O-Glycosylation Inhibitor Development Service

O-Glycosylation Inhibitor Development Service

O-Glycosylation Inhibitor Development Service at CD BioGlyco

O-Glycosylation plays an important role in cell signaling, protein stability, and functional regulation. However, abnormal O-glycosylation causes a variety of diseases. By developing O-glycosylation inhibitors, abnormal glycosylation modifications are interfered with, thereby intervening in the occurrence and progression of the disease and providing the possibility for new treatment strategies. CD BioGlyco is a world-leading biotechnology company. We have diversified technologies for Glycosylation Inhibitor Development and provide professional and various types of O-glycosylation inhibitor development services.

O-Glycan synthesis begins with the transfer of N-acetylgalactosamine (GalNAc) from UDP-N-acetylglucosamine (UDP-GalNAc) to Ser or Thr residues of the glycoprotein, which is catalyzed by polypeptide N-acetyl-α-galactosaminyltransferase (ppGalNAcTs). The ppGalNAcTs family is involved in the progression of many cancers, and the development of inhibitors of this enzyme could serve as potential targets for anticancer immunotherapy. CD BioGlyco provides various O-GalNAc inhibitor development services and conducts synthesis and structural optimization of screened inhibitors to improve the selectivity and affinity of the inhibitors.

Core 1 β1,3-galactosyltransferase (C1GalT1) transfers galactose to N-acetylgalactosamine to synthesize T antigen. Alterations in C1GalT1 expression lead to changes in the structure of O-glycans in glycoproteins. CD BioGlyco uses high-throughput screening technology to provide professional core 1 inhibitor development service and evaluates the inhibitory activity of candidate inhibitors through animal experimental studies and cell function analysis.

Core 1 branches through the core 2 β1,6-N-acetylglucosaminyltransferase (C2GnT) family to form core 2. CD BioGlyco provides a proven core 2 inhibitor development service, where our scientists will design and synthesize new core 2 inhibitor candidates and optimize their physicochemical properties. Core 2 inhibitors serve as research tools to study the molecular mechanisms and interactions of glycan regulation.

Core 3 structures are found only in mucins of certain tissues, such as the stomach, colon, and small intestine. The formation of the core 3 structure is catalyzed by β1,3-N-acetylglucosaminyltransferase 6 (β3GnT6). Anti-β3GnT6 drugs or antibodies selectively interfere with or inhibit the functions of the β3GnT6 enzyme, thereby affecting its catalytic reaction and biological processes. CD BioGlyco provides a highly efficient core 3 inhibitor development service. We have generated anti-β3GnT6 antibodies that inhibit or modulate the activity of the β3GnT6 enzyme.

The core 4 structure is implemented by adding N-acetylglucosamine (GlcNAc) to the 6 bits of GalNAc in the core 3 structure, which is catalyzed by core 4 β1,6-GlcNAc transferase. CD BioGlyco has an advanced glycosylation inhibitor development means and we provide a one-stop core 4 inhibitor development service. Core 4 has an important regulatory effect on immune cells. The development of core 4 inhibitors is used to interfere with immune cell activation and inflammatory responses, which has potential applications in the research of various diseases.

The biosynthetic pathway of sialyl-Tn antigen involves the interaction of multiple enzymes and substrates. Sialyl-Tn is an antigen expressed early in tumorigenesis. The development of sialyl-Tn antigen inhibitors interferes with the biosynthetic process of sialyl-Tn antigen and is of great significance to cancer research and other related fields. CD BioGlyco has established excellent glycosylation inhibitor development solutions and provides multiple modes of sialyl-Tn antigen inhibitor development service.

Sialyl-T antigen is synthesized from Tn antigen, and the development of sialyl-T antigen inhibitors is applied in the research of tumors or cancer. The specific adhesion formed by the interaction between the sialyl-T antigen and the lectin Galectin-3 (Gal-3) strongly erodes tumor cells and inhibits the occurrence and metastasis of tumor cells. Based on this, CD BioGlyco will provide development for tumor inhibitors with sialyl-T antigen as the core structure.

SLeX is a salivary laser-acidified polytetrasaccharide that is an endogenous antigen. It is highly expressed in many epithelial tumor cells and binds to the adhesion molecule E-selectin on vascular endothelial cells in the form of a ligand. Based on this feature, CD BioGlyco will develop an antigen inhibitor (ligand competitor) that binds to E-selectin through a competitive reaction with SLeX antigen, blocking the binding of SLeX antigen to intravascular adhesion molecules, thereby inhibiting tumor cell activity.

Glycans have multiple roles in the virus entry process. Blocking the glycosylation modification of O-glycans using glycobiology methods may effectively inhibit the virus entry process, which is an effective method for developing antiviral inhibitors. CD BioGlyco provides specialized blocking O-glycan-protein interaction inhibitor development service.

Fig.1 O-Glycosylation inhibitor development service. (CD BioGlyco)Fig.1 O-Glycosylation inhibitor development service. (CD BioGlyco)


  • Regulation of infection and inflammation: Glycosylation interactions between pathogens and host cells have important consequences for infection and inflammatory processes. The development of O-glycosylation inhibitors interferes with the glycosylation interaction between pathogens and host cells, blocks pathogen invasion and inflammatory responses, and provides new strategies for the study of infection and inflammation-related diseases.
  • Glycoprotein biology research: O-Glycosylation is an important regulatory mechanism for glycoprotein structure and functions. By developing O-glycosylation inhibitors, the biological functions of glycoproteins are studied and their roles in cell signaling, molecular recognition, and disease development may be explored.
  • Drug design and optimization: The activity and efficacy of certain drugs may be affected by glycosylation modifications. By developing O-glycosylation inhibitors, we interfere with the interaction between drugs and glycosylation targets and improve the selectivity and efficacy of drugs.


  • Advanced facilities: CD BioGlyco is equipped with advanced knowledge to support the development and evaluation needs of multiple types of O-glycosylation inhibitors.
  • Diverse technology solutions: CD BioGlyco has a variety of mature technology solutions, including high-throughput screening, computer-aided drug design, chemical synthesis, biological activity assessment, etc., to meet the development needs of different clients for O-glycosylation inhibitors.
  • Multi-level screening: CD BioGlyco has established a rich compound library, we use a multi-level screening method to screen out compounds with potential O-glycosylation inhibitory activity from the large-scale compound library and conduct further optimization and verification.

CD BioGlyco has an efficient team of researchers and experts that quickly respond to client needs and provide multiple types of mature O-glycosylation inhibitor development services. Please feel free to contact us if you are interested in our inhibitor development and we will provide you with the best quality service.


  1. Desko, M.M.; Kohler, J.J. Glycosylation of proteins in the Golgi apparatus. Wiley Encyclopedia of Chemical Biology. 2007, 1-15.
This service is for Research Use Only, not intended for any clinical use.

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