ISSN:
1573-4986
Keywords:
HepG2 cells
;
hepatocytes
;
asialoglycoprotein receptor
;
cluster galactosyl glycosides
;
targeting
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Abstract We have synthesized bi- and tri-antennary galactose ligands by coupling 1-thio-β-d-galactose derivatives to the α- and ε-amino groups ofl-lysine andl-lysyl-l-lysine via highly flexible hydrophilic spacer arms that allow variation of their intergalactose distances. The interaction of these ligands with the Gal/GalNAc receptor of HepG2 cells showed a binding affinity that was: (i) in agreement with the clustering effect known to occur with more complex oligomeric structures, i.e. tri- 〉 bi-antennary; ii) dependent on the intergalactose distances (optimal interactions were observed for the tri-antennary structures with distances 〉2 nm). These ligands, that can be easily conjugated to bioactive (macro) molecule carrier systems, could be useful for their targeting to hepatocytes.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00731330
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