The growth of tumor cells is closely related to metastasis and sialylation or the expression of transferases. CMP-Sialic acid is a donor substrate in sialside synthesis that is transported into the Golgi by specialized transporters. Meanwhile, sialyltransferase catalyzes the ligation of sialic acid components to glycans on ceramide and glycoproteins. CMP-Sialic acid analog is a potent inhibitor with selective and broad inhibitory properties against glycosyltransferases. CD BioGlyco offers high-quality CMP-sialic acid analog-based sialylation inhibitor development services through the ideal molecular design and continuous optimization of processes. Furthermore, we utilize the high affinity of the donor and the high selectivity of the recipients to provide dual substrate analog inhibitor development services.
To tissue or delay glycosylation by competing donor-like inhibitors with natural glycosyl donors. Cytidine is essential for inhibitor binding to the enzyme, and we provide inhibitor development services containing cytidine moieties, such as CMP. Our professional researchers use phosphate or phosphate groups to suspend the cleavage of glycosidic bonds by replacing the reaction or use sialyl mimics that do not have glycosidic bonds to achieve the purpose of preventing glycosyl transfer.
At CD BioGlyco, we design a new class of donor analog inhibitors that include the invariant CMP moiety and a simple, easily accessible sialyl mimic. Glycosyldonors are potent inhibitors of glycosyltransferases, they bind well to the active site of the enzyme. Thus, potent inhibitors most likely occupy multiple binding sites simultaneously by facilitating the orientation and display of processing binding groups.
Our investigators provide high-quality development services of transition-state similar inhibitors based on the dynamics of glycosyl transfer mechanisms and isotopic effects in sialyltransferases.
Fig.1 Schematic diagram of CMP-sialic acid analog-based sialylation inhibitor. (CD BioGlyco)
Technology: High-throughput mass spectrometry analysis
Journal: Journal of Medicinal Chemistry
IF: 8.039
Published: 2010
Results: Based on high-throughput mass spectrometry analysis, authors develop a novel method for screening glycosyltransferase inhibitors. This method enables rapid sensitive screening of a large number of compounds with quantitative analysis. They were screening for carbohydrate transfer activity inhibition using different glycosyltransferases in the presence of the indicated receptor substrate. They found that the modification of sialic acid at positions C-5 and C-9 does not affect the dynamic mechanism of the glycosylation catalyzed by this enzyme. However, steroid analogs modified at the C-5 position of CMP-Neu5Ac had a strong effect on the catalysis of sialyltransferase. Mass spectrometry-based high-sensitivity analysis for screening and detection of human cancer cells K562 found this method to be feasible.
Fig.2 Compound inhibition analysis and high-throughput screening of compound profiles. (Hosoguchi, et al., 2010)
CD BioGlyco provides comprehensive Glycosylation Inhibitor Development services. Our professional solutions and attentive service are recognized by our clients worldwide. Moreover, we provide high-quality Fucosylation Inhibitor and Sialylation Inhibitor development services. If you need anything, please feel free to contact us.
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