At CD BioGlyco, our team of scientists specializes in the development of Enzyme Inhibitors using a variety of click chemistry reactions, including Protein Kinase Inhibitor, mannosyltransferase inhibitors, Neuraminidase Inhibitors, etc. Mannosyltransferase acts on mannose and plays a role in various physiological and pathological processes. The development of its inhibitors helps to dissect the function of different mannosyltransferases. We provide a high-quality mannosyltransferase inhibitor development service to fulfill the mannosyltransferase-related research needs of our clients.
We utilize click chemistry reactions and fragment pro-inhibitor library screening to develop efficient enzyme inhibitor libraries for mannosyltransferase. Due to the efficiency of the click reaction and water compatibility, in most cases, the assembled products are screened directly for inhibition. The copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) is one of our most commonly used click chemistry reactions. We synthesize a variety of derivative libraries by CuAAC that are used for the development of mannosyltransferase inhibitors, including guanosine monophosphate library, carbohydrate-based triazole library, etc. The compounds with inhibitory activity against mannosyltransferase are then screened in high throughput by molecular docking mimicry and enzyme kinetic screening.
Technology: Click chemistry
Journal: PLoS One
IF: 2.74
Published: 2012
Results: In this study, researchers report an assay that can screen mannosyltransferase inhibitors from a compound library. Several mannosyltransferase inhibitors were screened by this screening method from a guanosine monophosphate library constructed by click chemistry. This study provides an effective strategy for the development of mannosyltransferase inhibitors.
Fig.1 Biphenyl-based mono/diphosphonucleotide triazole adducts. (Van Der Peet, et al., 2012)
HTS is one of the commonly used techniques in drug design to discover possible lead compounds from a library of compounds, thereby greatly accelerating the compound screening process. It rapidly tests thousands to millions of samples, validating activity at the molecular, cellular, or model organism level, screening small molecule compounds, mixtures, natural products, etc., of known structure.
CuAAC is a commonly used click chemistry reaction in enzyme inhibitor development, which has various advantages such as simple operation, high selectivity, mild reaction conditions, simple purification, and structural diversity in high yields. In addition to this, the triazolyl compounds synthesized by CuAAC have good physical and chemical properties. Therefore, CuAAC is often used to synthesize various compound libraries to develop enzyme inhibitors.
CD BioGlyco offers a one-stop mannosyltransferase inhibitor development service based on extensive experience in click chemistry. Please feel free to
for more information about mannosyltransferase inhibitor development. Our scientists will answer your questions and provide any technical consultation regarding the design and synthesis of the inhibitor that suits your needs.Reference