Patent application number | Description | Published |
20080206808 | GALACTOSYL NUCLEOTIDE SUGAR - The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide. | 08-28-2008 |
20080207487 | MANUFACTURING PROCESS FOR THE PRODUCTION OF POLYPEPTIDES EXPRESSED IN INSECT CELL-LINES - The present invention provides a manufacturing method for polypeptides that are produced in insect cells using a baculoviral expression system. In one example, the insect cell culture is supplemented with a lipid mixture immediately prior to infection (e.g., one hour prior to infection). The polypeptides are isolated from the insect cell culture using a method that employs anion exchange or mixed-mode chromatography early in the purification process. This process step is useful to remove insect-cell derived endoglycanases and proteases and thus reduces the loss of desired polypeptide due to enzymatic degradation. In another example, mixed-mode chromatography is combined with dye-ligand affinity chromatography in a continuous-flow manner to allow for rapid processing of the insect-cell culture liquid and capture of the polypeptide. In yet another example, a polypeptide is isolated from an insect cell culture liquid using a process that combines hollow fiber filtration, mixed-mode chromatography and dye-ligand affinity in a single unit operation producing a polypeptide solution that is essentially free of endoglycanase and proteolytic activities. In a further example, the isolated polypeptides are glycopeptides having an insect specific glycosylation pattern, which are optionally conjugated to a modifying group, such as a polymer (e.g., PEG) using a glycosyltransferase and a modified nucleotide sugar. | 08-28-2008 |
20080242607 | GLYCOSYLATION OF PEPTIDES VIA O-LINKED GLYCOSYLATION SEQUENCES - The present invention provides sequon polypeptides with an amino acid sequence including one or more exogenous O-linked glycosylation sequence of the invention. In addition, the present invention provides methods of making polypeptide conjugates as well as methods of using such conjugates and their pharmaceutical compositions. The invention further provides libraries of sequon polypeptides, wherein each member of such library includes at least one exogenous O-linked glycosylation sequence of the invention. Also provided are methods of making and using such libraries. | 10-02-2008 |
20080242846 | O-LINKED GLYCOSYLATION OF PEPTIDES - The present invention provides polypeptides that include an O-linked glycosylation site that is not present in the wild-type peptide. The polypeptides of the invention include glycoconjugates in which a species such as a water-soluble polymer, a therapeutic agent of a biomolecule is covalently linked through an intact O-linked glycosyl residue to the polypeptide. Also provided are methods of making the peptides of the invention and methods, pharmaceutical compositions containing the peptides and methods of treating, ameliorating or preventing diseased in mammals by administering an amount of a peptide of the invention sufficient to achieve the desired response. | 10-02-2008 |
20080248959 | GLYCOSYLATION OF PEPTIDES VIA O-LINKED GLYCOSYLATION SEQUENCES - The present invention provides sequon polypeptides with an amino acid sequence including one or more exogenous O-linked glycosylation sequence of the invention. In addition, the present invention provides methods of making polypeptide conjugates as well as methods of using such conjugates and their pharmaceutical compositions. The invention further provides libraries of sequon polypeptides, wherein each member of such library includes at least one exogenous O-linked glycosylation sequence of the invention. Also provided are methods of making and using such libraries. | 10-09-2008 |
20080253992 | METHODS FOR THE PURIFICATION OF POLYPEPTIDE CONJUGATES - The present invention provides processes for the manufacturing of polypeptide conjugates. In particular, the invention provides methods for the purification of polypeptide conjugates, which include at least one polymeric modifying groups, such as a poly(alkylene oxide) moiety. Exemplary poly(alkylene oxide) moieties include poly(ethylene glycol) (PEG) and poly(propylene glycol). In an exemplary process, hydrophobic interaction chromatography (HIC) is used to resolve different glycoforms of glycoPEGylated polypeptides. | 10-16-2008 |
20080255026 | Glycopegylated Factor Ix - The present invention provides conjugates between Factor Ix and PEG moieties. The conjugates are linked via a glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. Conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates. | 10-16-2008 |
