PerkinElmer's new technology taps into a growing need for drug researchers who rely on kinases as a viable pharmaceutical target. The technology was developed to address market demand from the world's drug discovery labs for a non-radioactive, antibody-free, homogeneous assay solution for screening these orphan kinases.
Kinases play a key role in the regulation of critical cellular processes and are targeted in a number of diseases, such as cancer, inflammatory and metabolic disorders.
The firm's bead-based AlphaScreen technology can be used to study biological interaction using small molecules, large molecules and binding partners of various sizes.
With AlphaScreen, sensitive tyrosine kinase and serine/threonine kinase assays can be set up as well as interaction assays and homogeneous ELISAs in the well western analysis and NR assays.
AlphaScreen is homogenous, functional up to 200nM, measures/utilises low affinity interaction and is scalable for HTS and uHTS.
"In order to directly measure the phosphorylation of kinase substrates without antibodies or radioactivity, researchers have been restricted to small peptide fragments," said Ken King, vice president and general manager, Molecular Medicine, for >PerkinElmer's Life and Analytical Sciences division.
"Now, using the AlphaScreen PhosphoSensor technology, scientists can directly measure the phosphorylation of large protein substrates with high sensitivity and accuracy, and without radioactivity."
The new AlphaScreen PhosphoSensor complements other proprietary technologies such as LANCE, FlashPlates, and EasyLite Kinase, adding another kinase research tool to PerkinElmer's current offering.
The AlphaScreen technology is suitable for mixing and reading immunoassays (direct and indirect sandwich formats) with increased sensitivity and shortened time of assay (0.5-2 hours) as well as protein-protein binding assays (direct and indirect formats)
It has also proved durable and reliable in Protein-DNA binding assays (direct format), cellular pathway studies, in the well western analysis and molecular biology assays.
The AlphaScreen PhosphoSensor technology has been introduced as the Human Genome Project has revealed the existence of more than 500 unique genes encoding kinases, most of which do not have a known substrate and therefore no available antibody.
Known as orphan kinase genes, more than 90 per cent of this important group encodes serine kinases.