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Journal of Biomolecular Screening
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A Liquid Chromatography/Mass Spectrometry-Based Method for the Selection of ATP Competitive Kinase Inhibitors

Sanjay S. Khandekar

Bingbing Feng

Tracey Yi

Gene Expression and Protein Biochemistry, GlaxoSmithKline, King of Prussia, PA.

Susan Chen

Chemical, Analytical and Structural Sciences, GlaxoSmithKline, King of Prussia, PA.

Nicholas Laping

CVU CEDD, Glaxo Smith Kline, King of Prussia, PA.

Neal Bramson

Assay Development and Compound Profiling, Glaxo Smith Kline, RTP, North Carolina

The currently approved kinase inhibitors for therapeutic uses and a number of kinase inhibitors that are undergoing clinical trials are directed toward the adenosine triphosphate (ATP) binding site of protein kinases. The 5ß-fluorosulfonylbenzoyl 5'-adenosine (FSBA) is an ATP-affinity reagent that covalently modifies a conserved lysine present in the nucleotide-binding site of most kinases. The authors have developed a liquid chromatography/mass spectrometry-basedmethod tomonitor binding ofATP competitive protein kinase inhibitors using FSBAas a nonselective activity-based probe for protein kinases. Their method provides a general, rapid, and reproducible means to screen and validate selective ATP competitive inhibitors of protein kinases.

Key Words: kinase inhibitors • FSBA • LC/MS • activity-based probe • ATP binding site

Journal of Biomolecular Screening, Vol. 10, No. 5, 447-455 (2005)
DOI: 10.1177/1087057105274846
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S. J. Ratcliffe, T. Yi, and S. S. Khandekar
Synthesis and Characterization of 5'-p-fluorosulfonylbenzoyl-2' (or 3')-(biotinyl)adenosine as an Activity-Based Probe for Protein Kinases
J Biomol Screen, February 1, 2007; 12(1): 126 - 132.
[Abstract] [PDF]