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Journal of Biomolecular Screening
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Synthesis and Characterization of 5'-p-fluorosulfonylbenzoyl-2' (or 3')-(biotinyl)adenosine as an Activity-Based Probe for Protein Kinases

Steven J. Ratcliffe

High Throughput Chemistry, Stevenage, GlaxoSmithKline, UK

Tracey Yi

Sanjay S. Khandekar

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

Most of the kinase inhibitors that are approved for therapeutic uses or that are undergoing clinical trials are directed toward the adenosine triphosphate (ATP) binding site of protein kinases. 5'-Fluorosulfonylbenzoyl 5'-adenosine (FSBA) is an activitybased probe (ABP) that covalently modifies a conserved lysine present in the nucleotide binding site of most kinases. Here the authors describe synthesis of FSBA derivatives, 2'-biotinyl-FSBA and 3'-biotinyl-FSBA as kinase ABPs, and delineate a Western blot method to screen and validate ATP competitive protein kinase inhibitors using biotinyl-FSBA as a nonselective activity-based probe for protein kinases.

Key Words: kinase inhibitors • biotinyl-FSBA • LC/MS • activity-based probes • Western blot • ATP binding site

This version was published on February 1, 2007

Journal of Biomolecular Screening, Vol. 12, No. 1, 126-132 (2007)
DOI: 10.1177/1087057106296685
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