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. 2015 May 1;14:99. doi: 10.1186/s12943-015-0346-9

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© Allen et al.; licensee BioMed Central. 2015

This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.

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Identification of TRAIL-inducing compounds by high-throughput luciferase reporter screen. (a) Plot of reporter induction versus signal for screen conducted with the NCI Diversity Set II at 1 μM in HCT116 Bax^−/− cells that stably express a luciferase gene reporter construct under transcriptional control of the first 504 base pairs of the human TRAIL gene promoter. Induction is expressed as luminescence relative to DMSO-treated cells. The horizontal red line represents the cutoff for selection. (b) Validation of reporter induction for candidate screen hits in HCT116 Bax^−/− cells at multiple doses and time points. Reporter signal is expressed relative to DMSO-treated cells and normalized to cell viability. The horizontal red line represents the cutoff for selection. Data represent an average of three replicates. The horizontal red line represents the cutoff for selection. (C) Molecular structures of the selected TRAIL-inducing compounds.