20080255040 | GLYCOSYLATION OF PEPTIDES VIA O-LINKED GLYCOSYLATION SEQUENCES - The present invention provides sequon polypeptides with an amino acid sequence including one or more exogenous O-linked glycosylation sequence of the invention. In addition, the present invention provides methods of making polypeptide conjugates as well as methods of using such conjugates and their pharmaceutical compositions. The invention further provides libraries of sequon polypeptides, wherein each member of such library includes at least one exogenous O-linked glycosylation sequence of the invention. Also provided are methods of making and using such libraries. | 10-16-2008 |
20080274958 | GLYCOSYLATION OF PEPTIDES VIA O-LINKED GLYCOSYLATION SEQUENCES - The present invention provides sequon polypeptides with an amino acid sequence including one or more exogenous O-linked glycosylation sequence of the invention. In addition, the present invention provides methods of making polypeptide conjugates as well as methods of using such conjugates and their pharmaceutical compositions. The invention further provides libraries of sequon polypeptides, wherein each member of such library includes at least one exogenous O-linked glycosylation sequence of the invention. Also provided are methods of making and using such libraries. | 11-06-2008 |
20080280818 | GLYCOSYLATION OF PEPTIDES VIA O-LINKED GLYCOSYLATION SEQUENCES - The present invention provides sequon polypeptides with an amino acid sequence including one or more exogenous O-linked glycosylation sequence of the invention. In addition, the present invention provides methods of making polypeptide conjugates as well as methods of using such conjugates and their pharmaceutical compositions. The invention further provides libraries of sequon polypeptides, wherein each member of such library includes at least one exogenous O-linked glycosylation sequence of the invention. Also provided are methods of making and using such libraries. | 11-13-2008 |
20080300173 | Branched Peg Remodeling and Glycosylation of Glucagon-Like Peptides-1 [Glp-1] - The present invention provides polypeptides that include an O-linked glycoconjugate in which a species such as a water-soluble polymer, a therapeutic agent of a biomolecule is covalently linked through an intact O-linked glycosyl residue to the polypeptide. The polypeptides of the invention include wild-type peptides and mutant peptides that include an O-linked glycosylation site that is not present in the wild-type peptide. Also provided are methods of making the peptides of the invention and methods, pharmaceutical compositions containing the peptides and methods of treating, ameliorating or preventing diseased in mammals by administering an amount of a peptide of the invention sufficient to achieve the desired response. | 12-04-2008 |
20080300175 | Glycopegylated erythropoietin - The present invention provides conjugates between erythropoietin and PEG moieties. The conjugates are linked via an intact glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates. | 12-04-2008 |
20080305991 | Factor IX: remodeling and glycoconjugation of factor IX - The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide. | 12-11-2008 |
20080305992 | Glycopegylated erythropoietin - The present invention provides conjugates between erythropoietin and PEG moieties. The conjugates are linked via an intact glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates. | 12-11-2008 |
20080318850 | Glycopegylated Factor Ix - The present invention provides conjugates between Factor IX and PEG moieties. The conjugates are linked via an intact glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates. | 12-25-2008 |
20080319183 | Branched Polymeric Sugars and Nucleotides Thereof - The present invention provides sugars, nucleotide sugars, activated sugars that include one or more polymeric modifying moiety within their structure. The invention is exemplified by reference to linear and branched polymers, such as the water-soluble polymer poly(ethylene glycol). | 12-25-2008 |
20090028822 | Glycopegylated Interferon Alpha - The present invention provides IFN-α conjugates including IFN-α peptides and modifying groups such as PEG moieties. The IFN-α peptide and modifying group are linked via an intact glycosyl linking group interposed between and covalently attached to the IFN-α peptide and the modifying group. The IFN-α conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar onto an amino acid or a glycosyl residue on the IFN-α peptide. Also provided are methods for preparing the IFN-α conjugates, methods for treating various disease conditions with the IFN-α conjugates, and pharmaceutical formulations including the IFN-α conjugates. | 01-29-2009 |
