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US 5,965,544 AGranted
Synthetic multivalent sLe.sup.x containing polylactosamines and methods for use
AssigneeGlycim Oy
InventorsOssi Renkonen, Risto Renkonen
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AssigneeGlycim Oy
InventorsOssi Renkonen, Risto Renkonen
Estimating the term…
The present invention is directed to novel compositions and their use in the treatment of inflammatory responses. Specifically, the invention is directed to novel synthetic oligosaccharide constructs, especially multiple sLe.sup.x decorated poly-N-acetyllactosamines and their use to block lymphocyte binding to correspondent oligosaccharides on the endothelial surface, and thus reduce or otherwise ameliorate an undesired inflammatory response and other disease states characterized by lymphocyte binding. Furthermore the invention is directed to the use of the novel saccharides to block bacterial adherence to endothelium and thus prevent and/or treat bacterial infections. A further use of the present invention lies in the field of cancer treatment where metastasis of sLe.sup.x -positive tumor cells is inhibited by these glycans.
A synthetic sLe.sup.x oligosaccharide, essentially free of contaminants, having a polylactosamine backbone (LacNAc).sub.n, wherein n.gtoreq.1 and having interresidual links that are .beta.1-3' and/or .beta.1-6', to which at least two NeuNAc.alpha.2-3Gal.beta.1-4(Fuc1-3) GlcNAc epitopes are linked by .beta.1-3' and/or .beta.1-6' bonds.
A method for synthesizing sLe.sup.x oligosaccharides having a branched polylactosamine backbone which utilizes N-acetyllactosamine, the hexasaccharide Gal.beta.1-4GlcNAc.beta.1-6(Gal.beta.1-4GlcNAc.beta.1-3)Gal.beta.1-4GalNAc , and the tetradecasaccharide Gal.beta.1-3GlcNAc.beta.1-6(Gal.beta.1-4GlcNAc.beta.1-3)Gal.beta.1-4GlcNAc .beta.1-6[Gal.beta.1-4GlcNAc.beta.1-6(GalB1-4GlcNAc.beta.1-3)Gal.beta.1-4Gl cNAc.beta.1-3]Gal.beta.1-4GlcNAc, as acceptors for mono-, di-, and tetravalent sLe.sup.x saccharides, respectively, said method comprising:
A method for synthesizing a tetravalent sLe.sup.x 22-meric oligosaccharide having a linear polylactosamine backbone from an octameric polylactosamine having the structure LacNAc.beta.1-3'(GlcNAc.beta.1-6 ')LacNAc.beta.1-3'(GlcNAc.beta.1-6')LacNAc, where LacNAc is the disaccharide Gal.beta.1-4GlcNAc, said method comprising the steps of:
Dependencies are inferred from the claim text.