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Combinatorial Chemistry & High Throughput Screening

Editor-in-Chief

ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

Development and Application of Fluorescence Polarization Assays in Drug Discovery

Author(s): T. J. Burke, K. R. Loniello, J. A. Beebe and K. M. Ervin

Volume 6, Issue 3, 2003

Page: [183 - 194] Pages: 12

DOI: 10.2174/138620703106298365

Price: $65

Abstract

Fluorescence polarization technology has been used in basic research and commercial diagnostic assays for many decades, but has begun to be widely used in drug discovery only in the past six years. Originally, FP assays for drug discovery were developed for single-tube analytical instruments, but the technology was rapidly converted to high-throughput screening assays when commercial plate readers with equivalent sensitivity became available. This review will discuss fluorescence polarization assays in current use in drug discovery research as well as those in development that will likely be used in the near future. These assays include targets such as kinases, phosphatases, proteases, G-protein coupled receptors, and nuclear receptors.

Keywords: Fluorescence polarization, phosphatases, proteases, G-protein


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