Kinases play a fundamental role in human biology, controlling many cellular processes through protein phosphorylation. Dysregulation of kinase function leads to diseases like cancer, inflammation and diabetes. Kinases are very similar in their active site architecture, which leads to cross-reactivity amongst kinase targeted small-molecule inhibitors.
It is important to determine the affinity and selectivity of such inhibitors to minimize off-target effects while optimizing desired selectivity profiles. Luceome’s KinaseSeeker™ is a high throughput screening and profiling service for evaluation of compounds against a panel of kinases.
Luceome’s kinase assay technology utilizes the luciferase fragment complementation, in which re-assembly of a split-protein leads to a functional luciferase enzyme and bioluminescence. In Luceome’s proprietary KinaseSeeker assay, the reassembly of the luciferase fragments is mediated by the interaction of a kinase with an active site dependent small molecule probe, where the competitive displacement of the probe by an inhibitor is measured by a change in luminescence signal. Luminescence readout translates into a highly sensitive and robust assay with low background and minimal interference from test compounds. The assay is a homogeneous binding assay, which enables rapid kinase profiling in a high-throughput format.