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Title: Comparison of different androgen bioassays in the screening for environmental (anti)androgenic activity
Authors: Christiaens, Valerie ×
Berckmans, Pascale
Haelens, Anna
Witters, Hilda
Claessens, Frank #
Issue Date: Oct-2005
Publisher: Elsevier Science
Series Title: Environmental Toxicology and Chemistry vol:24 issue:10 pages:2646-2656
Abstract: Endocrine disruptors pose a growing threat to human and wildlife health. Validated test systems are required to study the mechanisms by which chemicals may interfere with the endocrine system. In order to identify compounds with (anti)androgenic activity, we used several in vitro bioassays, based on different androgen receptor (AR) functions, including AR transactivation and interaction between the amino-terminal domain and the ligand-binding domain. The AR activity assay, based on activation of the transcription of an androgen-responsive reporter gene in the presence of androgen, proved to excel in terms of high fold induction range and low minimal detection limit. The EC50 value, defined as the concentration that leads to half the maximal response and reflecting the potency of the synthetic androgen R1881 (methyltrienolone), was found to be 250 pM, consistent with the high affinity of this ligand to the human AR. A number of environmental samples were tested in the bioassay. The bioassay also could be used to detect antiandrogenic activity, because known AR-antagonists were able to inhibit R1881-mediated transactivation.
ISSN: 0730-7268
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Molecular and Vascular Biology
Biochemistry Section (Medicine) (-)
Laboratory of Molecular Endocrinology
Laboratory of Computational Biology
× corresponding author
# (joint) last author

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