Abstract: A novel gene defining a novel enzyme UDP-galactose: ?-D-galactose-R 4-?-D-galactosyltransferase, termed ?4Gal-T1, with unique enzymatic properties is disclosed. The invention provides isolated DNA molecules and DNA constructs encoding ?4Gal-T1 and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting ?4Gal-T1 activity, as well as cloning and expression vectors including such DNA, host cells comprising DNA encoding ?4Gal-T1, and recombinant methods for providing ?4Gal-T1. The enzyme ?4Gal-T1 and ?4Gal-active derivatives thereof are disclosed. Further, the invention discloses methods of obtaining ?1, 4galactosyl glycosylated glycosphingolipids by use of an enzymatically active ?4Gal-T1 protein thereof or by using cells stably transfected with a vector including DNA encoding an enzymatically active ?4Gal-T1 protein as an expression system for recombinant production of such glycosphingolipids.

Abstract: A novel gene defining a novel enzyme in the UDP-D-galactose: ?-N-acetylglucosamine / ?-N-acetylgalactosamine ?1,3galactosyltransferase family, termed ?3Gal-T5, with unique enzymatic properties is disclosed. The enzymatic activity of ?3Gal-T5 is shown to be distinct from that of previously identified enzymes of this gene family. The invention discloses isolated DNA molecules and DNA constructs encoding ?3Gal-T5 and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting ?3Gal-T5 activity, as well as cloning and expression vectors including such DNA, cells transfected with the vectors, and recombinant methods for providing ?3Gal-T5. The enzyme ?3Gal-T5 and ?3Gal-T5-active derivatives thereof are disclosed, in particular soluble derivatives comprising the catalytically active domain of ?3Gal-T5.

Abstract: A novel gene defining a novel enzyme UDP-galactose: ?-D-galactose-R 4-?-D-galactosyltransferase, termed ?4Gal-T1, with unique enzymatic properties is disclosed. The invention provides isolated DNA molecules and DNA constructs encoding ?4Gal-T1 and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting ?4Gal-T1 activity, as well as cloning and expression vectors including such DNA, host cells comprising DNA encoding ?4Gal-T1, and recombinant methods for providing ?4Gal-T1. The enzyme ?4Gal-T1 and ?4Gal-active derivatives thereof are disclosed. Further, the invention discloses methods of obtaining ?1, 4galactosyl glycosylated glycosphingolipids by use of an enzymatically active ?4Gal-T1 protein thereof or by using cells stably transfected with a vector including DNA encoding an enzymatically active ?4Gal-T1 protein as an expression system for recombinant production of such glycosphingolipids.

Abstract: A novel gene defining a novel human UDP-GlcNAc: Gal/Gl cNAc? 1-3GalNAc ??1, 6GlcNAc-transferase, termed C2/4GnT, with unique enzymatic properties is disclosed. The enzymatic activity of C2/4GnT is shown to be distinct from that of previously identified enzymes of this gene family. The invention discloses isolated DNA molecules and DNA constructs encoding C2/4GnT and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting C2/4GnT activity, as well as cloning and expression vectors including such DNA, cells transfected with the vectors, and recombinant methods for providing C2/4GnT. The enzyme C2/4GnT and C2/4GnT-active derivatives thereof are disclosed, in particular soluble derivatives comprising the catalytically active domain of C2/4GnT.

Abstract: A novel gene defining a novel enzyme in the UDP-D-galactose: b-N-acetyl-glucosamine ?-1,4-galactosyltransferase family, termed ?4Gal-T2, with unique enzymatic properties is disclosed. The enzymatic activity of ?4Gal-T2 is shown to be distinct from that of previously identified enzymes of this gene family. The invention discloses isolated DNA molecules and DNA constructs encoding ?4Gal-T2 and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting ?4Gal-T2 activity, as well as cloning and expression vectors including such DNA, cells transfected with the vectors, and recombinant methods for providing ?4Gal-T2. The enzyme ?4Gal-T2 and ?4Gal-T2-active derivatives thereof are disclosed, in particular soluble derivatives comprising the catalytically active domain of ?4Gal-T2.

