ST6Gal Inhibitor Development Service at CD BioGlyco

CD BioGlyco has a compound-rich natural product library, etc., to meet the needs of Glycosylation Inhibitor Development. Sialic acid is one of the most vital sugars in the human body after glucose. It plays a key role in intercellular recognition, adhesion, protein-lectin interaction, receptor binding, etc. Sialyltransferase (ST) mediates the synthesis of sialic acid-containing glycoconjugates. ST6Gal is a type of ST that adds α2,6-conjugated sialic acid to galactose residues of N-glycans. We provide ST6Gal inhibitor development services in multiple orientations. Our goal is to screen compounds from natural products or high throughput for high inhibitory activity even at high concentrations of ST6Gal substrates.

Fig.1 Classes of ST6Gal inhibitor development. (CD BioGlyco)

• Substrate analog-based ST6Gal inhibitor development service

Different STs catalyze different chemical bonds and receptor substrates. Based on the differences in bond and receptor substrates, several types of ST inhibitors have been developed. Among them, transition state analogs have relatively good inhibitory activity. Based on the receptor specificity of ST6Gal, we screen, design, and synthesize transition-state analogs, dual-substrate analogs, donor analogs, and acceptor analogs that effectively inhibit ST6Gal based on CMP-Neu5Ac or acceptor oligosaccharides.

• Natural product-based ST6Gal inhibitor development service

Natural products, including aromatic compounds, Flavonoids, Lithocholic Acid Analogs, etc., have a variety of biological activities such as antioxidant, anticancer and antibacterial. Their natural products have excellent biological activities and specific active skeletons and active groups, which are important resources for inhibitor development. Our natural product library contains a rich variety of compounds. Rare natural products, selected products, and natural product analogs are available, which fully meet the needs of ST6Gal inhibitor development.

Publication

Technology: Computer-aided drug design

Journal: Bioorganic & Medicinal Chemistry

IF: 2.429

Published: 2017

Results: In this study, a series of uridine analogs were designed and synthesized by coupling hetaryl α-hydroxyphosphonates and coupling aryl with a 5'-amino-5'-deoxyuridine fragment. The design strategy for this class of compounds was to replace the phosphodiester junction with carbamate and cytidine with uridine. Five of these compounds were tested and found to exhibit inhibitory activity against recombinant human ST6Gal I. This study provides a new compound design idea for the development of ST inhibitors.

Tab.1 Affinity of CMP Neu5Ac (K_m) to recombinant hST6Gal I and inhibition data for selected compounds. (Montgomery, et al., 2017)

Applications of ST6Gal Inhibitor Development

• The developed ST6Gal inhibitor is used to study carbohydrate-selectin interactions.
• Cell surface sialic acid expression levels are highly correlated with cancer. The developed ST6Gal inhibitor is expected to be a valuable chemical tool for the discovery of novel anti-cancer drugs.

Highlights of Us

• During the design and screening of our compound libraries, we employ a range of methods to ensure the high specificity and diversity of our compound libraries.
• Our diverse compound libraries fulfill a wide range of uses such as high-throughput screening by researchers, control studies, etc.
• We have an experienced inhibitor development team and a well-established client project management system to ensure high quality and timely delivery of research results.

CD BioGlyco uses computer-aided drug design and high-throughput screening in the development of glycosylation inhibitors. In addition to ST6Gal inhibitors, we also provide ST3Gal Inhibitors, ST8Sia Inhibitors, and other inhibitor development services. Please feel free to contact us to inquire about any object of inhibitor development. We guarantee to give you the best quality ST6Gal Inhibitor development service.