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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...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
2021
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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. |
format | Online Article Text |
id | pubmed-8371548 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
record_format | MEDLINE/PubMed |
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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