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Journal of Biomolecular Screening
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12/5/628    most recent
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High-Throughput Mass Spectrometry Screening for Inhibitors of Phosphatidylserine Decarboxylase

Chris D. Forbes

Department of Research Technologies, Bayer Pharmaceuticals Corporation, West Haven, CT

Joshuaine G. Toth

Department of Research Technologies, Bayer Pharmaceuticals Corporation, West Haven, CT

Can C. Özbal

BioTrove, Inc., Woburn, MA

William A. Lamarr

BioTrove, Inc., Woburn, MA

Jennifer A. Pendleton

Department of Research Technologies, Bayer Pharmaceuticals Corporation, West Haven, CT

Sandra Rocks

Department of Research Technologies, Bayer Pharmaceuticals Corporation, West Haven, CT

Richard W. Gedrich

Department of Research Technologies, Bayer Pharmaceuticals Corporation, West Haven, CT

David G. Osterman

Department of Research Technologies, Bayer Pharmaceuticals Corporation, West Haven, CT

James A. Landro

Department of Research Technologies, Bayer Pharmaceuticals Corporation, West Haven, CT

Kevin J. Lumb

Department of Research Technologies, Bayer Pharmaceuticals Corporation, West Haven, CT, kevin.lumb.b{at}bayer.com

A high-throughput mass spectrometry assay to measure the catalytic activity of phosphatidylserine decarboxylase (PISD) is described. PISD converts phosphatidylserine to phosphatidylethanolamine during lipid synthesis. Traditional methods of measuring PISD activity are low throughput and unsuitable for the high-throughput screening of large compound libraries. The high-throughput mass spectrometry assay directly measures phosphatidylserine and phosphatidylethanolamine using the RapidFireTM platform at a rate of 1 sample every 7.5 s. The assay is robust, with an average Z' value of 0.79 from a screen of 9920 compounds. Of 60 compounds selected for confirmation, 54 are active in dose-response studies. The application of high-throughput mass spectrometry permitted a high-quality screen to be performed for an otherwise intractable target. (Journal of Biomolecular Screening 2007:628-634)

Key Words: high-throughput screening • mass spectrometry • phosphatidylserine decarboxylase

This version was published on August 1, 2007

Journal of Biomolecular Screening, Vol. 12, No. 5, 628-634 (2007)
DOI: 10.1177/1087057107301320
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This article has been cited by other articles:


Home page
 J Biomol ScreenHome page
R. Rathore, J. Corr, G. Scott, P. Vollmerhaus, and K. D. Greis
Development of an Inhibitor Screening Platform via Mass Spectrometry
J Biomol Screen, December 1, 2008; 13(10): 1007 - 1013.
[Abstract] [PDF]