of ligands by the asialoglycoprotein receptor on hepatocytesin vitro and in vivo

PCN Rensen, LAJM Sliedregt, M Ferns… - Journal of biological …, 2001 - ASBMB
The asialoglycoprotein receptor (ASGPr) on hepatocytes plays a role in the clearance of
desialylated proteins from the serum. Although its sugar preference (N-acetylgalactosamine …

Stepwise synthesis of a GalNAc‐containing cluster glycoside ligand of the asialoglycoprotein receptor

MA Findeis - International journal of peptide and protein …, 1994 - Wiley Online Library
A series of peptidylglycoside derivatives, including the tris (GalNAc‐aminohexyl) glycoside
of tyrosyl (glutamyl)‐glutamate (1) which is known to have sub‐nanomolar affinity for the …

Targeted delivery of DNA using YEE (GalNAcAH) 3, a synthetic glycopeptide ligand for the asialoglycoprotein receptor

JR Merwin, GS Noell, WL Thomas… - Bioconjugate …, 1994 - ACS Publications
In vivogene therapy shows promise as a treatment for both genetic and acquired disorders.
The hepatic asialoglycoprotein receptor (ASGPr) binds asialoorosomucoid—polylysine …

Solid-phase synthesis of lysine-based cluster galactosides with high affinity for the asialoglycoprotein receptor

ARPM Valentijn, GA van der Marel, LAJM Sliedregt… - Tetrahedron, 1997 - Elsevier
Structurally well defined di-and tri-antennary lysine-based galactose-and N-
acetylgalactosamine-containing ligands for the hepatic asialoglycoprotein receptor (ASGP …