Test No. 458: Stably Transfected Human Androgen Receptor Transcriptional Activation
Assay for Detection of Androgenic Agonist and Antagonist Activity of Chemicals
This Test Guideline describes in vitro assays, which use Androgen Receptor TransActivation
(ARTA) to detect Androgen Receptor Agonists and Antagonists. The ARTA assay methods
are mechanistically and functionally similar test methods that provide information
on the transcription and translation of a reporter gene following the binding of a
chemical to the androgen receptor and subsequent transactivation. The cell lines used
in these assays express AR and have been stably transfected with an AR-responsive
luciferase reporter gene, and are used to identify chemicals that activate (i.e. act
as agonist) or inhibit (i.e. act as antagonists) AR-dependent transcription. Some
chemicals may, in a cell type-dependent manner, display both agonist and antagonist
activity and are known as selective AR modulators. The AR is activated following ligand
binding, after which the receptor-ligand complex binds to specific DNA responsive
elements and transactivates the receptor gene, resulting in an increase cellular expression
of the luciferase enzyme. The enzyme then transforms the substrate to a bioluminescent
product that can be quantitatively measured with a luminometer. This Test Guideline
includes ARTA assays using the AR-EcoScreenTM cell line, the AR-CALUX® cell line,
and 22Rv1/MMTV_GR-KO cell line.
Published on June 29, 2020Also available in: French
In series:OECD Guidelines for the Testing of Chemicals, Section 4: Health Effectsview more titles