Abstract: Attachment of O-glycans to proteins is controlled by a large family of homologous polypeptide GalNAc-transferases. Polypeptide GalNAc-transferases contain a C-terminal sequence with similarity to lectins. This invention discloses that the putative lectin domains of GalNAc-transferase isoforms, GalNAc-T4, -T7, -T2, and -T3, are functional and recognize carbohydrates, glycopeptides, and peptides and discloses the lectin domains of GalNAc-T1-T16. These lectin domains have different binding specificities and modulate the functions of GalNAc-transferase isoforms differently. Novel methods for identification of inhibitors or modulators of binding activities mediated by lectin domains of polypeptide GalNAc-transferases are disclosed. Direct binding activity of GalNAc-transferase lectins has been demonstrated for the first time and methods to measure lectin mediated binding of isolated lectins or enzymes with lectin domains are disclosed.

Abstract: A novel gene defining a novel enzyme in the UDP-D-galactose: beta-N-acetylglucosamine/beta-N-acetylgalactosamine beta 1,3galactosyltransferase family, termed beta3Gal-T5, with unique enzymatic properties is disclosed. The enzymatic activity of beta3Gal-T5 is shown to be distinct from that of previously identified enzymes of this gene family. The invention discloses isolated DNA molecules and DNA constructs encoding beta3Gal-T5 and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting beta3Gal-T5 activity, as well as cloning and expression vectors including such DNA, cells transfected with the vectors, and recombinant methods for providing beta3Gal-T5. The enzyme beta3Gal-T5 and beta3Gal-T5-active derivatives thereof are disclosed, in particular soluble derivatives comprising the catalytically active domain of beta3Gal-T5.

Abstract: Novel methods for identification of inhibitors or modulators of binding activities mediated by lectin domains of polypeptide GalNAc-transferases are disclosed. Direct binding activity of GalNAc-transferase lectins has been demonstrated for the first time and methods to measure lectin mediated binding of isolated lectins or enzymes with lectin domains are disclosed. The present invention specifically discloses a novel selective inhibitor of polypeptide GalNAc-transferase lectin domains, which provides a major advancement in that this inhibitor and related inhibitors sharing common characteristics of activity bind lectin domains without serving as acceptor substrate for glycosyltransferases involved in synthesis of O-glycans. This inhibitor is represented by the O-anomeric configuration of GalNAc-benzyl, GalNAc?-benzyl.

Abstract: A novel gene defining a novel enzyme UDP-Galactose: ?-D-Galactose-R 4-?-D-galactosyltransferase, termed ?4Gal-T1, with unique enzymatic properties is disclosed. The invention discloses isolated DNA molecules and DNA constructs encoding ?4Gal-T1 and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting ?4Gal-T1 activity, as well as cloning and expression vectors including such DNA, cells transfected with vectors, and recombinant methods for providing ?4Gal-T1. The enzyme ?4Gal-T1 and ?4Gal-active derivatives thereof are disclosed. Further, the invention discloses methods of obtaining ?1, 4galactosyl glycosylated glycosphingolipids by use of an enzymatically active ?4Gal-T1 protein thereof or by using cells stably transfected with a vector including DNA encoding an enzymatically active ?4Gal-T1 protein as an expression system for recombinant production of such glycosphingolipids.

Abstract: A novel gene defining a novel human UDP-GlcNAc: Gal?1-3GalNAca ?1,6GlcNAc-transferase, termed C2GnT3, with unique enzymatic properties is disclosed. The enzymatic activity of C2GnT3 is shown to be distinct from that of previously identified enzymes of this gene family. The invention discloses isolated DNA molecules and DNA constructs encoding C2GnT3 and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting C2GnT3 activity, as well as cloning and expression vectors including such DNA, cells transfected with the vectors, and recombinant methods for providing C2GnT3. The enzyme C2GnT3 and C2GnT3-active derivatives thereof are disclosed, in particular soluble derivatives comprising the catalytically active domain of C2GnT3.

