α-1,3-Fucosyltransferase Inhibitor Development Service at CD BioGlyco

Fucoidan glycosylation is often the final step in the biosynthesis of many oligosaccharides and glycoconjugates that are essential for various biological processes in eukaryotes. Fucosyltransferases play a key role in the process of fucosylation genesis. At CD BioGlyco, we will provide comprehensive α-1,3-fucosyltransferase inhibitor development services.

• We utilize fluorescently labeled substrates for the fucosylation reaction to probe the onset of fucosylation and screen for compound molecules that bind to α-1,3-fucosyltransferase.
• We design and optimize the structures of these molecules and examine their inhibitory capabilities.
• We establish α-1,3-fucosyltransferase inhibitor libraries to provide clients with high-throughput screening of α-1,3-fucosyltransferase inhibitors.

In addition, we offer in vivo and in vitro studies of α-1,3-fucosyltransferase inhibitors.

• In vivo: The inhibitor is injected into a variety of mouse tumor models to examine the anti-tumor activity it exhibits.
• In vitro: Its inhibitory effects are examined by flow cytometry and fluorescent labeling.

Fig.1 Development process for the α-1,3-fucosyltransferase inhibitors. (CD BioGlyco)

Publication

Technology: Single-cell ultrahigh-throughput screening method

Journal: Science Advance

IF: 13.6

Published: 2019

• Results: A fluorescence-activated cell sorting system was developed for ultra-high-throughput screening of α-1,3-fucosyltransferases, and a companion strategy was designed to evaluate the screening performance of the system. After three rounds of directed evolution, a mutant M32 of α-1,3-fucosyltransferases was identified, which synthesized Lewis x and 3'-fucosylated fructose with 6-fold and 14-fold higher catalytic efficiency (kcat/Km), respectively. At the same time, the structure of the M32 mutant shows that it produces a pincer-like structure that appears to improve the binding of the galactopyranose ring of the receptor substrate. This explains the increased activity of α-1,3-fucosyltransferase when it catalyzes fucosylation.

Fig.2 Fucosylation reactions catalyzed by fucosylation enzymes. (Tan, et al., 2019)

Advantages

• We have custom R&D solutions.
• We develop α-1,3-fucosyltransferase inhibitors with high purity.
• We provide not only the development of α-1,3-fucosyltransferase inhibitors but also in vivo and in vitro studies of the inhibitors.

CD BioGlyco provides professional Glycosylation Inhibitor Development services to our clients. Our development techniques are efficient and comprehensive in type, helping our clients to solve their challenges in glycosylation inhibitors. If you are interested in our services, please feel free to contact us for more details.