Kinex™ Protein Kinase Microarrays
Protein kinases are well recognized by the pharmaceutical and biotech industries as fruitful targets for drugs to potentially treat over 400 human diseases. Presently, over 150 kinase inhibitors are being tested in human clinical trials, and at least another 500 appear to be undergoing pre-clinical studies in animal models. While there are at least 515 human protein kinases, only about 75 have been seriously targeted by Pharma. Consequently, there are exciting possibilities for the identification of new kinase drug targets and new applications for existing drugs.
Counter screening protein kinases to establish the specificity of promising therapeutic inhibitors of target kinases has previously been a costly exercise. Now with our proprietary Kinase Microarray Screening service, this can be done quickly and expensively by Kinexus for our clients. For as low as $1.66 per compound per kinase with triplicate measurements, over 150 different human kinases can be profiled for inhibition of the binding of an ATP analogue by up to 3 compounds per microarray (or 2 compounds and a control).
The ability of a compound to reduce binding of ATP analogues to the active site of protein kinases is a strong indication that the compound will act as an inhibitor of protein kinase activity. The compound may act as a competitive inhibitor of ATP binding, or it could induce conformational changes that close access to the active site.
Counter screening protein kinases to establish the specificity of promising therapeutic inhibitors of target kinases has previously been a costly exercise. Now with our proprietary Kinase Microarray Screening service, this can be done quickly and expensively by Kinexus for our clients. For as low as $1.66 per compound per kinase with triplicate measurements, over 150 different human kinases can be profiled for inhibition of the binding of an ATP analogue by up to 3 compounds per microarray (or 2 compounds and a control).
The ability of a compound to reduce binding of ATP analogues to the active site of protein kinases is a strong indication that the compound will act as an inhibitor of protein kinase activity. The compound may act as a competitive inhibitor of ATP binding, or it could induce conformational changes that close access to the active site.
Our ATP analogue probe better resembles the actual structure of ATP than staurosporin-based binding probes that are used by our competitors.
Any specific kinases that are shown to be targeted by certain compounds with our Kinase Microarray Screening service can be further validated for direct effects in vitro on the enzymatic activities of these kinases with our Kinase-Inhibitor Activity Profiling service. Using our Kinase-Substrate Profiling service, endogenous physiological substrates of target kinases can be defined so that the effects of drug leads can be evaluated in vivo in cultured cells and tissues from treated animals.
Our Kinase Microarray Screening service can also be used to test the specificity of suspected protein kinase-protein interactions. In one example, the kinase microarray is incubated with a target recombinant protein that is fluorescently tagged to reveal its binding on the chip. In another examples, a biotinylated pseudosubstrate peptide based on a phosphorylation site can be used to probe the kinase microarray to identify candidate kinases that target this site. Clients should contact Kinexus for a quotation on these applications of the Kinex™ Protein Kinase Microarray. Kinexus can produce these recombinant proteins and synthetic peptides with our Custom Protein and Peptide Production Services.
Any specific kinases that are shown to be targeted by certain compounds with our Kinase Microarray Screening service can be further validated for direct effects in vitro on the enzymatic activities of these kinases with our Kinase-Inhibitor Activity Profiling service. Using our Kinase-Substrate Profiling service, endogenous physiological substrates of target kinases can be defined so that the effects of drug leads can be evaluated in vivo in cultured cells and tissues from treated animals.
Our Kinase Microarray Screening service can also be used to test the specificity of suspected protein kinase-protein interactions. In one example, the kinase microarray is incubated with a target recombinant protein that is fluorescently tagged to reveal its binding on the chip. In another examples, a biotinylated pseudosubstrate peptide based on a phosphorylation site can be used to probe the kinase microarray to identify candidate kinases that target this site. Clients should contact Kinexus for a quotation on these applications of the Kinex™ Protein Kinase Microarray. Kinexus can produce these recombinant proteins and synthetic peptides with our Custom Protein and Peptide Production Services.
Download Kinex™ Protein Kinase Microarray Services Fillable Forms in .doc format.