20090047710 | ST3Gal-1/ST6GalNAc-1 Chimeras - The present invention features compositions and methods related to increasing the solubility and enzymatic activity of GalNAc-α-2,6-sialyltransferase I (STÌGalNAcI) proteins expressed in prokaryotic host cells. Methods for increasing the solubility of STÌGalNAcI polypeptides include modifying cysteine residues, modifying N-linked glycosylation sites, deleting polypeptide regions, and constructing chimeric polypeptides comprising sequences from a STÌGalNAcI and another protein, for example, a Gal-β-1,3GalNAc-α-2,3-sialyltransferase (ST3GalI) and a STÌGalNAcI. The invention also features nucleic acids encoding such improved polypeptides, as well as vectors, host cells, expression systems, and methods of expressing and using such polypeptides. | 02-19-2009 |
20090048440 | Nucleotide Sugar Purification Using Membranes - The invention provides methods of removing contaminants from a mixture of a desired product and contaminants by pH adjustments and molecular weight cut-offs. The contaminants include phosphate groups, magnesium sulfate, sodium pyruvate and tetrasodium pyrophosphate groups. The desired product includes nucleotide sugars, glycolipids, LnNT, sialyl lactose, and salts. | 02-19-2009 |
20090053167 | C-, S- and N-glycosylation of peptides - The present invention provides polypeptide conjugates wherein a modifying group such as a water-soluble polymer, a therapeutic agent or a biomolecule is covalently linked to the polypeptide through a glycosyl linking group. In one embodiment, the polypeptide includes a glycosylation consensus sequence, wherein glycosylation occurs at an aromatic amino acid residue, such as the C-2 or the N-1 position of a tryptophan side chain. Exemplary polypeptides of the invention are those in which the glycosylation consensus sequence has been introduced into the amino acid sequence of the polypeptide by mutation. In another aspect the invention provides polypeptide conjugates wherein the modifying group is covalently linked to the polypeptide via a glycosyl mimetic linking group. Also provided are methods of making and using as well as pharmaceutical compositions containing the polypeptide conjugates of the invention. Further provided are methods of treating, ameliorating or preventing diseases in mammals by administering an amount of a polypeptide conjugate of the invention sufficient to achieve the desired response. | 02-26-2009 |
20090054623 | Lipo-Conjugation of Peptides - The present invention provides peptide conjugates that are formed between a modified lipid and a glycosyl residue and/or an amino acid residue on a peptide. The modified lipid includes a modifying group and a lipid linking group. Exemplary lipid linking groups include myristoyl, palmitoyl, and isoprenyl moieties. | 02-26-2009 |
20090081188 | GLYCOPEGYLATED FACTOR IX - The present invention provides conjugates between Factor IX and PEG moieties. The conjugates are linked via an intact glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates. | 03-26-2009 |
20090093399 | Glycopegylation methods and proteins/peptides produced by the methods - The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide. | 04-09-2009 |
20090124544 | COMPOSITIONS AND METHODS FOR THE PREPARATION OF PROTEASE RESISTANT HUMAN GROWTH HORMONE GLYCOSYLATION MUTANTS - The present invention relates to protease resistant mutants of human growth hormone, which contain newly introduced proteolysis resistant mutations and N-linked or O-linked glycosylation site(s), such that these recombinantly produced polypeptides have glycosylation patterns distinctly different from that of the naturally occurring human growth hormone. The polynucleotide coding sequences for the mutants, expression cassettes comprising the coding sequences, cells expressing the mutants, and methods for producing the mutants are also disclosed. Further disclosed are pharmaceutical compositions comprising the mutants and method for using the mutants. | 05-14-2009 |
20090137763 | GLUCOSAMINE NUCLEOTIDE SUGARS - The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide. | 05-28-2009 |
20090169509 | O-linked glycosylation of peptides - The present invention provides polypeptides that include an O-linked glycosylation site that is not present in the wild-type peptide. The polypeptides of the invention include glycoconjugates in which a species such as a water-soluble polymer, a therapeutic agent of a biomolecule is covalently linked through an intact O-linked glycosyl residue to the polypeptide. Also provided are methods of making the peptides of the invention and methods, pharmaceutical compositions containing the peptides and methods of treating, ameliorating or preventing diseased in mammals by administering an amount of a peptide of the invention sufficient to achieve the desired response. | 07-02-2009 |
