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The design, synthesis and potential utility of fluorescence probes that target DFG-out conformation of p38alpha for high throughput screening binding assay
Ist Teil von
Chemical biology & drug design, 2009-12, Vol.74 (6), p.547-559
Ort / Verlag
England
Erscheinungsjahr
2009
Quelle
Wiley Online Library Journals Frontfile Complete
Beschreibungen/Notizen
The design, synthesis and utility of fluorescence probes that bind to the DFG-out conformation of p38alpha kinase are described. Probes that demonstrate good affinity for p38alpha, have been identified and one of the probes, PF-04438255, has been successfully used in an high throughput screening (HTS) assay to identify two novel non-classical p38alpha inhibitors. In addition, a cascade activity assay was utilized to validate the selective binding of these non-classical kinase inhibitors to the unactive form of the enzyme.