Protein / target
Androgen receptor
Protein at a glance
Biological role
RNA polymerase II core promoter sequence-specific DNA binding
Primary system
Endocrine & metabolic
Strongest disease association
androgen insensitivity syndrome
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
19 approved · 20 in clinical development
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues (PubMed:19022849). Transcription factor activity is modulated by bound coactivator and corepressor proteins like ZBTB7A that recruits NCOR1 and NCOR2 to the androgen response elements/ARE on target genes, negatively regulating androgen receptor signaling and androgen-induced cell proliferation (PubMed:20812024). Transcription activation is also down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3
Subcellular location
Domains and Gene Ontology detail (57)Hide
Domains & features
Gene Ontology
- Cchromatin
- Ccytoplasm
- Ccytosol
- Cnuclear speck
- Cnucleoplasm
- Cnucleus
- Cplasma membrane
- Cprotein-containing complex
- Fandrogen binding
- FATPase binding
- Fbeta-catenin binding
- Fchromatin binding
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
View supporting evidenceHide supporting evidence
Nuclear receptor signalling
- ·Steroid hormone receptors are ligand-activated transcription factors that regulate eukar…
- ·DNA-binding transcription factor activity
- ·DNA-binding transcription factor activity, RNA polymerase II-specific
- ·nuclear receptor activity
Transcriptional regulation
- ·Steroid hormone receptors are ligand-activated transcription factors that regulate eukar…
- ·DNA-binding transcription activator activity, RNA polymerase II-specific
- ·DNA-binding transcription factor activity
- ·DNA-binding transcription factor activity, RNA polymerase II-specific
Immune signalling
- ·Steroid hormone receptors are ligand-activated transcription factors that regulate eukar…
Proteolysis
- ·Ub-specific processing proteases
View underlying pathways (6)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Drugs targeting this protein
Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.
Androgen Receptor antagonist
Appears in clinical studies involving prostate cancer, prostate carcinoma, prostate neoplasm, neoplasm
Androgen Receptor antagonist
Appears in clinical studies involving prostate cancer, Hot flashes, prostate adenocarcinoma, endometriosis
Androgen Receptor antagonist
Appears in clinical studies involving prostate cancer, acute myeloid leukemia by FAB classification, prostate neoplasm, neoplasm
Androgen Receptor antagonist
Appears in clinical studies involving acne, acne, androgenetic alopecia
Androgen Receptor agonist
Appears in clinical studies involving hypogonadism, hypogonadotropic hypogonadism, orchitis, Klinefelter syndrome
Androgen Receptor antagonist
Appears in clinical studies involving prostate cancer, neoplasm, breast cancer, prostate cancer
Androgen Receptor antagonist
Appears in clinical studies involving prostate cancer, prostate neoplasm, neoplasm, cancer
ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.
Translational evidence
Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.
Strongest genetic associations
Human genetic evidence — the most direct causal link between this target and a disease.
Highest-confidence therapeutic associations
Diseases where a drug acting on this target has already reached clinical development.
Show all associationsHide all associations
Open Targets ranks 2,938 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.
Known drugs · 40 total
alcoholic hepatitis · Turner syndrome · Weight loss
breast cancer
heart failure
aplastic anemia · hip fracture · sarcopenia
hypogonadism · orchitis · neoplasm
Cachexia
breast cancer · prostate cancer
hip fracture · musculoskeletal system disorder
prostate cancer · pancreatic adenocarcinoma
osteoporosis
Tractability
Safety liabilities
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.
Show remaining trials (24)Hide
ClinicalTrials.gov via the drug-target graph.
Related literature
Papers indexed under “Receptors, Androgen” — a subject heading that covers this protein without being specific to it. Shown as context; not counted as this protein's own research activity.
Europe PMC literature, reached through a MeSH descriptor linked to this protein.
Forefront confidence
Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.
The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.
What's happening now
Recent activity around this target, drawn from one canonical event stream. Every item is reached through 6 drugs that target this protein, so each event is news about that drug rather than about the protein directly.
- Indication expanded
Indication expansion: ENZALUTAMIDE (NDA213674)
- Indication expanded
Indication expansion: ENZALUTAMIDE (NDA203415)
- Industry developmentOpinion: Pete Hegseth, ‘The Odyssey,’ and the testosterone myth
- Industry developmentOpinion: Beware the unintended consequences of testosterone screening for military servicemembers
- Industry developmentWho can access testosterone hormone medication in the U.S.?
- Industry developmentPete Hegseth’s announcement of annual testosterone screenings for service members divides medical experts
- Label change
Label change: APALUTAMIDE (NDA210951)
- Industry developmentBriefing Chat: Testosterone and sperm might get a boost from obesity drugs
- Industry development‘Not simply saving cost’: Inside Astellas CEO’s 5-year strategy to counter Xtandi’s patent cliff
- Industry development‘Not simply saving cost’: Inside Astellas CEO’s 5-year strategy to counter Xtandi’s patent cliff
- Label change
Label change: APALUTAMIDE (NDA210951)
- Label change
Label change: ENZALUTAMIDE (NDA213674)
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.