Identifying androgen receptor antagonists using a metabolically competent high-throughput screening assay.

ABSTRACT: Androgen receptor (AR) is a nuclear receptor with a well-established role in sexual function and development. Modifications in AR can lead to endocrine disruption, cancer, and other diseases, making it imperative to identify compounds that influence these changes. AR modulators have been identified using immortalized cell lines in a high-throughput screening assay. However, most of these methods do not incorporate metabolism, leading to misclassification of compounds that normally require it to become AR modulators. Metabolism transforms exogenous parent compounds into metabolites that are easier to excrete, and normally less active than the parent. However, some metabolites modulate AR more effectively than the parent compound. Incorporating metabolism into a large compound screen can ide

SUBMITTER: Lynch C 

PROVIDER: S-EPMC12818260 | biostudies-literature | 2026

REPOSITORIES: biostudies-literature