Evaluation of a rapid in vitro androgen receptor transcriptional activation assay using AR-EcoScreen™ cells

QSAR Model for Androgen Receptor Antagonism - Data from CHO Cell Reporter Gene Assays

“…The data originates primarily from our laboratory of the National Food Institute, the Technical University of Denmark (laboratory 1) [4,42,45,48,49] Comparison of common data from the different laboratories showed a 83% (29/35)-91% (40/44) agreement. The compounds "2,4,5-trichlorophenoxyacetic acid" and "di-n-butyl phthalate" were indicated as weak AR antagonisms by Araki et al [46] and this was in agreement with the finding in Vinggaard et al [4], classifying the compound as negative. The remaining data was further evaluated.…”

“…CHO data from literature: The data in the training set is comprised of experimental AR antagonism data from 15 publications [2][3][4]37,[39][40][41][42][43][44][45][46][47][48][49]. The data represents a wide range of chemical structures and various functions and covers natural hormones, synthetic hormones and drugs, pesticides, Polyaromatic hydrocarbons (PAHs), polychlorinated biphenyls (PCBs), brominated flame retardants (BFRs), plasticizers and plastic additives, food additives and cosmetics, antioxidants, plant compounds, roast mutagens and various industrial chemicals.…”

Androgenic and Antiandrogenic Effects of Alkylphenols and Parabens Assessed Using the Reporter Gene Assay with Stably Transfected CHO-K1 Cells (AR-EcoScreen System)

“…We have reported the AR-reporter gene assay using two different types of stably transfected Chinese hamster ovary (CHO) cells (CHO-K1 cells do not metabolize steroid hormones and do not express endogenous steroid hormone receptors), AREcoScreen, which expresses androgen-inducible luciferase, and c-luc, which expresses it without the need for hormonal induction. 9,10) This method enabled us to detect simultaneously the hormonal effects and cell toxicity of the test chemicals. This reporter gene assay is useful for high-throughput screening of androgen agonists and antagonists because of the high reproducibility and sensitivity.…”

Estrogenic and Anti-Androgenic Activities of Benzophenones in Human Estrogen and Androgen Receptor Mediated Mammalian Reporter Gene Assays

“…[14][15][16][17] They can detect the transcriptional activities mediated with the human estrogen receptor α (hERα) or androgen receptor (hAR). In this study, we investigated the estrogenic and anti-androgenic activities of benzophenone and 19 hydroxylated benzophenones using these cell lines.…”

“…[14][15][16][17] To evaluate the cell viability from test chemicals, the cLucEcoScreen™ cell was stably transfected luciferase gene (pcDNA-luc) into CHO-K1 cells, which constitutively expressed luciferase without any induction. 16,17) They are cultured in assay medium composed of D-MEM/F12 (Invitrogen, CA, U.S.A.) without phenol red, and supplemented with 5% charcoaldextran treated FBS (Hyclone, UT, U.S.A.). The cells were grown at 37°C in an atmosphere containing 5% CO 2 /95% air under saturating humidity and passaged every 3-4 days by trypsinization with 0.25% …”