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Screening for androgen agonists using autonomously bioluminescent HEK293 reporter cells

Due to the public health concerns of endocrine-disrupting chemicals, there is an increasing demand to develop improved high-throughput detection assays for enhanced exposure control and risk assessment. A substrate-free, autobioluminescent HEK293(ARE/Gal4-Lux) assay was developed to screen compounds...

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Detalles Bibliográficos
Autores principales: Xu, Tingting, Gilliam, Madison, Sayler, Gary, Ripp, Steven, Close, Dan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8371548/
https://www.ncbi.nlm.nih.gov/pubmed/34350768
http://dx.doi.org/10.2144/btn-2021-0017
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author Xu, Tingting
Gilliam, Madison
Sayler, Gary
Ripp, Steven
Close, Dan
author_facet Xu, Tingting
Gilliam, Madison
Sayler, Gary
Ripp, Steven
Close, Dan
author_sort Xu, Tingting
collection PubMed
description Due to the public health concerns of endocrine-disrupting chemicals, there is an increasing demand to develop improved high-throughput detection assays for enhanced exposure control and risk assessment. A substrate-free, autobioluminescent HEK293(ARE/Gal4-Lux) assay was developed to screen compounds for their ability to induce androgen receptor (AR)-mediated transcriptional activation. The assay was validated against a group of 40 recommended chemicals and achieved an overall 87.5% accuracy in qualitatively classifying positive and negative AR agonists. The HEK293(ARE/Gal4-Lux) assay was demonstrated as a suitable tool for Tier 1 AR agonist screening. By eliminating exogenous substrate, this assay provided a significant advantage over traditional reporter assays by enabling higher-throughput screening with reduced testing costs while maintaining detection accuracy.
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spelling pubmed-83715482021-08-18 Screening for androgen agonists using autonomously bioluminescent HEK293 reporter cells Xu, Tingting Gilliam, Madison Sayler, Gary Ripp, Steven Close, Dan Biotechniques Article Due to the public health concerns of endocrine-disrupting chemicals, there is an increasing demand to develop improved high-throughput detection assays for enhanced exposure control and risk assessment. A substrate-free, autobioluminescent HEK293(ARE/Gal4-Lux) assay was developed to screen compounds for their ability to induce androgen receptor (AR)-mediated transcriptional activation. The assay was validated against a group of 40 recommended chemicals and achieved an overall 87.5% accuracy in qualitatively classifying positive and negative AR agonists. The HEK293(ARE/Gal4-Lux) assay was demonstrated as a suitable tool for Tier 1 AR agonist screening. By eliminating exogenous substrate, this assay provided a significant advantage over traditional reporter assays by enabling higher-throughput screening with reduced testing costs while maintaining detection accuracy. 2021-08-05 2021-08 /pmc/articles/PMC8371548/ /pubmed/34350768 http://dx.doi.org/10.2144/btn-2021-0017 Text en https://creativecommons.org/licenses/by-nc-nd/4.0/Open access This work is licensed under the Attribution-NonCommercial-NoDerivatives 4.0 Unported License. To view a copy of this license, visit http://creativecommons.org/licenses/by-nc-nd/4.0/ (https://creativecommons.org/licenses/by-nc-nd/4.0/)
spellingShingle Article
Xu, Tingting
Gilliam, Madison
Sayler, Gary
Ripp, Steven
Close, Dan
Screening for androgen agonists using autonomously bioluminescent HEK293 reporter cells
title Screening for androgen agonists using autonomously bioluminescent HEK293 reporter cells
title_full Screening for androgen agonists using autonomously bioluminescent HEK293 reporter cells
title_fullStr Screening for androgen agonists using autonomously bioluminescent HEK293 reporter cells
title_full_unstemmed Screening for androgen agonists using autonomously bioluminescent HEK293 reporter cells
title_short Screening for androgen agonists using autonomously bioluminescent HEK293 reporter cells
title_sort screening for androgen agonists using autonomously bioluminescent hek293 reporter cells
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8371548/
https://www.ncbi.nlm.nih.gov/pubmed/34350768
http://dx.doi.org/10.2144/btn-2021-0017
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