O-glycan inhibitors of selectin mediated inflammation derived from PSGL-1
US6124267A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Apr 20, 1998 |
| Grant date | Sep 26, 2000 |
| Priority date | — |
| Expiry date | Apr 20, 2018 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K2317/34
- WIPO fieldBiotechnology
- WIPO sectorChemistry
Abstract
Tyrosine sulfate on PSGL-1, particularly at least one of residues 46, 48 and 51, functions in conjunction with sialylated and fucosylated glycans, most preferably Thr-57, to mediate high affinity binding to P-selectin. PSGL-1 O-glycans have been determined to consist of disialylated or neutral forms of the core-2 tetrasaccharide Gal.beta.1.fwdarw.4GlcNAc.beta.1.fwdarw.6(Gal.beta.1.fwdarw.3)GalNAcOH. A minority of the O-glycans are .alpha.1,3 fucosylated that occur as two major species containing the sialyl Lewis x antigen--one species is a disialylated monofucosylated glycan: Fuc.alpha.1 .dwnarw. 3 NeuAc.alpha.2.fwdarw.3Gal.beta.1.fwdarw.4GlcNAc.beta.1 .dwnarw. 6 NeuAc.alpha.2.fwdarw.3Gal.beta.1.fwdarw.3GalNAc-R, and the other is a monosialylated, trifucosylated glycan having a polylactosamine backbone: Fuc.alpha.l .dwnarw. 3 NeuAc.alpha.2.fwdarw.3Gal.beta.1.fwdarw.4GlcNAc.beta.1.fwdarw.3Gal.beta.1. fwdarw. Fuc.alpha.l Fuc.alpha.l .dwnarw. .dwnarw. 3 3 4GlcNAc.beta.1.fwdarw.3Gal.beta.1.fwdarw.4GlcNAc.beta.1 .dwnarw. 6 Gal.beta.1.fwdarw.3GalNAc-R wherein R=H, OH, another sugar or an aglycone such as an amino acid, peptide, or polypeptide. The O-glycans defined herewith can be used t…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.