Abstract: A novel gene defining a novel human UDP-GlcNAc: Gal?1-3GalNAc? ?1,6GlcNAc-transferase, termed C2GnT3, with unique enzymatic properties is disclosed. The enzymatic activity of C2GnT3 is shown to be distinct from that of previously identified enzymes of this gene family. The invention discloses isolated DNA molecules and DNA constructs encoding C2GnT3 and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting C2GnT3 activity, as well as cloning and expression vectors including such DNA, cells transfected with the vectors, and recombinant methods for providing C2GnT3. The enzyme C2GnT3 and C2GnT3-active derivatives thereof are disclosed, in particular soluble derivatives comprising the catalytically active domain of C2GnT3.

Abstract: A novel gene defining a novel human UDP-GlcNAc: Gal?1-3GalNAc? ?1,6GlcNAc-transferase, termed C2GnT3, with unique enzymatic properties is disclosed. The enzymatic activity of C2GnT3 is shown to be distinct from that of previously identified enzymes of this gene family. The invention discloses isolated DNA molecules and DNA constructs encoding C2GnT3 and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting C2GnT3 activity, as well as cloning and expression vectors including such DNA, cells transfected with the vectors, and recombinant methods for providing C2GnT3. The enzyme C2GnT3 and C2GnT3-active derivatives thereof are disclosed, in particular soluble derivatives comprising the catalytically active domain of C2GnT3.

Abstract: A novel gene defining a novel enzyme in the UDP-D-galactose: ?-N-acetylglucosamine/?-N-acetylgalactosamine ?1,3galactosyltransferase family, termed ?3Gal-T5, with unique enzymatic properties is disclosed. The enzymatic activity of ?3Gal-T5 is shown to be distinct from that of previously identified enzymes of this gene family. The invention discloses isolated DNA molecules and DNA constructs encoding ?3Gal-T5 and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting ?3Gal-T5 activity, as well as cloning and expression vectors including such DNA, cells transfected with the vectors, and recombinant methods for providing ?3Gal-T5. The enzyme ?3Gal-T5 and ?3Gal-T5-active derivatives thereof are disclosed, in particular soluble derivatives comprising the catalytically active domain of ?3Gal-T5.

Abstract: A novel gene defining a novel enzyme UDP-galactose: ?-D-galactose-R 4-?-D-galactosyltransferase, termed ?4Gal-T1, with unique enzymatic properties is disclosed. The invention provides isolated DNA molecules and DNA constructs encoding ?4Gal-T1 and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting ?4Gal-T1 activity, as well as cloning and expression vectors including such DNA, host cells comprising DNA encoding ?4Gal-T1, and recombinant methods for providing ?4Gal-T1. The enzyme ?4Gal-T1 and ?4Gal-active derivatives thereof are disclosed. Further, the invention discloses methods of obtaining ?1, 4galactosyl glycosylated glycosphingolipids by use of an enzymatically active ?4Gal-T1 protein thereof or by using cells stably transfected with a vector including DNA encoding an enzymatically active ?4Gal-T1 protein as an expression system for recombinant production of such glycosphingolipids.

Abstract: A novel gene defining a novel human UDP-GlcNAc: Gal/Gl cNAc? 1-3GalNAc ??1, 6GlcNAc-transferase, termed C2/4GnT, with unique enzymatic properties is disclosed. The enzymatic activity of C2/4GnT is shown to be distinct from that of previously identified enzymes of this gene family. The invention discloses isolated DNA molecules and DNA constructs encoding C2/4GnT and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting C2/4GnT activity, as well as cloning and expression vectors including such DNA, cells transfected with the vectors, and recombinant methods for providing C2/4GnT. The enzyme C2/4GnT and C2/4GnT-active derivatives thereof are disclosed, in particular soluble derivatives comprising the catalytically active domain of C2/4GnT.

