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Journal of Biomolecular Screening
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Article

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

Steven J. Ratcliffe1, Tracey Yi2, Sanjay S. Khandekar2*

1 High Throughput Chemistry, Stevenage, GlaxoSmithKline, UK.
2 Gene Expression and Protein Biochemistry, GlaxoSmithKline King of Prussia, PA.

* To whom correspondence should be addressed. E-mail: sanjay.khandekar-1{at}gsk.com.


  Abstract

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 activity-based 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

First published on December 8, 2006, doi:10.1177/1087057106296685

Journal of Biomolecular Screening 2007;12:126.

A more recent version of this article appeared on February 1, 2007

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