Androgen receptor is the intracellular protein that mediates biological actions of physiological androgens (testosterone and 5 alpha-dihydrotestosterone). Androgen receptor belongs to a large family of ligand-dependent proteins whose function is to modulate expression of genes and gene networks in a cell- and tissue-specific manner. The present overview describes the structurally important domains of the receptor protein, and discusses several aspects in the structure-function relationship, using naturally occurring receptor mutants in androgen insensitivity patients or experimental animals as examples. In addition, characteristics of androgen receptor expressed in a heterologous system are described, and their potential usefulness in specific molecular studies discussed.