Protein Activator & Inhibitor Screening Service

Profacgen offers a comprehensive list of high-throughput screening services for the identification of potential protein activators & inhibitors to accelerate our customer’s preclinical drug development process.

Proteins participate in numerous physiological activities through a comprehensive network, including signal transduction, cell surface recognition and protein modification. To determine possible activator/inhibitor(s) of a certain protein, Profacgen has developed a highly efficient screening system to select candidates by the detection of fluorescence, chemo-luminescence or isotopic signal. Generally, the candidate molecules will be selected or synthesized, which is followed by immobilization on a solid surface. Detection is performed after incubation with the target protein according to the specific experimental setting.

Our protein targets includes all kinds of enzymes ranging from kinase, phosphatase, methyltransferase, glycosyltransferase, acetyltransferase to proteases, etc. You can profile your target protein (enzymes) against thousands of substrate compounds or proteins, or study various types of post-modification, like methylation, nitrosylation, NEDDylation, phosphorylation, SUMOylation and ubiquitination. Profacgen offers versatile substrates with extensive species origins including human, rat, mouse, bovine and chicken, etc. We also possess phosphorylation library containing different phosphorylation sites (threonine/serine/tyrosine) for the recognition of kinases/phosphatases. Our target protein (enzyme) screening service will enhance the discovery and identification processes for novel downstream protein binding partners.

Besides, Profacgen is also capable of offering activator or inhibitor screening service by adding the mixture of candidate compounds with target enzyme into the substrate. Effect of candidate compounds on the kinetics of a given enzymatic reaction can be then quantified by EC50 or IC50 determination compared to control groups.

Application of Protein Activator & Inhibitor Screening Service:

• Identification of (novel) substrates for known/orphan/new enzymes
• Identification of phosphorylation or proteolytic sites
• Elucidation of signal transduction pathways
• Evaluation of enzyme activators / inhibitors
• Enzyme profiling in disease states or under treatments (drug, growth factors, hormones, etc.)
• Fingerprinting difference in substrate specificity among different enzymes

Please contact us for more details of our preclinical protein activator/inhibitor screening service. Our experts will provide and help design an optimal solution for your screening project and trouble-shooting for you throughout the whole process.