摘要:
Disclosed are methods for screening compound libraries using frontal chromatography in combination with mass spectrometry to identify and rank those members of the library that bind to a target receptor. Methods are also disclosed which permit a compound library to be rapidly screened to determine if any member of the library has an affinity for the target receptor as measured by a pre-selected indicator compound.
摘要:
The present invention provides an improved method of preparing a 4,7-di-O-alkyl chromogenic ketoside of N-acetylneuraminic acid (Neu5Ac) for use in detecting influenza virus types A and B. The ketosides are substrates that are selectively cleaved by a neuraminidase on influenza virus, but not be neuraminidases found on other viruses or on bacteria. The synthesis is efficient and provides large quantities of the ketoside for commercial development. The synthesis includes a step of alkylating the 4- and 7-hydroxyl groups of a protected alkyl ester alkyl ketoside derivative of Neu5Ac by a process that comprises contacting the derivative with a composition comprising an alkyl halide to form a 4,7-di-O-alkyl protected alkyl ester alkyl ketoside derivative of Neu5Ac. The synthesis alternatively includes protecting the 8- and 9-hydroxyl groups of an alkyl ester alkyl ketoside derivative of Neu5Ac by forming an 8,9-epoxide protected alkyl ester alkyl ketoside derivative of Neu5Ac.
摘要:
Disclosed are novel oligosaccharide glycosides having mammalian immunosuppressive and tolerogenic properties, pharmaceutical compositions containing such oligosaccharide glycosides and to methods of using such oligosaccharide glycosides to modulate cell-mediated immune responses in a mammal.
摘要:
Glycopeptides having the following structure are described: ##STR1## wherein: X.sub.1 is hydrogen, an acetyl group, an acyl group or amino acid; R is .alpha.-L-fucose, .alpha.-D-fucose, .beta.-L-fucose or .beta.-D-fucose, wherein R is O-glucosidically linked to A.sub.1 ; A.sub.1 is serine, threonine, tyrosine, hydroxyproline, asparagine, glutamine, homeoserine and hydroxylysine; A.sub.2 is a glycine, an L-amino acid, a D-amino acid or a modified amino acid; A.sub.3 is L or D aspartic acid, glycine or glutamic acid; and X.sub.2 is a hydroxyl, an amine or an amino acid.
摘要:
Synthetic glycosaminosyl transferase-V acceptors and inhibitors are disclosed. Minimal trisaccharide inhibitors and acceptors specific for GnT-V, which is associated with the ability of cells to metastasize are useful, in diagnosis and treatment of conditions characterized by metastatic cells.
摘要:
The present invention relates to a novel method for analysing carbohydrates. The invention is in particular useful in detecting a terminal monosaccharide which may be released from a glycosylated substrate for example using an exoglucosidase. After relase from the glycosylated substrate the terminal monosaccharide may be captured on a solid support, incubated with a boronate detection agent and detected by aid of the boronate detection agent. The methods of the invention are useful for a variety of purposes including sequencing of carbohydrates, wherein exoglycosidases with predetermined specificity are employed for the release.
摘要:
Disclosed are methods for screening compound libraries using frontal chromatography in combination with mass spectrometry to identify and rank those members of the library that bind to a target receptor. Methods are also disclosed which permit a compound library to be rapidly screened to determine if any member of the library has an affinity for the target receptor as measured by a pre-selected indicator compound.
摘要:
Disclosed are methods for screening compound libraries using frontal chromatography in combination with mass spectrometry to identify and rank those members of the library that bind to a target receptor. Methods are also disclosed which permit a compound library to be rapidly screened to determine if any members of the library have a higher affinity for the target receptor relative to a pre-selected indicator compound.
摘要:
Disclosed are novel solid support matrices having a toxin-binding oligosaccharide covalently attached to a solid support through a linking arm which has at least 8 atoms separating the oligosaccharide from the solid support. The disclosed solid support matrices are useful for neutralizing toxins from disease-causing microrganisms.
摘要:
Disclosed are methods for synthesizing very large collections of diverse thiosaccaride derivatives optionally attached to a solid support. Also disclosed are libraries of diverse thiosaccaride derviatives.