20090170155 | Mutant Endoglycoceramidases With Enhanced Synthetic Activity - 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. | 07-02-2009 |
20090176278 | SOLVENTS FOR MUTANT ENDOGLYCOCERAMIDASES WITH SYNTHETIC ACTIVITY - The present invention provides reaction mixtures comprising a solvent having at least one of an alkoxy ether and/or a polyhydric alcohol for use in reactions with a mutant endoglycoceramidase having enhanced synthetic activity. | 07-09-2009 |
20090203579 | Glycopegylated Granulocyte Colony Stimulating Factor - The present invention provides conjugates between Granulocyte Colony Stimulating Factor and PEG moieties. The conjugates are linked via an intact glycosyl linking group that is interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from both glycosylated and unglycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto either an amino acid or glycosyl residue on the peptide. Also provided are pharmaceutical formulations including the conjugates. Methods for preparing the conjugates are also within the scope of the invention. | 08-13-2009 |
20090292110 | Enzymatic modification of glycopeptides - The present invention provides glycoconjugates that are formed through the enzymatically-mediated coupling of a glycosyl moiety, e.g., on a peptide or lipid, and a modifying group that includes an acyl group. The conjugates include the modifying group tethered to the glycosyl moiety through a linking moiety that includes an acyl residue. Also provided are methods for preparing the conjugates of the invention | 11-26-2009 |
20090305349 | EXPRESSION OF SOLUBLE FACTOR VIII PROTEINS IN BACTERIA - The present invention provides enhanced methods of producing soluble Factor VIII proteins in microorganisms that have an oxidizing environment. | 12-10-2009 |
20090305967 | GLYCOPEGYLATED FACTOR VII AND FACTOR VIIA - The present invention provides conjugates between Factor VII or Factor VIIa peptides and PEG moieties. The conjugates are linked via an intact glycosyl linking group that is interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from both glycosylated and unglycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto either an amino acid or glycosyl residue on the peptide. Also provided are pharmaceutical formulations including the conjugates. Methods for preparing the conjugates are also within the scope of the invention. | 12-10-2009 |
20090311744 | EXPRESSION OF O-GLYCOSYLATED THERAPEUTIC PROTEINS IN PROKARYOTIC MICROORGANISMS - The invention relates to methods of producing an O-glycosylated soluble therapeutic protein in a prokaryotic microorganism by co-expressing the therapeutic protein and a heterologous glycosyltransferase that transfers a sugar moiety to an amino acid acceptor on the therapeutic protein. | 12-17-2009 |
20100009902 | Glycoconjugation Using Saccharyl Fragments - The present invention provides conjugates between a substrate, e.g., peptide, glycopeptide, lipid, etc., and a modified saccharyl fragment bearing a modifying group such as a water-soluble polymer, therapeutic moiety or a biomolecule. The conjugates are linked via the enzymatic conversion of the activated modified saccharyl fragment into a glycosyl linking group that is interposed between and covalently attached to the substrate and the modifying group. The conjugates are formed from substrates by the action of a sugar transferring enzyme, e.g., a glycosyltransferase. For example, when the substrate is a peptide, the enzyme conjugates a modified saccharyl fragment moiety onto either an amino acid or glycosyl residue of the peptide. Also provided are pharmaceutical formulations that include the conjugates. Methods for preparing the conjugates are also within the scope of the invention. | 01-14-2010 |
20100015684 | FACTOR VII: REMODELING AND GLYCOCONJUGATION OF FACTOR VII - The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide. | 01-21-2010 |
20100035299 | METHODS FOR THE PURIFICATION OF POLYPEPTIDE CONJUGATES - The present invention provides processes for the manufacturing of polypeptide conjugates. In particular, the invention provides methods for the purification of polypeptide conjugates, which include at least one polymeric modifying groups, such as a poly(alkylene oxide) moiety. Exemplary poly(alkylene oxide) moieties include poly(ethylene glycol) (PEG) and poly(propylene glycol). In an exemplary process, hydrophobic interaction chromatography (HIC) is used to resolve different glycoforms of glycoPEGylated polypeptides. | 02-11-2010 |
20100041872 | GLYCEROL LINKED PEGYLATED SUGARS AND GLYCOPEPTIDES - The present invention provides conjugates between peptides and PEG moieties through glycerol linkers. | 02-18-2010 |
20100048456 | GLYCOPEGYLATION METHODS AND PROTEINS/PEPTIDES PRODUCED BY THE METHODS - The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide. | 02-25-2010 |
