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Journal of Biomolecular Screening
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HTRF-Based Assay for Microsomal Prostaglandin E2 Synthase-1 Activity

Eric R. Goedken

Abbott Bioresearch Center, Worcester, Massachusetts, eric.goedken{at}abbott.com

Andrew I. Gagnon

Abbott Bioresearch Center, Worcester, Massachusetts

Gary T. Overmeyer

Abbott Bioresearch Center, Worcester, Massachusetts

Junjian Liu

Abbott Bioresearch Center, Worcester, Massachusetts

Richard A. Petrillo

Abbott Bioresearch Center, Worcester, Massachusetts

Andrew F. Burchat

Abbott Bioresearch Center, Worcester, Massachusetts

Medha J. Tomlinson

Abbott Bioresearch Center, Worcester, Massachusetts

Microsomal prostaglandin E2 synthase-1 (mPGES-1) catalyzes the formation of prostaglandin E2 (PGE2) from the endoperoxide prostaglandin H 2 (PGH2). Expression of this enzyme is induced during the inflammatory response, and mouse knockout experiments suggest it may be an attractive target for antiarthritic therapies. Assaying the activity of this enzyme in vitro is challenging because of the unstable nature of the PGH 2 substrate. Here, the authors present an mPGES-1 activity assay suitable for characterization of enzyme preparations and for determining the potency of inhibitor compounds. This plate-based competition assay uses homogenous time-resolved fluorescence to measure PGE2 produced by the enzyme. The assay is insensitive to DMSO concentration up to 10% and does not require extensive washes after the initial enzyme reaction is concluded, making it a simple and convenient way to assess mPGES-1 inhibition. (Journal of Biomolecular Screening 2008:619-625)

Key Words: prostaglandin synthase • microsomal prostaglandin E2 synthase-1 • homogenous time-resolved fluorescence • prostaglandin E2 • prostaglandin H2

This version was published on August 1, 2008

Journal of Biomolecular Screening, Vol. 13, No. 7, 619-625 (2008)
DOI: 10.1177/1087057108321145
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