Abstract: A novel gene defining a novel enzyme in the UDP-D-galactose: b-N-acetyl-glucosamine ?-1,4-galactosyltransferase family, termed ?4Gal-T2, with unique enzymatic properties is disclosed. The enzymatic activity of ?4Gal-T2 is shown to be distinct from that of previously identified enzymes of this gene family. The invention discloses isolated DNA molecules and DNA constructs encoding ?4Gal-T2 and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting ?4Gal-T2 activity, as well as cloning and expression vectors including such DNA, cells transfected with the vectors, and recombinant methods for providing ?4Gal-T2. The enzyme ?4Gal-T2 and ?4Gal-T2-active derivatives thereof are disclosed, in particular soluble derivatives comprising the catalytically active domain of ?4Gal-T2.

Abstract: A novel gene defining a novel enzyme in the UDP-D-galactose: b-N-acetyl-glucosamine ?-1,4-galactosyltransferase family, termed ?4Gal-T2, with unique enzymatic properties is disclosed. The enzymatic activity of ?4Gal-T2 is shown to be distinct from that of previously identified enzymes of this gene family. The invention discloses isolated DNA molecules and DNA constructs encoding ?4Gal-T2 and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting ?4Gal-T2 activity, as well as cloning and expression vectors including such DNA, cells transfected with the vectors, and recombinant methods for providing ?4Gal-T2. The enzyme ?4Gal-T2 and ?4Gal-T2-active derivatives thereof are disclosed, in particular soluble derivatives comprising the catalytically active domain of ?4Gal-T2.

Abstract: A novel gene defining a novel human UDP-GlcNAc: Gal/Gl cNAc? 1-3GalNAc ??1, 6GlcNAc-transferase, termed C2/4GnT, with unique enzymatic properties is disclosed. The enzymatic activity of C2/4GnT is shown to be distinct from that of previously identified enzymes of this gene family. The invention discloses isolated DNA molecules and DNA constructs encoding C2/4GnT and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting C2/4GnT activity, as well as cloning and expression vectors including such DNA, cells transfected with the vectors, and recombinant methods for providing C2/4GnT. The enzyme C2/4GnT and C2/4GnT-active derivatives thereof are disclosed, in particular soluble derivatives comprising the catalytically active domain of C2/4GnT.

Abstract: Novel methods for identification of inhibitors or modulators of binding activities mediated by lectin domains of polypeptide GalNAc-transferases are disclosed. Direct binding activity of GalNAc-transferase lectins has been demonstrated for the first time and methods to measure lectin mediated binding of isolated lectins or enzymes with lectin domains are disclosed. The present invention specifically discloses a novel selective inhibitor of polypeptide GalNAc-transferase lectin domains, which provides a major advancement in that this inhibitor and related inhibitors sharing common characteristics of activity bind lectin domains without serving as acceptor substrate for glycosyltransferases involved in synthesis of O-glycans. This inhibitor is represented by the ?-anomeric configuration of GalNAc-benzyl, GalNAc?-benzyl.

Abstract: A novel gene defining a novel human UDP-GlcNAc: Gal&bgr;1-3GalNAca &bgr;1,6GlcNAc-transferase, termed C2GnT3, with unique enzymatic properties is disclosed. The enzymatic activity of C2GnT3 is shown to be distinct from that of previously identified enzymes of this gene family. The invention discloses isolated DNA molecules and DNA constructs encoding C2GnT3 and derivatives thereof by way of amino acid deletion, substitution or insertion exhibiting C2GnT3 activity, as well as cloning and expression vectors including such DNA, cells transfected with the vectors, and recombinant methods for providing C2GnT3. The enzyme C2GnT3 and C2GnT3-active derivatives thereof are disclosed, in particular soluble derivatives comprising the catalytically active domain of C2GnT3.