20100075375 | METHODS FOR THE PURIFICATION OF POLYPEPTIDE CONJUGATES - The present invention provides processes for the manufacturing of polypeptide conjugates. In particular, the invention provides methods for the purification of polypeptide conjugates, which include at least one polymeric modifying groups, such as a poly(alkylene oxide) moiety. Exemplary poly(alkylene oxide) moieties include poly(ethylene glycol) (PEG) and poly(propylene glycol). In an exemplary process, hydrophobic interaction chromatography (HIC) is used to resolve different glycoforms of glycoPEGylated polypeptides. | 03-25-2010 |
20100081791 | GLYCOPEGYLATED FACTOR IX - The present invention provides conjugates between Factor IX and PEG moieties. The conjugates are linked via a glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. Conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates. | 04-01-2010 |
20100113743 | GLYCOPEGYLATED FACTOR VII AND FACTOR VIIA - The present invention provides conjugates between Factor VII or Factor VIIa peptides and PEG moieties. The conjugates are linked via an intact glycosyl linking group that is interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from both glycosylated and unglycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto either an amino acid or glycosyl residue on the peptide. Also provided are pharmaceutical formulations including the conjugates. Methods for preparing the conjugates are also within the scope of the invention. | 05-06-2010 |
20100174059 | PROCESS FOR THE PRODUCTION OF NUCLEOTIDE SUGARS - The current invention provides methods (e.g., large-scale processes) for the production of nucleotide sugars, which are modified with a polymeric modifying group, such as poly(alkylene oxide) moieties (e.g., poly(ethylene glycol) or poly(propylene glycol)) moieties. A typical process of the invention includes anion exchange chromatography followed by an ultrafiltration procedure, such as tangential flow filtration. The process of the invention provides modified nucleotide sugars in unexpectedly high purity and high overall yields. | 07-08-2010 |
20100261872 | Factor VIII: remodeling and glycoconjugation of factor VIII - The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide. | 10-14-2010 |
20100286067 | GLYCOCONJUGATION OF POLYPEPTIDES USING OLIGOSACCHARYLTRANSFERASES - The current invention provides polypeptides and polypeptide conjugates that include an exogenous N-linked glycosylation sequence. The N-linked glycosylation sequence is preferably a substrate for an oligosaccharyltransferase (e.g., bacterial PgIB), which can catalyze the transfer of a glycosyl moiety from a lipid-bound glycosyl donor molecule (e.g., a lipid-pyrophosphate-linked glycosyl moiety) to an asparagine (N) residue of the glycosylation sequence. In one example, the asparagine residue is part of an exogenous N-linked glycosylation sequence of the invention. The invention further provides methods of making the polypeptide conjugates that include contacting a polypeptide having an N-linked glycosylation sequence of the invention and a lipid-pyrophosphate-linked glycosyl moiety (or phospholipid-linked glycosyl moiety) in the presence of an oligosaccharyltransferase under conditions sufficient for the enzyme to transfer the glycosyl moiety to an asparagine residue of the N-linked glycosylation sequence. Exemplary glycosyl moieties that can be conjugated to the glycosylation sequence include GlcNAc, GlcNH, bacillosamine, 6-hydroybacillosamine, GalNAc, GaINH, GlcNAc-GlcNAc, GlcNAc-GlcNH, GlcNAc-Gal, GlcNAc-GlcNAc-Gal-Sia, GlcNAc-Gal-Sia, GlcNAc-GlcNAc-Man, and GlcNAc-GlcNAc-Man(Man)2. The transferred glycosyl moiety is optionally modified with a modifying group, such as a polymer (e.g., PEG). In one example, the modified glycosyl moiety is a GIcNAc or a sialic acid moiety. | 11-11-2010 |
20100324274 | NOVEL SYNTHETIC GANGLIOSIDE DERIVATIVES AND COMPOSITIONS THEREOF - Novel synthetic gangliosides and pharmaceutical compositions containing such synthetic gangliosides are described. Methods of making the novel synthetic ganglioside compounds and compositions as well as their use in the field of neuroprotection and cancer treatment is also described. | 12-23-2010 |
20100330060 | GLYCOPEGYLATED FACTOR IX - The present invention provides conjugates between Factor IX and PEG moieties. The conjugates are linked via an intact glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates. | 12-30-2010 |
