Target intelligence / Profile preview

Androgen Receptor (AR)

Target
AR
Molecular classification
Nuclear receptor, Transcription factor, Steroid hormone receptor
01

Overview

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.

Other names
Dihydrotestosterone receptorNuclear receptor subfamily 3, group C, member 4NR3C4
02

Mechanism of action

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.

03

Biological functions

Transcriptional regulationMale sexual developmentRegulation of gene expressionRegulation of hair growthRegulation of sex driveRegulation of muscle massRegulation of bone densityRegulation of cardiovascular healthRegulation of immune functionHematopoiesisNervous system activityHomeostasis
04

Disease associations

Prostate cancerBladder cancerLiver cancerKidney cancerLung cancerAndrogen insensitivity syndromeInfertility
05

Safety considerations

Androgen deprivation therapy side effects (e.g., sexual dysfunction, fatigue, bone loss)Resistance to anti-androgen therapiesOff-target effects of AR-modulating drugsCardiovascular side effectsCognitive impairment
06

Interacting drugs

Testosterone

4 more in the full profile.

07

Biomarkers

AR expression levels in tumor tissuePSA (prostate-specific antigen)AR mutationsAR splice variants

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