Click chemistry reactions are an important part of the medicinal chemistry toolbox, which is used in constructing compound libraries and helps to discover bioactive compounds and drugs. CD BioGlyco has extensive experience in the field of synthesis, and we provide efficient GlycoCLICK™-based drug development service.
We design click chemistry reaction protocols suitable for drug molecules according to specific needs. Copper-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry is a bioorthogonal reaction widely used in medicinal chemistry.
We synthesize the corresponding click reagents through chemical synthesis, enzymatic reaction, or biosynthesis. These reagents often include click-active groups and adapter sites, such as the synthesis of compounds with alkyne and azide groups.
We perform click reactions with click reagents and different substrate structures to achieve the synthesis of diverse compounds. The substrate is a compound in an existing compound library or a new compound designed and synthesized according to needs. Click-based reactions facilitate the rapid construction of compound libraries.
We use high-throughput screening technology to screen compound libraries and develop target compounds based on different targets and modes of action (such as targeting enzymes or lectins). This process helps to accelerate the drug development process.
We use enzymes as targets and use click technology to glycosylate enzymes, which changes the activity, stability, and specificity of enzymes, thereby developing selective and efficient enzyme inhibitors, For example, Protein Tyrosine Phosphatase (PTP) Inhibitor, Protein Kinase Inhibitor, Fucosyltransferase Inhibitor, Mannosyltransferase Inhibitor, Nicotinamide Phosphoribosyltransferase Inhibitor, O-GlcNAcase Inhibitor, Glycogen Phosphorylase Inhibitor, Glycosidase Inhibitor, and Neuraminidase Inhibitor. These inhibitors are widely applied in the fields of enzyme biological functions and drug development.
We use reliable carbohydrate click reactions to synthesize and modify carbohydrate compounds for the development and research of lectin ligands, for example, developing Galectin Inhibitor and Selectin Antagonist. The development of lectin ligands is of great significance for biological research.
We provide professional synthesis and purification for the compounds obtained through screening. Common purification methods include column chromatography, solvent extraction, and gel electrophoresis. At the same time, we conduct comprehensive structural characterization and analysis of the purified target compound to ensure its quality and purity, which may involve nuclear magnetic resonance, mass spectrometry, high-performance liquid chromatography (HPLC), and other technologies.
We evaluate the activity and pharmacokinetic properties of target compounds through appropriate biological experiments or in vitro tests, which help determine the pharmacological properties and potential pharmaceutical effects of the compound. In addition, we also provide mature GlycoCLICK™-based Drug Delivery Service.
Fig.1 GlycoCLICK™-based drug development service. (CD BioGlyco)
Technology: In situ click chemistry
Journal: European Journal of Medicinal Chemistry
IF: 7.088
Published: 2020
Results: The authors used HIV-1 RT as a target, synthesized a small combinatorial library using CuAAC reaction of click chemistry, and identified 22 effective HIV-1 NNRTIs through in situ screening. These compounds were then further synthesized and evaluated for their anti-HIV-1 activity in vitro. The results showed that A3N19 had the strongest activity against HIV-1 IIIB. The authors believed that the strategy of in situ click chemistry-based was suitable for the future discovery of more effective HIV-1 NNRTIs.
Fig.2 Discovery strategies for HIV-1 NNRTIs. (Kang, et al., 2020)
CD BioGlyco provides high-quality GlycoCLICK™-based drug development services. We respond quickly to market demand and flexibly adjust research directions and development strategies to meet clients' different drug development needs. Please feel free to
if you are interested in our development service.References