20100330645 | ONE POT DESIALYLATION AND GLYCOPEGYLATION OF THERAPEUTIC PEPTIDES - The present invention provides conjugates between peptides and PEG moieties. The conjugates are linked via an intact glycosyl linking group that is interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from both glycosylated and unglycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto either an amino acid or glycosyl residue on the peptide. Also provided are pharmaceutical formulations including the conjugates. Methods for preparing the conjugates are also within the scope of the invention. | 12-30-2010 |
20100331489 | BRANCHED WATER-SOLUBLE POLYMERS AND THEIR CONJUGATES - The present invention provides branched water-soluble polymers that allow two or more water-soluble polymers to be conjugated to another species. The branched polymers provide access to therapeutic agents that are conjugated at a single site to two or more water-soluble polymers. The branched polymers are based upon branch points that are simple branched alkyl structures, reactive side-chain amino acids and small peptides of reactive side-chain amino acids, and saccharides. Also provided is a method for preparing mono-disperse poly(ethylene glycol) of a well-defined and determinable molecular weight, and a method for the rational end-functionalization of poly(ethylene glycol). Conjugates of the branched water-soluble polymers with diverse species, e.g., peptides, lipids, glycolipids and small molecules are also provided. | 12-30-2010 |
20110003744 | Glycopegylated Erythropoietin Formulations - The present invention provides conjugates between erythropoietin and PEG moieties. The conjugates are linked via an intact glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates. | 01-06-2011 |
20110177029 | O-LINKED GLYCOSYLATION USING N-ACETYLGLUCOSAMINYL TRANSFERASES - The present invention provides covalent conjugates between a polypeptide and a modifying group, such as a water-soluble polymer (e.g., PEG). The amino acid sequence of the polypeptide includes one or more O-linked glycosylation sequence, each being a substrate for a GIcNAc transferase. The modifying group is covalently linked to the polypeptide via a glycosyl-linking group interposed between and covalently linked to both the polypeptide and the modifying group. In one embodiment, a glucosamine linking group is directly attached to an amino acid residue of the O-linked glycosylation sequence. The invention further provides methods of making polypeptide conjugates. The present invention also provides non-naturally occurring polypeptides that include at least one O-linked linked glycosylation sequence of the invention, wherein each glycosylation sequence is a substrate for a GIcNAc transferase. The invention further provides pharmaceutical compositions that include a polypeptide conjugate of the invention. | 07-21-2011 |
20110318780 | ENZYMATIC MODIFICATION OF GLYCOPEPTIDES - The present invention provides glycoconjugates that are formed through the enzymatically-mediated coupling of a glycosyl moiety, e.g., on a peptide or lipid, and a modifying group that includes an acyl group. The conjugates include the modifying group tethered to the glycosyl moiety through a linking moiety that includes an acyl residue. Also provided are methods for preparing the conjugates of the invention | 12-29-2011 |
20120016105 | PURIFICATION OF PEPTIDE CONJUGATES BY HYDROPHOBIC INTERACTION CHROMATOGRAPHY - The present invention provides polypeptides that include an O-linked glycosylation site that is not present in the wild-type peptide. The polypeptides of the invention include glycoconjugates in which a species such as a water-soluble polymer, a therapeutic agent of a biomolecule is covalently linked through an intact O-linked glycosyl residue to the polypeptide. Also provided are methods of making a glycoconjugate, methods of isolating a glycoconjugate from a reaction mixture, pharmaceutical compositions containing a glycoconjugate, and methods of treating, ameliorating or preventing diseased in mammals by administering an amount of a glycoconjugate sufficient to achieve the desired response. | 01-19-2012 |
20120035120 | GLYCOLIPIDS AS TREATMENT FOR DISEASE - This invention provides compounds, compositions, and methods for treating a disorder selected from cancer, hyperinsulinemia, hypoglycemia, hyperinsulinemia with hypoglycemia, atypical Parkinson's disease, Huntington's disease, multiple systems atrophy, GM3 synthase deficiency, GM2 synthase deficiency or tauopathy. | 02-09-2012 |
20120083600 | NUCLEOTIDE SUGAR PURIFICATION USING MEMBRANES - The invention provides methods of removing contaminants from a mixture of a desired product and contaminants by pH adjustments and molecular weight cut-offs. The contaminants include phosphate groups, magnesium sulfate, sodium pyruvate and tetrasodium pyrophosphate groups. The desired product includes nucleotide sugars, glycolipids, LnNT, sialyl lactose, and salts. | 04-05-2012 |
