High-throughput AR dimerization assay identifies androgen disrupting chemicals and metabolites.

ABSTRACT: Introduction: Analysis of streamlined computational models used to predict androgen disrupting chemicals revealed that assays measuring androgen receptor (AR) cofactor recruitment/dimerization were particularly indispensable to high predictivity, especially for AR antagonists. As the original dimerization assays used to develop the minimal assay models are no longer available, new assays must be established and evaluated as suitable alternatives to assess chemicals beyond the original 1,800+ supported by the current data. Here we present the AR2 assay, which is a stable, cell-based method that uses an enzyme complementation approach. Methods: Bipartite domains of the NanoLuc luciferase enzyme were fused to the human AR to quantitatively measure ligand-dependent AR homodimeriz

SUBMITTER: Brown EC 

PROVIDER: S-EPMC10112521 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature