Domain functions of the androgen receptor.

Molecular cloning of the androgen receptor cDNA has facilitated analysis of structure/function relationships of this ligand activated transcription factor. Amplification of mutant androgen receptor DNA using the polymerase chain reaction has revealed single base and deletion mutations in the androgen receptor gene that cause the androgen insensitivity syndrome in rats and humans. Site directed mutagenesis of the NH2-terminal and hinge regions indicates specific sequences required for full transcriptional activation and nuclear targeting of the androgen receptor. Finally, transient transfection systems have shown that the antiandrogen cyproterone acetate is both an agonist and antagonist, while hydroxyflutamide acts only as an antagonist and thus is a pure antiandrogen.