Androgens affect the growth and development of a wide variety of cell types in both males and females and produce their effects by binding to androgen receptors, which modulate the transcription of specific genes. Testosterone is the major active androgen circulating in blood, but in many tissues it is metabolized by 5alpha-reductase to 5alpha-dihydrotestosterone, which binds to and activates the androgen receptor. Androgen receptors are members of the nuclear receptor family of transcription factors, and these nuclear receptors control transcription by recruitment of a variety of co-activators and co-repressors. Mutations in the androgen receptor and 5alpha-reductase can affect male sexual development. 5alpha-Reductase is also critical for parturition and fetal survival in mice. Inhibitors of 5alpha-reductase are being used increasingly to treat some androgen-dependent disorders. Because androgens also suppress the growth of certain cancer cells, they might also have a role in treating prostate cancer.