The Design, Synthesis and Potential Utility of Fluorescence Probes that Target DFG-out Conformation of p38α for High Throughput Screening Binding Assay.

Autor:	Tecle, Haile, Feru, Frederic, Hu Liu, Kuhn, Cyrille, Rennie, Glen, Morris, Mark, Jiangxing Shao, Cheng, Alan C., Gikunju, Diana, Miret, Juan, Coli, Rocco, Xi, Simon, Clugston, Susan L., Low, Simon, Kazmirski, Steven, Yuan-Hua Ding, Qing Cao, Johnson, Theresa L., Deshmukh, Gayatri D., DiNitto, Jonathan P.
Předmět:	DRUG development HIGH throughput screening (Drug development) MOLECULAR dynamics FLUORESCENCE ENZYME inhibitors
Zdroj:	Chemical Biology & Drug Design; Dec2009, Vol. 74 Issue 6, p547-559, 13p, 7 Diagrams, 3 Charts, 1 Graph
Abstrakt:	The design, synthesis and utility of fluorescence probes that bind to the DFG-out conformation of p38α kinase are described. Probes that demonstrate good affinity for p38α, 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 p38α 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. [ABSTRACT FROM AUTHOR]
Databáze:	Complementary Index
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