Core 2 Inhibitor Development Service at CD BioGlyco

Core 1 branches through the core 2 β1,6-N-acetylglucosaminyltransferase (C2GnT) family to form core 2, and core 2 O-glycans serve as scaffolding structures for sialyl-Lewis x. High levels of C2GnT contribute to the increase in core 2 O-glycan structure, which plays a key role in cell adhesion and cell migration. CD BioGlyco provides mature core 2 inhibitor development service.

• Target enzyme screening service

CD BioGlyco uses efficient high-throughput screening technology and computational methods to screen potential target enzyme inhibitor candidates from our compound library.

• Molecular design and synthesis

CD BioGlyco will conduct structure-activity relationship studies on the screened enzyme inhibitors, and our scientists will design and synthesize new core 2 inhibitor candidates and optimize their pharmaceutical properties. We have developed a potent C2GnT1 inhibitor, the substrate Galβ1-3GalNAcα-p-nitrophenyl (PNP), which acts as an effective inhibitor of C2GnT1 under UV irradiation at 350 nm. We have verified that other PNP-sugar derivatives also act as specific inhibitors of C2GnT1. In addition, we also have developed a divalent imidazolium salt compound, which is a new class of glycosyltransferase inhibitors that selectively inhibits the synthesis of core 2.

• Bioactivity evaluation service

CD BioGlyco evaluates the biological activity, selectivity, and toxicological properties of core 2 inhibitors through specialized in vitro cell and animal model experiments. We also provide core 2 inhibitors research service on the mechanism of action including cell signaling pathway analysis or protein interaction research.

Fig.1 Core 2 inhibitor development service. (CD BioGlyco)

Publication

Technology: Western blot analysis

Journal: Biochimica et Biophysica Acta (BBA)-General Subjects

IF: 4.117

Published: 2013

Results: The authors expressed recombinant soluble human galactose (Gal) and N-acetylglucosamine (GlcNAc) transferases that synthesize O-glycan core 2. The authors determined the properties and substrate specificity of the enzyme using synthetic receptor substrate analogs and tested them as inhibitors. The results showed that imidazolium salt effectively inhibited C2GnT1.

Fig.2 Inhibition of human C2GnT1 with different concentrations of bis-imidazolium salt inhibitors. (Gao, et al., 2013)

Applications

• Research tools: Core 2 inhibitors are used as research tools to study the molecular mechanisms of glycan regulation, interactions, and interrelationships with related proteins and cells.
• Research on disease mechanisms: By using core 2 inhibitors, the functional loss or inhibition of core 2 sugar chain synthase is simulated, thereby helping researchers gain a deeper understanding of the pathogenesis of diseases related to core 2 sugar chains. For example, core 2 inhibitors are applied to study the invasion and metastasis mechanisms of tumor cells.
• Drug screening and discovery: Core 2 inhibitor development service provides support for drug screening and discovery. By designing and synthesizing core 2 inhibitors with different structures, and conducting drug screening and evaluation, potential drug candidates for the diseases related to core 2 sugar chain abnormalities may be found.

Advantages

• CD BioGlyco has a team of multidisciplinary experts in organic chemistry, medicinal chemistry, biology, etc., they collaborate across fields and provide a one-stop core 2 inhibitor development service.
• CD BioGlyco has established relevant cell model and animal model experimental solutions to provide professional core 2 inhibitors evaluation and verification service.
• We strictly adhere to quality control and compliance standards to ensure the reproducibility and reliability of our core 2 inhibitor development process.

CD BioGlyco has established reliable Glycosylation Inhibitor Development Solutions, and we tailor the core 2 inhibitor development strategy according to client needs. Please feel free to contact us promptly if you would like to inquire about specific inhibitor development content.