Abstract:
: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.
journal_name
Chem Biol Drug Desjournal_title
Chemical biology & drug designauthors
Tecle H,Feru F,Liu H,Kuhn C,Rennie G,Morris M,Shao J,Cheng AC,Gikunju D,Miret J,Coli R,Xi SH,Clugston SL,Low S,Kazmirski S,Ding YH,Cao Q,Johnson TL,Deshmukh GD,DiNitto JP,Wu JC,English JMdoi
10.1111/j.1747-0285.2009.00884.xsubject
Has Abstractpub_date
2009-12-01 00:00:00pages
547-59issue
6eissn
1747-0277issn
1747-0285pii
JPP884journal_volume
74pub_type
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