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Kinex™ Kinase Substrate Microarray (KKSM) Services

The vast majority of the proteins phosphorylated by specific protein kinases in humans and other species are unknown after more than 40 years of intense effort. However, with the emergence of protein kinases as one of the most promising families of drug targets in the pharmaceutical industry today, it is critical to define the proteins that are controlled by these important regulatory enzymes. In response to this challenge, Kinexus has developed a suite of diverse proteomics and bioinformatics services to permit identification of protein kinase substrates. Our Custom Kinase Substrate Peptide Profiling Service uniquely permits experimental definition of key substrate specificity determinants for most known human protein kinases. This permits the development of artificial substrates for protein kinases that may be useful for high throughput drug screening and can help identify physiological substrates of protein kinases of interest.

For kinase specificity profiling, our peptide microarray is superior to other more random peptide arrays that are available from competitors, because the peptide sequences on our microarrays have been pre-selected with our bioinformatics program at Kinexus. The kinase substrate peptide sequences were generated with a novel Kinase Predictor algorithm developed by Kinexus and its academic partners at the University of British Columbia and Simon Fraser University. The algorithm utilizes our in-house databases of the carefully aligned sequences of 488 human protein kinase catalytic domains and 10,000 known kinase-substrate phospho-site pairs. From this data and the application of our algorithm, we have been able to generate predicted phospho-site amino acid frequency matrices for all of these human protein kinase domains and define optimal peptide sequences for recognition by each of these protein kinases. These sequences have been used for the synthesis of the peptides that have been spotted on the Kinex™ Kinase Substrate Microarray chip.
With this flexible and convenient protein kinase specificity identification service, clients can send us their own preparations of protein kinases or choose from our vast collection of over 340 diverse and active human kinases. Each Kinex™ Kinase Substrate Microarray chip permits the testing of 3 different protein kinases and a control incubation that monitors the background binding of the phosphorylation detection stain to unphosphorylated peptides. Incubation of the Kinex™ Kinase Substrate Microarray with purified protein kinases results in the highest phosphorylation for those peptides that conform to the best structures for access to the active sites of these kinases. The phosphorylation of these peptides is detected with a commercial stain for bound phosphate that is measured with our fluorescent scanners and quantification software. Within three to four weeks of receipt of a client order, Kinexus will provide information about the best peptides from our panel of 445 optimal kinase substrate peptides.

Alignment of the amino acid sequences of the best performing peptides for a target kinase permits definition of the key positive determinants for specific kinase substrate recognition. The results from this unique service can be used to define signalling pathways impacted by specific kinases, identify reagents to enable kinase inhibitor discovery in vitro, and ascertain the effectiveness and specificity of kinase inhibitor drugs in living systems.

To obtain more information about our Kinex™ Kinase Substrate Microarrays please download our Customer Information Package for this service. After reviewing this package, interested clients should contact our Technical Services representatives toll free at 1-866-KINEXUS or by e-mail at