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Review
. 2015 May;33(3):225-34.
doi: 10.1055/s-0035-1552989. Epub 2015 Jun 2.

Cell-based assays for screening androgen receptor ligands

Carmela Campana  1 , Vincenzo Pezzi  2 , William E Rainey  1
Affiliations
Review

Cell-based assays for screening androgen receptor ligands

Carmela Campana et al. Semin Reprod Med. 2015 May.

Abstract

The androgen receptor (AR, NR3C4) mediates the majority of androgen effects on target cells. The AR is activated following ligand binding that result is enhanced of target gene transcription. Several cell-based model systems have been developed that allow sensitive detection and monitoring of steroids or other compounds with AR bioactivity. Most cell-based AR reporter models use transgenic gene constructs that include an androgen response element that controls reporter gene expression. The DNA cis-regulatory elements that respond to AR share sequence similarity with cis-regulatory elements for glucocorticoid (GR, NR3C1), mineralocorticoid (MR, NR3C2), and progesterone (PGR, NR3C3) receptors, which has compromised AR selectivity for some models. In recent years, the sensitivity and selectivity of AR bioassays have been significantly improved through careful selection of cell models, utilization of improved reporter genes, and the use of yeast two-hybrid AR systems. This review summarizes and compares the currently available androgen-responsive cell model systems.

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Figures

Figure 1
Figure 1. Cell-based bioassays for the study of AR activity
(A) Models using native androgen receptor rely on ligand/antagonist effects on AR regulation of reporter gene transcription. AR binding causes translocation of the cytosolic AR into the nucleus and its binding to androgen responsive elements that drive a variety of reporters. Models are available that use GFP, luciferase or β-galactosidase. (B) Models using yeast-two-hybrid system for determining androgen activity and activation of reporter gene transcription. Androgen binding causes the translocation of cytosolic AR receptor hybrid, [GAL4 DNA binding domain (DBD)/AR ligand binding domain (LBD)] into the nucleus and its binding and activation of GAL4 promoter-driven luciferase, β-galactosidase or β-lactamase reporter systems.
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