20120107867 | GLYCOPEGYLATED ERYTHROPOIETIN - The present invention provides conjugates between erythropoietin and PEG moieties. The conjugates are linked via an intact glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates. | 05-03-2012 |
20120172300 | REMODELING AND GLYCOPEGYLATION OF FIBROBLAST GROWTH FACTOR (FGF) - The present invention relates to mutants of Fibroblast Growth Factor (FGF), particularly FGF-20 and FGF-21, which contain newly introduced N-linked or O-linked glycosylation site(s). The polynucleotide coding sequences for the mutants, expression cassettes comprising the coding sequences, cells expressing the mutants, and methods for producing the mutants are also disclosed. Further disclosed are pharmaceutical compositions comprising the mutants and method for using the mutants. | 07-05-2012 |
20120220517 | Glycopegylation Methods and Proteins/Peptides Produced by the Methods - The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide. | 08-30-2012 |
20130059780 | BRANCHED PEG REMODELING AND GLYCOSYLATION OF GLUCAGON-LIKE PEPTIDE-1 [GLP-1] - The present invention provides polypeptides that include an O-linked glycoconjugate in which a species such as a water-soluble polymer, a therapeutic agent of a biomolecule is covalently linked through an intact O-linked glycosyl residue to the polypeptide. The polypeptides of the invention include wild-type peptides and mutant peptides that include an O-linked glycosylation site that is not present in the wild-type peptide. Also provided are methods of making the peptides of the invention and methods, pharmaceutical compositions containing the peptides and methods of treating, ameliorating or preventing diseased in mammals by administering an amount of a peptide of the invention sufficient to achieve the desired response. | 03-07-2013 |
20130137157 | GLYCOPEGYLATED FACTOR VII AND FACTOR VIIA - The present invention provides conjugates between Factor VII or Factor VIIa peptides and PEG moieties. The conjugates are linked via an intact glycosyl linking group that is interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from both glycosylated and unglycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto either an amino acid or glycosyl residue on the peptide. Also provided are pharmaceutical formulations including the conjugates. Methods for preparing the conjugates are also within the scope of the invention. | 05-30-2013 |
20130137638 | CONJUGATED FACTOR VIII MOLECULES - The present invention relates to B-domain truncated Factor VIII molecules with a modified circulatory half life, said molecule being covalently conjugated with a hydrophilic polymer. The invention furthermore relates to methods for obtaining such molecules as well as use of such molecules. | 05-30-2013 |
20130189239 | Conjugated Factor VIII Molecules - The present invention relates to B-domain truncated Factor VIII molecules with a modified circulatory half life, said molecule being covalently conjugated with a hydrophilic polymer. The invention furthermore relates to methods for obtaining such molecules as well as use of such molecules. | 07-25-2013 |
20130344050 | Glycopegylated Factor IX - Conjugates between Factor IX and PEG moieties. are disclosed in the present application. The conjugates are linked via a glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. Conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates. | 12-26-2013 |
20140112903 | Glycopegylated Factor IX - Conjugates between Factor IX and PEG moieties. are disclosed in the present application. The conjugates are linked via a glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. Conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates. | 04-24-2014 |
20140147891 | MUTANT ENDOGLYCOCERAMIDASES WITH ENHANCED SYNTHETIC ACTIVITY - 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. | 05-29-2014 |
20140154230 | Glycopegylated Factor IX - Conjugates between Factor IX and PEG moieties. are disclosed in the present application. The conjugates are linked via a glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. Conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates. | 06-05-2014 |
20140170728 | Factor IX: Remodeling and Glycoconjugation of Factor IX - The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide. | 06-19-2014 |
20140242057 | CONJUGATED FACTOR VIII MOLECULES - The present invention relates to B-domain truncated Factor VIII molecules with a modified circulatory half life, said molecule being covalently conjugated with a hydrophilic polymer. The invention furthermore relates to methods for obtaining such molecules as well as use of such molecules. | 08-28-2014 |
20140294762 | GLYCOPEGYLATION METHODS AND PROTEINS/PEPTIDES PRODUCED BY THE METHODS - The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide. | 10-02-2014 |