Fluorescence based-assays have greatly facilitated high-throughput screening (HTS) in drug discovery. However, in doing so, they created a bottleneck relating to false positives and false negatives, which may arise due to interferences from light scattering, inner filter effects, and compound fluorescence. Unlike fluorescence intensity, a fluorescence lifetime-based measurement is resistant to light scattering and inner filter effects, and provides the selectivity needed to discriminate the target fluorescence signal from background fluorescence. In Phase I we will demonstrate a homogenous fluorescence lifetime-based kinase assay that is resistant to fluorescence interferences and does not require the use of antibodies. Overcoming fluorescence interferences will cut costs associated with secondary screening and assist quicker identification of lead compounds. Furthermore, it will create an opportunity to screen compound libraries and/or natural products that are known to have some fluorescent properties, but were previously inaccessible by means of traditional fluorescence-based methods. Kinases are a major class of drug targets, which are involved in human diseases such as cancer, diabetes, and arthritis. This technology will advance the speed and efficiency in which we can find drugs to treat these important diseases.
Thesaurus Terms: Drug Discovery /Isolation, Fluorescence, High Throughput Technology, Protein Kinase, Technology /Technique Development Chemical Binding, Cyclic Amp, Fluorescent Dye /Probe, Ionophore, Iron Compound, Light Scattering, Phosphopeptide, Phosphorylation
