title: Studies on selectin blocker. 1. Structure-activity relationships of sialyl Lewis X analogs.
abstract: 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.
authors.affiliation: Department of Biology, Institute of Cancer Research Laboratories, Osaka, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Ohmoto
authors.forename: K
authors.initials: K
authors.lastname: Nakamura
authors.forename: T
authors.initials: T
authors.lastname: Inoue
authors.forename: N
authors.initials: N
authors.lastname: Kondo
authors.forename: Y
authors.initials: Y
authors.lastname: Inoue
authors.forename: K
authors.initials: K
authors.lastname: Yoshino
authors.forename: H
authors.initials: H
authors.lastname: Kondo
authors.forename: H
authors.initials: H
authors.lastname: Ishida
authors.forename: M
authors.initials: M
authors.lastname: Kiso
authors.forename: A
authors.initials: A
authors.lastname: Hasegawa
mesh_terms: 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
chemical_list: D019040:E-Selectin; D016256:Lewis X Antigen; D019007:P-Selectin; D019041:L-Selectin