Target intelligence / Profile preview

Androgen receptor (AR) (AR)

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

Overview

The Androgen receptor (AR) is a ligand-dependent transcription factor and a member of the nuclear receptor superfamily (UniProt P10275). It mediates the biological effects of androgens, such as testosterone and dihydrotestosterone, which are critical for male sexual differentiation, pubertal development, and the maintenance of bone and muscle mass (StatPearls NBK557562). In the context of prasterone (DHEA), the AR is activated by androgenic metabolites produced through the enzymatic conversion of DHEA within peripheral tissues, a process known as intracrinology (PubChem CID 5881). The AR is a major therapeutic target in oncology, where its signaling drives the progression of prostate cancer, and in endocrinology for conditions like androgen insensitivity syndrome (NCBI Gene 367). Because prasterone can also be converted into estrogens, it indirectly interacts with estrogen receptors (ERα and ERβ), making the "prasterone-derived" pathway relevant for treating conditions like vulvovaginal atrophy. Pharmacological modulation of the AR includes the use of direct agonists for replacement therapy and potent antagonists or synthesis inhibitors to treat androgen-dependent malignancies.

Other names
NR3C4Nuclear receptor subfamily 3 group C member 4Dihydrotestosterone receptorDHTRAndrogen receptor
02

Mechanism of action

Ligand-activated transcription factor that regulates gene expression by binding to androgen response elements (AREs) in the promoter regions of target genes.

03

Biological functions

Signal transductionCell proliferationSexual developmentGene expression regulationBone and muscle maintenance
04

Disease associations

Prostate cancerAndrogen insensitivity syndromeSpinal and bulbar muscular atrophyAndrogenetic alopeciaHirsutismVulvovaginal atrophy
05

Safety considerations

Risk of prostate cancer progressionVirilization in femalesHepatotoxicityCardiovascular disease riskMood and behavioral changes
06

Interacting drugs

Prasterone

11 more in the full profile.

07

Biomarkers

Prostate-specific antigen (PSA)AR-V7 splice variantSerum testosteroneSerum dihydrotestosterone (DHT)

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