Of chemical libraries and fireflies

To aid in the interpretation of HTS results derived from luciferase-based assays, we used quantitative HTS, an approach that defines the concentration-response behavior of each library sample, to profile the ATP-dependent luciferase from Photinus pyralis (lucPpy) against more than 70,000 samples. We...

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Veröffentlicht in:Assay and drug development technologies 2008-06, Vol.6 (3), p.322-322
1. Verfasser: Thomas, Craig
Format: Artikel
Sprache:eng
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Zusammenfassung:To aid in the interpretation of HTS results derived from luciferase-based assays, we used quantitative HTS, an approach that defines the concentration-response behavior of each library sample, to profile the ATP-dependent luciferase from Photinus pyralis (lucPpy) against more than 70,000 samples. We found that approximately 3% of the library was active, containing only compounds with inhibitory concentration-responses, of which 681 (0.9%) exhibited 50% inhibitory concentration (IC sub(50)) < 0 mu M. Representative compounds were shown to inhibit purified P. pyralis as well as several commercial luciferase-based detection reagents but were found to be largely inactive against Renilla reni-formis luciferase. Light attenuation by the samples was also examined and found to be more prominent in the blue-shifted bioluminescence produced by R. reniformis luciferase than in the bioluminescence produced by lucPpy. We describe the structure-activity relationship (SAR) of the luciferase inhibitors and discuss the use of these data in the interpretation of HTS results and configuration of luciferase-based assays.
ISSN:1540-658X