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The androgen receptor (AR) is a nuclear receptor that functions as a ligand-activated transcription factor. It mediates the effects of androgens, such as testosterone and dihydrotestosterone, regulating gene expression involved in male sexual development, reproductive function, and various other physiological processes including hair growth, muscle mass, bone density, and cardiovascular health. Aberrant AR signaling is implicated in prostate cancer and androgen insensitivity syndrome, making it a significant therapeutic target.
Androgens bind to the AR, causing a conformational change, dissociation from chaperone proteins, translocation to the nucleus, dimerization, binding to androgen response elements (AREs) on DNA, and modulation of gene transcription. Anti-androgens competitively inhibit androgen binding to the AR, preventing AR activation and downstream signaling.
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