The binding affinities of a series of D-galactose-terminated glycerol
glycosides and oligosaccharides for the asialoglycoprotein receptor is
olated from rabbit liver were determined in vitro using a radiorecepto
r-inhibition assay with I-125-asialoorosomucoid. The relative affiniti
es of the synthetic ligands increased with the number of exposed D-gal
actose termini. Of the compounds examined, 1,2,3-tri-O-beta-lactosylgl
ycerol associated with the greatest affinity (estimated K-d = 7.97 x 1
0(-5) M). Examination of the affinities of the synthetic series indica
ted that both the number and propinquity of the D-galactose termini in
fluenced the strength of the binding interactions.