Galectins act through a "receptor"-"ligand" mechanism during apoptosis and metastasis of tumor cells. The use of carbohydrates to develop relevant inhibitors effectively interferes with the galectin and ligand binding pathway. At CD BioGlyco, we provide systematic Lectin Ligand Development Services that are effectively integrated with Drug Development Services. Here, we provide our clients with high-quality carbohydrate click-based galectin inhibitor development services.
We utilize Cu(I)-assisted cycloaddition reactions of alkynes and azides to generate linear oligogalactopyranosides and use them to construct libraries of galectin inhibitors. The conditions throughout the reaction are mild and efficient, no protecting groups are required, and purification is not necessary in most cases.
Throughout the process, we provide animal models or cellular models for in vitro experiments to analyze the inhibitory activity and semi-inhibitory concentration values of galectin inhibitors in the library. We also provide fluorescent labeling methods to analyze the binding sites of compounds in the inhibitor library to the carbohydrate recognition domain (CRD) of galectin.
Fig.1 Process of developing galectin inhibitors based on carbohydrate clicks. (CD BioGlyco)
Technology: Click chemical methods, X-ray crystallography
Journal: Chemical Biology & Drug Design
IF: 3.0
Published: 2020
Results: The authors synthesized a linear oligogalactoside by simple click chemistry. Not only does it mimic the polygalactosamine sequence expressed on the surface of eukaryotic cells, but it is also capable of specifically recognizing the extracellular form of galectin 3. The next authors describe the X-ray crystal structure of the galactoglucan lectin 3 CRD in complex with synthesized di- and tri-galactopyranosides, confirming the binding of these compounds within the carbohydrate-binding site. Initial structures indicate that binding interactions occur primarily in the galactose portion of the nonreducing end, mainly in the C and D sites of the CRD. In contrast to oligogalactosamine, the latter binds more consistently throughout the groove formed by the five substituents of the galactagogue 3 CRD.
CD BioGlyco has extensive experience in click chemistry research. With our first-class click chemistry technology, we provide our clients with high-quality drug development services. For example, inhibitor development, antagonist development, and so on. If you are interested in our click chemistry services, please feel free to
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