Studies on selectin blocker. 1. Structure-activity relationships of sialyl Lewis X analogs.
As part of our studies of selectin blockers, we prepared 1-deoxy-3'-O-sulfo LeX analogs (1-3), 1-deoxy-3'-O-phosphono LeX analogs (4), and 1-deoxy sLeX analogs (5-7), and examined their inhibitory activities against natural ligand (sLeX) binding to E-selectin, P-selectin, and L-selectin. The 1-deoxy sLeX 5 was up to 20 times more potent an inhibitor than the sLeX tetrasaccharide toward P- and L-selectin binding. This indicates that the modification of the 1 or 2 position of sLeX is useful in the design of a more potent selectin blocker.
Ohmoto
H
H
Department of Biology, Institute of Cancer Research Laboratories, Osaka, Japan.
Nakamura
K
K
Inoue
T
T
Kondo
N
N
Inoue
Y
Y
Yoshino
K
K
Kondo
H
H
Ishida
H
H
Kiso
M
M
Hasegawa
A
A
D019040:E-Selectin / Q000378:metabolism*; D019041:L-Selectin / Q000378:metabolism*; D016256:Lewis X Antigen / Q000494:pharmacology*; D008968:Molecular Conformation; D019007:P-Selectin / Q000378:metabolism*; D013329:Structure-Activity Relationship
D019040:E-Selectin; D016256:Lewis X Antigen; D019007:P-Selectin; D019041:L-Selectin