Acceptor Analog-based Glycosphingolipid Inhibitor Development Service

Acceptor Analog-based Glycosphingolipid Inhibitor Development Service

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CD BioGlyco is experienced in the development of Glycosphingolipid (GSL) Inhibitors. GSL has important biological functions such as maintaining the stability of the plasma membrane, mediating cell recognition and adhesion, regulating signal transduction, etc. Specific GSLs are found to be aberrantly expressed in many tumor diseases and involved in related molecular mechanisms. The development of GSL inhibitors is one of the ways to study its physiological function and so on. The advantage of receptor analogs is that they should be selective for specific enzymes. It has also become one of the directions for inhibitor development. We provide receptor analog-based GSL inhibitor development services.

Fig.1 Process for receptor analog-based GSL inhibitor development. (CD BioGlyco)Fig.1 Process for receptor analog-based GSL inhibitor development. (CD BioGlyco)

  • Ceramide analog development services
    We aim to synthesize compounds with strong structural homology to ceramides, such as iminosugars with two or three alkyl chains. Such compounds mimic the ceramide receptor during Glucosylceramide Synthase (GCS) catalysis and thus act as competitive inhibitors. By studying the inhibitory effects of compounds on GCS, etc., effective GSL inhibitors are screened.
  • Other receptor analog development services
    It is found that compounds with greater structural homology may have stronger inhibitory effects. We have a specialized library of compounds for inhibitor development, which contains a variety of natural products and synthetic compounds. We utilize computer simulation to screen receptor analogs and study the mechanism of inhibition.

Publication

Technology: Synthesis of ceramide analogs

Journal: Tetrahedron: Asymmetry

IF: 2.126

Published: 2005

Results: In the present study, several iminosugars bearing two or three alkyl chains were synthesized. These compounds are ceramide mimics and have some inhibitory effect on GCS. The present study also examined the effect of the position and length of the alkyl chains on the inhibitory effect of GCS. The results showed that the addition of a second alkyl chain did not improve their inhibitory activity. The compounds containing two octyl chains (13b, 14b, and 7b) showed the best inhibitory effect.

Fig.2 Inhibitory effect on GCS. (Boucheron, et al., 2005)Fig.2 Inhibitory effect on GCS. (Boucheron, et al., 2005)

Applications

  • Abnormalities in GSL metabolism contribute to the development of some diseases. GSL inhibitors developed based on receptor analogs are used in the research of disease pathogenesis.
  • The development of GSL inhibitors based on receptor analogs contributes to the study of intracellular GSL catabolism and metabolism.
  • The development of GSL inhibitors with high efficiency, low toxicity, and more stable performance is a hot spot in therapeutic research for cancer and other diseases. GSL inhibitors developed based on receptor analogs are used for disease studies.

Advantages

  • Our compound libraries for glycosylation inhibitor development include tens of thousands of natural products, synthetic compounds, and more.
  • Our high-throughput screening capabilities have greatly improved the efficiency of inhibitor development through computer-assisted screening.
  • GSL inhibitors based on receptor analogs are readily taken up by cells, which contributes to the research of sphingolipid-related diseases.

At CD BioGlyco, our Glycosylation Inhibitor development services are well established. Our experienced scientists will customize a solution to meet your needs. Feel free to contact us with your needs. We will be happy to help you with all your glycosylation inhibitor development needs.

Reference

  1. Boucheron, C.; et al. Design and synthesis of iminosugar-based inhibitors of glucosylceramide synthase: the search for new therapeutic agents against Gaucher disease. Tetrahedron: Asymmetry. 2005, 10(16): 1747-1756.
This service is for Research Use Only, not intended for any clinical use.

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CD BioGlyco is a world-class biotechnology company with offices in many countries. Our products and services provide a viable option to what is otherwise available.

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