O-GalNAc Inhibitor Development Service

O-GalNAc Inhibitor Development Service

O-GalNAc Inhibitor Development Service at CD BioGlyco

The O-glycans synthesis begins with the transfer of N-acetylgalactosamine (GalNAc) from UDP-N-acetylgalactosamine (UDP-GalNAc) to Ser or Thr residues of the glycoprotein, yielding the Tn antigen. The entire process is catalyzed by a multigene family of enzymes called polypeptide N-acetyl-α-galactosaminyltransferases (ppGalNAcTs). The ppGalNAcTs family participates in the progression of many cancers and be used as tumor diagnostic and prognostic markers. At the same time, the development of inhibitors of this enzyme is used as potential targets for anti-cancer immunotherapy.

  • Inhibitor screening and synthesis service

CD BioGlyco provides various types of O-GalNAc inhibitor development services and conducts synthesis and structural optimization of the screened inhibitors to improve the selectivity and affinity of the inhibitors.

CD BioGlyco has performed a kinetic analysis of ppGalNAcT for the development of peptide inhibitors, observing that endogenous peptide O-GalNAc transferase inhibitor (EPO-G) inhibits ppGalNAc and helping to determine its enzymatic mechanism of action. Another method to inhibit ppGalNAc and thereby inhibit overall O-glycosylation is to use UDP-GalNAc derivatives.

  • CD BioGlyco provides aryl glycosides of GalNAc and its derivatives development service, which inhibit the extension of O-GalNAc chains. The derivative benzyl-α-GalNAc reduces the sialylation level of mucin secreted by human colon cancer cell lines.
  • CD BioGlyco synthesizes peracetylated GalNAc analogs with hydrophilic substitutions on the N-acetyl group (e.g., azidoacetyl and glycoloyl), which is incorporated into cell surface glycoproteins at slightly lower levels than native GalNAc, which may be used for passive cancer immunotherapy targeting tumor-associated O-glycans on the cell surface.
  • CD BioGlyco has synthesized a C-glycoside UDP-GalNAc mimetic, and evaluation has shown a similar inhibitory pattern to UDP-GlcNAc in vitro.

In addition, CD BioGlyco provides high-throughput screening for ppGalNAcT inhibitors based on uridine libraries. The library retains the uridine portion of the nucleotide sugar substrate and uses three different linkers to combine uridine with a variety of bases through oxime or hydrazone bonds. We screen candidate compounds with the potential to inhibit O-GalNAc from the compound library. For example: We have identified ppGalNAcT inhibitors containing 2,3,4-trihydroxyphenyl groups from the library. They inhibit O-glycosylation and induce apoptosis in different cells. We also have screened a class of quinoline compounds T3Inh-1, which is a direct inhibitor of ppGalNAc-T3.

  • Inhibitor activity assessment service

CD BioGlyco uses cell models or in vitro experimental systems to provide O-GalNAc inhibitor activity assessment service, including experiments to determine inhibitor activity and effects on O-GalNAc modification.

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


Technology: High-throughput screening, Flow cytometry

Journal: Chemistry & Biology

IF: 9.039

Published: 2004

Results: The authors screened ppGalNAcT inhibitors that initiate O-linked glycosylation. They used novel high-throughput technology to screen two mppGalNAcT-1 inhibitors 1-68A and 2-68A from a uridine-based library, which inhibited ppGalNAcT 1 -5, 7, 10, and 11, were broad-spectrum inhibitors of the ppGalNAcT family. At the same time, these compounds destroyed O-linked glycosylation in cells and induced apoptosis of human T-cell lymphoma cells.

Fig.2 Screened ppGalNAcT inhibitors. (Hang, et al., 2004)Fig.2 Screened ppGalNAcT inhibitors. (Hang, et al., 2004)


  • Drug research: O-GalNAc inhibitors are applied as potential drug targets for the development of drugs for cancer, diabetes, genetic diseases, and other diseases. The development of effective O-GalNAc inhibitors intervenes and modulates the key role of O-GalNAc modification in disease development.
  • Biological research: By selectively inhibiting O-GalNAc transferase activity, the impact of this modification on cell signaling, and cell adhesion are explored, thereby revealing its importance in biological processes.
  • Protein engineering: O-GalNAc modification plays a vital role in the protein expression process. By developing O-GalNAc inhibitors, the O-GalNAc modification level of proteins is regulated, thereby improving the stability, activity, and pharmacokinetic properties of the protein.


  • CD BioGlyco is equipped with advanced laboratory facilities and Glycosylation Inhibitor Development Solutions. Our scientists conduct various key experiments such as high-throughput screening, chemical synthesis, and pharmacokinetic evaluation to ensure the success of O-GalNAc inhibitor development projects.
  • CD BioGlyco has established a diverse compound library covering multiple chemical classes and structurally diverse molecular models to support O-GalNAc inhibitor development from screening to optimization stages.
  • CD BioGlyco has good communication skills and maintains close contact with clients, promptly reports the progress and results of the O-GalNAc inhibitor project, and ensures clients' tracking and participation in the project.

CD BioGlyco has extensive experience in drug research and enzyme inhibitor development, especially the development of inhibitors for O-GalNAc transferase. We provide a full range of O-GalNAc inhibitor development support and solutions based on client needs. Please feel free to contact us if you're interested in the details of our development.


  1. Song, L.; Linstedt, A.D. Inhibitor of ppGalNAc-T3-mediated O-glycosylation blocks cancer cell invasiveness and lowers FGF23 levels. Elife. 2017, 6: e24051.
  2. Hang, H.C.; et al. Small molecule inhibitors of mucin-type O-linked glycosylation from a uridine-based library. Chemistry & Biology. 2004, 11(3): 337-345.
This service is for Research Use Only, not intended for any clinical use.

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