Chemical biology & drug design, 2009-12, Vol.74 (6), p.547-559
2009
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Details
- Autor(en) / Beteiligte
- Titel
- 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.
- Sprache
- Englisch
- Identifikatoren
- eISSN: 1747-0285DOI: 10.1111/j.1747-0285.2009.00884.xTitel-ID: cdi_proquest_miscellaneous_734138927
- Format
- –
- Schlagworte
- Binding Sites, Computer Simulation, Crystallography, X-Ray, Fluorescent Dyes - chemical synthesis, Fluorescent Dyes - chemistry, Fluorescent Dyes - pharmacology, High-Throughput Screening Assays, Kinetics, Mitogen-Activated Protein Kinase 14 - chemistry, Mitogen-Activated Protein Kinase 14 - metabolism, Naphthalenes - chemistry, Naphthalenes - pharmacology, Protein Kinase Inhibitors - chemical synthesis, Protein Kinase Inhibitors - chemistry, Protein Kinase Inhibitors - pharmacology, Pyrazoles - chemistry, Pyrazoles - pharmacology, Structure-Activity Relationship