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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
Descripción
Sumario: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.