Aromatic Compound-based Sialylation Inhibitor Development at CD BioGlyco

Aromatic compounds inhibit anticancer and anti-inflammatory therapeutically relevant salivary acid transferase, which is central to the process of sialylation. Therefore, at CD BioGlyco, we screen aromatic compounds to develop sialylation inhibitors and test their inhibitory effects.

• Inhibitor screening service
  We screen aromatic compounds involved in the synthesis of sialyltransferase, as well as those with the ability to bind specifically to sialyltransferase, by high-throughput screening or computer-assisted methods. A library of sialylation inhibitors is constructed and evaluated for activity.
• Inhibitor modification service
  Based on the screening of aromatic compounds for sialylation inhibitors, we provide liquid chromatography (LC), nuclear magnetic resonance (NMR) techniques, infrared (IR), and mass spectrometry (MS) to analyze their structures.
  Then, we optimize their structures using chemical and biological methods to expand the library of salivation inhibitors.
• Inhibitor testing and analysis service
  • Reversibility: We test the reversibility of the inhibition of the sialyltransferase by aromatic compounds using dialysis and buffer solutions. In this procedure, we replace the compounds with DMSO as a control.
  • Inhibitory activity: First, we determine the sialyltransferase activity by scintillation proximity assay (SPA). The enzyme activity is recorded without the addition of aromatic compounds. Secondly, after the addition of aromatic compounds, the sialyltransferase activity is again measured. The inhibitory effect of aromatic compounds on sialyltransferase is obtained by this comparison.

Fig.1 Aromatic compound-based sialylation inhibitor development services. (CD BioGlyco)

Publication

Technology: Tests on the inhibitory effect of gallic acid and its derivatives on transferases

Journal: Archives of Biochemistry and Biophysics

IF: 3.9

Published: 2004

Results: By screening the natural products, gallic acid (GA), (−)-epigallocatechin gallate (EGCG), ellagic acid (EA), and other related aromatic compounds were identified as inhibitors of fucosyltransferase VII. As shown, the inhibition isotherms for GA and EGCG shifted to the left as the preincubation time of the enzymatic reaction increased. Overnight (15 h) preincubation of these aromatic compounds and the enzyme before the start of the reaction with guanosine diphosphate-[³H] provided a stable and more effective inhibition of the transferase. Under these conditions, the semi-inhibitory concentration values of GA, EA, and EGCG were 0.06, 1.2, and 0.7 μM, respectively.

Fig.2 Structures of GA, EA, and EGCG. (Niu, et al., 2004)

Applications

• Aromatic compound-based sialylation inhibitors can be used to study physiological activities such as inhibition of cell adhesion, and apoptosis in tumor cells.
• Aromatic compound-based sialylation inhibitors can be used for the development of probe molecules in glycobiology studies.
• Sialylation inhibitors based on aromatic compounds can be used in the study of antitumor or immunomodulatory drugs.

Advantages

• Our inhibitor development technology is proven and our development programs are comprehensive to ensure client satisfaction.
• We are knowledgeable in the development of salivary acidification inhibitors of aromatic compounds and help our clients in inhibitor development.

CD BioGlyco has extensive expertise in the field of Glycosylation Inhibitor Development, providing reliable glycosylation inhibitor development services to our clients. We develop numerous types of inhibitors including but not limited to Metabolic Interconversion Inhibitor, Capping Modification Inhibitor, and glycosylation inhibitor. If you are interested in our services, please feel free to contact us.