Glycan Sulfation Inhibitor Development

Glycan Sulfation Inhibitor Development

Glycan Sulfation Inhibitor Development Services at CD BioGlyco

Sulfation modification of glycans is one of the major modes of chemical modification of glycans, and sulfation-modified glycans tend to have excellent biological activities. Abnormal glycan sulfation leads to disease. At CD BioGlyco, we are dedicated to the development of Postsynthetic Glycan Modification Inhibitors and provide our clients with glycan sulfation inhibitor development services.

  • Exploration of glycan sulfation modifications
    Sulfation modification of glycans is controlled by a family of sulfotransferases. All sulfotransferases have a binding site, as well as different receptor binding sites. CD BioGlyco provides fluorescent probe technology to trace the course of action of sulfotransferases to clarify the mechanism of glycan sulfation.
  • Development of glycan sulfation inhibitors
    We have developed glycan sulfation inhibitors by targeting sulfotransferases.
    • High-throughput screening
      We provide a fluorescent labeling method to preliminarily screen subject scaffold structures with inhibitory effects and analyze their inhibitory ability in cells.
    • Kinetic analysis
      We provide a first-level kinetic analysis technique to compare the inhibitory effects of different sulfotransferases on the production of glycosylation based on the obtained kinetic constants and reaction speed values, as well as to explore the inhibitory mechanism of the inhibitors.
    • Optimization and validation
      We optimize and validate different compounds in plates. The half inhibitory concentration values and inhibitory effects of different inhibitors are compared to optimize the inhibitor with optimal inhibitory effect.

Fig.1 Development process of glycan sulfation inhibitors. (CD BioGlyco)Fig.1 Development process of glycan sulfation inhibitors. (CD BioGlyco)

Publication

Technology: Chemo-biological approach to the development of glycosaminoglycans (GAG) sulfotransferase-based inhibitors

Journal: ACS Chemical Biology

IF: 4

Published: 2017

Results: The authors report on the process of developing a cell permeability-selective small molecule inhibitor of GAG sulfotransferase. After a series of experiments, it was demonstrated that the molecule specifically inhibits GAG sulfotransferase in vitro, decreasing cell surface chondroitin sulfate-E and overall sulfation levels while secreting chondroitin sulfate proteoglycans (CSPGs) and reversing CSPG-mediated axonal growth inhibition. These studies pave the way for a new set of pharmacological tools for interrogating GAG sulfation-dependent processes and may represent a new therapeutic approach to nerve regeneration.

Applications

  • The development of glycan sulfation inhibitors can be applied to research the signaling pathways of glycans in cells or the mechanism of inducing the expression of a gene or protein.
  • Glycan sulfation inhibitors can be used as key structural elements for protein recognition and regulation of downstream signaling.
  • Glycan sulfation inhibitors can be used to probe the immune response of an organism.

Advantages

  • We have a high sensitivity to keep up with the trend of glycobiology and update our inhibitor R&D technology on time.
  • We have a systematic R&D platform for Glycosylation Inhibitors and provide custom R&D solutions for our clients.
  • We have complete pre-sale and after-sale services to help clients solve the problems in glycosylation inhibitor research as much as possible.

CD BioGlyco has constructed a strong R&D solution for glycosylation inhibitors, and our professional research team provides custom R&D solutions for clients. We are researching most of the organism's glycans to ensure that the applications of the developed glycosylation inhibitors are wide-ranging. We hope to be your good helper in the field of glycobiology. Please feel free to contact us for more detailed information.

Reference

  1. Cheung, S.T.; et al. Discovery of a small-molecule modulator of glycosaminoglycan sulfation. ACS Chemical Biology. 2017, 12(12): 3126-3133.
This service is for Research Use Only, not intended for any clinical use.

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