Wholeheartedly Dedicated Protein Kinase Inhibitor Development Service for Clients

CD BioGlyco specializes in the development of Enzyme Inhibitors using a variety of click chemistry reactions, including Protein Tyrosine Phosphatase (PTP) Inhibitor, Protein Kinase (PK) Inhibitor, Fucosyltransferase Inhibitor, and others. PK are key regulators of cellular function and constitute one of the most diverse and largest gene families. We offer a high-quality PK inhibitor development service based on our extensive experience in click chemistry. We develop corresponding inhibitors with high selectivity according to the type of PK.

PK is in turn activated by signals such as increased Ca²⁺ concentration, diacylglycerol, etc. Based on this, we develop a variety of PK inhibitors through click chemistry, including bisubstrate-based PK inhibitors, noncompetitive inhibitors, etc. The strategies we develop include the following:

• We use alkyne/azide-derived purine analogs to click various aromatic azides/alkynes and screen them to obtain compounds with efficient inhibitory activity.
• We synthesize dual-substrate-based kinase inhibitors using arginine residues with acetylene or azide portions on their side chains. The bis-substrate kinase inhibitors obtained by screening show good affinity and selectivity.
• We synthesize two types of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates by click chemistry and screen them for PK inhibitors.
• We use click chemistry as a synthetic tool to synthesize bisaryl maleimide derivatives from which we screen compounds with inhibitory activity against PK.
• We use click chemistry to generate azide libraries from which we screen efficient PK inhibitors.

Publication Data

Applications

• PK catalyzes the phosphorylation of tyrosine, serine, threonine, and histidine residues of proteins. Aberrant PK expression is associated with a variety of diseases, including cancer and inflammation. PK inhibitors are used to study the mechanisms of development of these diseases.
• PK inhibitors are used to study disease therapeutics.
• PK inhibitors help to explore the regulatory mechanisms.

Advantages of Us

• We have extensive and in-depth expertise in click chemistry and extensive experience working with complex compounds.
• We have high-throughput screening capabilities, which significantly reduce inhibitor screening time.
• We combine computer-aided drug design and click chemistry to develop PK inhibitors, which improve development efficiency.

CD BioGlyco develops a variety of innovative enzyme inhibitors through click chemistry. Please feel free to contact us to learn more about PK inhibitor development. Our experienced click chemistry scientists will customize a proprietary inhibitor development program to meet your needs.

• GlycoCLICK™-based Protein Tyrosine Phosphatase (PTP) Inhibitor Development Service
• GlycoCLICK™-based Fucosyltransferase Inhibitor Development Service
• GlycoCLICK™-based Mannosyltransferase Inhibitor Development Service
• GlycoCLICK™-based Nicotinamide Phosphoribosyltransferase Inhibitor Development Service
• GlycoCLICK™-based O-GlcNAcase Inhibitor Development Service
• GlycoCLICK™-based Glycogen Phosphorylase Inhibitor Development Service
• GlycoCLICK™-based Glycosidase Inhibitor Development Service
• GlycoCLICK™-based Neuraminidase Inhibitor Development Service