In Vitro Androgen Receptor Modulation Assay

Androgen Receptor modulation and its measurement in vitro:

• The androgen receptor (AR) is a nuclear receptor activated by binding either testosterone or dihydrotestosterone in the cytoplasm and translocating to the nucleus¹.
• Environmental contaminants such as industrial and agricultural chemicals have been shown to alter androgen receptor (AR) function through agonistic or antagonistic modulation.
• Androgen disruptors can lead to reduced sperm count, infertility, prostate cancer and can interfere with normal male development.
• AR agonists and some antagonists induce nuclear translocation. This can be detected using GFP-tagged proteins which are monitored in the cytoplasm and nucleus of the cells. The assay can also detect nuclear foci (punctuate distribution in the nucleus) which is characteristic of AR agonists.
• The in vitro Androgen Receptor (AR) modulation assay can be applied as a therapeutic screening assay (e.g., in the development of prostate cancer therapies) or to assess potential endocrine disruption effects.

_{1) Hua Y, et al, (2014) High-content positional biosensor screening assay for compounds to prevent or disrupt androgen receptor and transcriptional intermediary factor 2 protein-protein interactions. ASSAY Drug Dev Technol 12(7); 395-418
2) Tan MHE et al., (2015) Androgen receptor: structure, role in prostate cancer and drug discovery. Acta Pharmacologica Sinica 36; 3-23}