GlycoCLICK™-based Fucosyltransferase Inhibitor Development Service
Accelerating Your Research with Fucosyltransferase Inhibitor Development
CD BioGlyco provides one-stop click chemistry-based Enzyme Inhibitor development services, including Protein Tyrosine Phosphatase (PTP) Inhibitors, fucosyltransferase (FUT) inhibitors, Glycogen Phosphorylase Inhibitors, etc. FUT plays an important role in various physiological and pathological processes. The development of FUT inhibitors has been used as an effective strategy to study the physiological function of FUT and the treatment of diseases. We provide a one-stop FUT inhibitor development service to support our client's related research.
We develop inhibitors of various FUTs such as α-1,3-fucosyltransferase and α 1,6-fucosyltransferase. After synthesizing various compound libraries by click chemistry, we perform high-throughput screening by various assays such as bioluminescence assay, molecular docking simulation, and enzyme kinetic screening. Finally, FUT inhibitors with selective and efficient inhibitory activities are obtained through screening. Different FUTs have different substrate preferences. Based on the mechanism by which FUTs function, we develop acceptor-substrate and donor-substrate analogs, dual-substrate inhibitors, non-substrate inhibitors, non-guanosine diphosphate-related inhibitors, etc. Our development strategy is as follows:
- We prepare GDP-triazole libraries by attaching GDP-derived acetylene to azide libraries via a Cu(I)-catalyzed cycloaddition reaction between acetylene reactants and azide. After that, FUT inhibitors with good selectivity and inhibitory effects are subsequently obtained by in situ screening.
- We screen libraries of compounds constructed by 1,3-dipolar cycloaddition of various alkynes with desired azidosugar nucleotides for FUT inhibitors with good inhibitory effects and selectivity.
Publication Data
Technology: High-throughput screening
Journal: Molecules
IF: 4.927
Published: 2021
Results: In this study, the inhibition of FUT and O-GlcNAc transferase (OGT) was tested using UDP-Glo and GDP-Glo bioluminescence assays. The results showed that the method was resistant to chemical interference, robust, and highly sensitive. The application of bioluminescent biochemical assay in the high-throughput screening of enzyme inhibitors such as FUT was finally validated experimentally.
Fig.1 Detection of glycosyltransferase inhibitor effect. (Engel, et al., 2021)
Applications
- FUT inhibitors provide a valuable tool for the study of cell metabolism, cell-cell adhesion, immune regulation, etc.
- Abnormal expression of FUT is present in many cancer cells. FUT inhibitors are potential drugs for the treatment of cancer.
- FUT inhibitors are used to study the function of fucose-containing glycans in various biological processes.
Advantages of Us
- We provide very tailored and personalized FUT inhibitor development programs according to the different needs of our clients.
- We synthesize multiple libraries of compounds for high-throughput screening of FUT inhibitors.
- We develop FUT inhibitors through computer-aided drug design, which greatly reduces project cycle time and improves efficiency.
At CD BioGlyco, our extensive click chemistry experience ensures that inhibitor development programs move forward quickly. Please feel free to contact us to learn more about FUT inhibitor development. Our rigorous and comprehensive quality management system ensures high-quality project delivery.
Reference
- Engel, L.; et al. Utility of bioluminescent homogeneous nucleotide detection assays in measuring activities of nucleotide-sugar dependent glycosyltransferases and studying their inhibitors. Molecules. 2021, 26(20): 6230.
For research use only. Not intended for any clinical use.
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