# US 7,078,206 B2 · UDP-N-acetylglucosamine: galactose-β1,3-N-acetylgalactosamine-α-R/ (GlcNAc to GalNAc) β1,6N-acetylglucosaminyltransferase, C2GnT3

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- Number: US 7,078,206 B2
- Document ID: US7078206B2
- Status: Granted
- Kind: B2
- Application number: 10/843,723
- Filed: 2004-05-11
- Published: 2004-10-14
- Granted: 2006-07-18
- Earliest claimed: 1999-08-24
- Assignees: Glycozym ApS
- Inventors: Tilo Schwientek; Henrik Clausen
- Web page: https://patentgrep.com/patent/US7078206B2

## CPC

- C12N 9/1051: {Hexosyltransferases (2.4.1)}
- A61P 5/00: Drugs for disorders of the endocrine system
- A61P 31/18: for HIV
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 35/04: specific for metastasis
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- A61K 48/00: Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

A novel gene defining a novel human UDP-GlcNAc: Galβ1-3GalNAcα β1,6GlcNAc-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. Further, the invention discloses methods of obtaining 1,6-N-acetylglucosaminyl glycosylated saccharides, glycopeptides or glycoproteins by use of an enzymically active C2GnT3 protein or fusion protein thereof or by using cells stably transfected with a vector including DNA encoding an enzymatically active C2GnT3 protein as an expression system for recombinant production of such glycopeptides or glycoproteins. Methods are disclosed for the identification of agents with the ability to inhibit or stimulate the biological activity of C2GnT3. Furthermore, methods of using C2GnT3 in the structure-based design of inhibitors or stimulators thereof are also disclosed in the invention. Also a method for the identification of DNA sequence variations in the C2GnT3 gene by isolating DNA from a patient, amplifying C2GnT3-coding exons by PCR, and detecting the presence of DNA sequence variation, are disclosed.

## Claims

### Claim 1

An isolated UDP-N-Acetylglucosamine: Galactose β1,3 N-Acetylgalactosamine-α-R β1,6 N-Acetylglucosaminyl transferase (C2GnT3) polypeptide having glycosyltransferase activity and at least 80% amino acid sequence identity to the amino acid sequence of SEQ ID NO: 2.

### Claim 2 (depends on 1)

The isolated C2GnT3 polypeptide of claim 1, wherein said amino acid sequence identity is at least 85%.

### Claim 3

A UDP-N-Acetylglucosamine: Galactose β1,3 N-Acetylgalactosamine-α-R β1,6 N-Acetylglucosaminyl transferase (C2GnT3) polypeptide produced by a method comprising:
(i) introducing into a host cell an isolated DNA molecule encoding a human C2GnT3 polypeptide, or a DNA construct comprising a DNA sequence encoding a C2GnT3 polypeptide;
(ii) growing the host cell under conditions suitable for human C2GnT3 expression; and
(iii) isolating C2GnT3 polypeptide produced by the host cell,
wherein said C2GnT3 polypeptide has glycosyltransferase activity and is at least 80% identical to SEQ ID NO: 2.

### Claim 4 (depends on 3)

The C2GnT3 polypeptide of claim 3, wherein said C2GnT3 polypeptide is at least 85% identical to SEQ ID NO: 2.