QTL launch non-radioactive kinase platform
Kinase platform and four new kinase Activity Assays, which uses a
unique polymer technology that does not require antibodies or
radioactive labels, providing a distinct advantage over current
homogeneous high-throughput kinase assays.
The kinase assays are ideal in targeting the molecular processes of the cell and to develop new future treatments for cancer, diabetes and other diseases. The kinase platform is built utilizing QTL's patented superquenching polymer technology which delivers universal mix and measure assays.
The superquenching technology consists of a QTL Sensor, which is comprised of highly fluorescent conjugated polymers co-located with phosphate coordinating metal ions on the surface of microspheres. As kinase substrates, peptides are used that contain a fluorescence quencher within their sequence. After the kinase phosphorylates the peptide substrate the phosphorylated product binds to the QTL Sensor resulting in superquenching of polymer fluorescence. The decrease in fluorescence is a measure of kinase enzymatic activity.
Eddie Wood, group leader in the kinase biochemistry group at GlaxoSmithKline said: "The QTL kinase assay has several key features that provide a distinct advantage over existing homogeneous high-throughput kinase assays."
"The PKC assay is non-radioactive, requires no specific antibody reagents to detect a phosphorylated product, and has a broad acceptable ATP concentration range. It is very sensitive enabling the use of 10-20 times less enzyme than my standard SPA format."
Protein kinases act as regulators of signal cascades that are central to cellular growth, differentiation and proliferation. These enzymes catalyze phosphorylation reactions by transferring a phosphate group from adenosine triphosphate (ATP) to one or more tyrosine, serine or threonine residues in protein substrates. Kinase pathways play an essential role in signal transduction and the control of metabolism, transcription, apoptosis and differentiation. As a result, kinases have been implicated in a number of diseases processes such as cancer, inflammation and diabetes. Over 500 different kinases have been identified, representing approximately 1.7 per cent of all human genes.
QTL's platform is compatible with standard fluorescent instrumentation and works with peptide or protein substrates.
QTL plan to release the PKC-alpha and Src assay, which are targeted at drugs for diabetes, leukaemia, and lymphoma. In addition there is the Akt 1 and P38-alpha, both targeted at drugs for cancer.
Building on the introduction of the QTL LightSpeed Kinase platform, the company plans to introduce an additional nine kinase assays during the next three months with rapid expansion continuing through 2005.
The Lightspeed Kinase platform, which includes assay buffer, sensor buffer, QTL Sensor, substrate and calibrator, is available now at QTL's website.
