Binding of D-galactose-terminated ligands to rabbit asialoglycoprotein receptor.
The binding affinities of a series of D-galactose-terminated glycerol glycosides and oligosaccharides for the asialoglycoprotein receptor isolated from rabbit liver were determined in vitro using a radioreceptor-inhibition assay with 125I-asialoorosomucoid. The relative affinities of the synthetic ligands increased with the number of exposed D-galactose termini. Of the compounds examined, 1,2,3-tri-O-beta-lactosylglycerol associated with the greatest affinity (estimated Kd = 7.97 x 10(-5) M). Examination of the affinities of the synthetic series indicated that both the number and propinquity of the D-galactose termini influenced the strength of the binding interactions.
Krebs
A
A
Department of Medicine, Queen's University, Kingston, Ontario, Canada.
Depew
W T
WT
Szarek
W A
WA
Hay
G W
GW
Hronowski
L J
LJ
D000818:Animals; D037263:Asialoglycoprotein Receptor; D001212:Asialoglycoproteins / Q000378:metabolism; D001667:Binding, Competitive; D002236:Carbohydrate Conformation; D002240:Carbohydrate Sequence; D005690:Galactose; D007457:Iodine Radioisotopes; D007700:Kinetics; D008024:Ligands; D008099:Liver / Q000378:metabolism*; D008969:Molecular Sequence Data; D009844:Oligosaccharides / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D009961:Orosomucoid / Q000031:analogs & derivatives / Q000378:metabolism; D011817:Rabbits; D011956:Receptors, Cell Surface / Q000187:drug effects / Q000302:isolation & purification / Q000378:metabolism*
D037263:Asialoglycoprotein Receptor; D001212:Asialoglycoproteins; D007457:Iodine Radioisotopes; D008024:Ligands; D009844:Oligosaccharides; D009961:Orosomucoid; D011956:Receptors, Cell Surface; C017030:asialoorosomucoid; D005690:Galactose