Androgens sculpture the male and female body in a number of ways, and androgen receptor (AR) regulates these events in a tissue-specific fashion by activation or repressing specific genes and gene networks. However, the regulatory mechanisms involved are not well understood. AR is a hormone-dependent transcription factor that belongs to the superfamily of nuclear receptors. The pharmacology of steroid hormones, such as androgens, is tripartite, in that it includes hormone-dependent interactions with (i) the receptor, (ii) DNA sequences, and (iii) coregulatory proteins. For many known nuclear receptors, including the steroid receptor subfamily (androgen, estrogen, progesterone, glucocorticoid, and mineralocorticoid receptors), current evidence points to formation of large, multi-component complexes in the nucleus, at the promoter and/or enhancer region of a target gene, to elicit regulation of gene expression. This presentation deals with various aspects of androgen signaling and highlights some novel aspects of AR function that have emerged from recent genome-wide studies on AR binding and androgen signaling.