Journal
JOURNAL OF BIOMOLECULAR SCREENING
Volume 10, Issue 5, Pages 447-455Publisher
SAGE PUBLICATIONS INC
DOI: 10.1177/1087057105274846
Keywords
kinase inhibitors; FSBA; LC/MS; activity-based probe; ATP binding site
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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 5'-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-based method to monitor binding of ATP competitive protein kinase inhibitors using FSBA as 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.
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