Neose Technologies, Inc.

Cytel Corporation

Schering Corporation

The University of British Columbia

La Jolla Pharmaceutical Company

Shawn Defrees

Robert J Bayer

Murray Ratcliffe

Andrew William Stamford

Samuel Chackalamannil

Brian Alexander McKittrick

Stephen G Withers

Karl Frank Johnson

Michael F Czarniecki

Mark Vaughan

Shin Chung

The present invention relates to a novel endoglycoceramidase whose hydrolytic activity has been substantially reduced or eliminated, such that the enzyme is useful for synthesis of glycolipids from a monosaccharide or oligosaccharide and a ceramide. More specifically, the endoglycoceramidase is a mutant version of a naturally occurring endoglycoceramidase, preferably comprising a mutation within the active site or the nucleophilic site of the enzyme and more preferably comprising a substitution mutation of the Glu residue within the active site or the nucleophilic site. Also disclosed are a method for generating the mutant endoglycoceramidase and a method for enzymatically synthesizing glycolipids using this mutant enzyme.

Mutant endoglycoceramidases with enhanced synthetic activity

The invention provides methods for purifying carbohydrates, including oligosaccharides, nucleotide sugars, and related compounds, by use of ultrafiltration, nanofiltration and/or reverse osmosis. The carbohydrates are purified away from undesired contaminants such as compounds present in reaction mixtures following enzymatic synthesis or degradation of oligosaccharides.

Carbohydrate purification using ultrafiltration, reverse osmosis and nanofiltration

This invention provides methods for practical in vitro synthesis of gangliosides and other glycolipids. The synthetic methods typically involve enzymatic synthesis, or a combination of enzymatic and chemical synthesis. One or more of the enzymatic steps is preferably carried out in the presence of an organic solvent.

Enzymatic synthesis of gangliosides

The present invention provides improved methods for the preparation of sialyl galactosides. The methods use sialyl transferase cycle in which the reaction conditions are optimized to provide increased yields.

Enzymatic synthesis of oligosaccharides

The present invention provides improved methods for the formation of glycosidic linkages. These methods are useful for the preparation of compounds of formula:

Enzymatic synthesis of glycosidic linkages

Phosphinic acid derivatives of the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene;

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San Marcos, CA, United States of America

Shawn Defrees