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DrugBank target: P10275

DrugBank target: P10275 (ANDR_HUMAN)     

Example drug-target structure: 1z95

( There are 78 structures corresponding to this UniProt sequence in the PDB. Click the orange, plus icon above for a list. )

Androgen receptor

Dihydrotestosterone receptor, Nuclear receptor subfamily 3 group C member 4.

Function

Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription factor activity is modulated by bound coactivator and corepressor proteins. Transcription activation is down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3. {ECO:0000269|PubMed:14664718, ECO:0000269|PubMed:15563469, ECO:0000269|PubMed:17591767, ECO:0000269|PubMed:17911242, ECO:0000269|PubMed:18084323, ECO:0000269|PubMed:19345326, ECO:0000269|PubMed:20980437}..

Disease(s)

Androgen insensitivity syndrome (AIS) [MIM:300068]: An X- linked recessive form of pseudohermaphroditism due end-organ resistance to androgen. Affected males have female external genitalia, female breast development, blind vagina, absent uterus and female adnexa, and abdominal or inguinal testes, despite a normal 46,XY karyotype. {ECO:0000269|PubMed:10022458, ECO:0000269|PubMed:10221692, ECO:0000269|PubMed:10221770, ECO:0000269|PubMed:10404311, ECO:0000269|PubMed:10458483, ECO:0000269|PubMed:10571951, ECO:0000269|PubMed:10590024, ECO:0000269|PubMed:10690872, ECO:0000269|PubMed:11587068, ECO:0000269|PubMed:11744994, ECO:0000269|PubMed:1307250, ECO:0000269|PubMed:1316540, ECO:0000269|PubMed:1426313, ECO:0000269|PubMed:1430233, ECO:0000269|PubMed:1464650, ECO:0000269|PubMed:1480178, ECO:0000269|PubMed:1487249, ECO:0000269|PubMed:1569163, ECO:0000269|PubMed:1609793, ECO:0000269|PubMed:1775137, ECO:0000269|PubMed:1999491, ECO:0000269|PubMed:2082179, ECO:0000269|PubMed:2594783, ECO:0000269|PubMed:7537149, ECO:0000269|PubMed:7581399, ECO:0000269|PubMed:7633398, ECO:0000269|PubMed:7641413, ECO:0000269|PubMed:7671849, ECO:0000269|PubMed:7929841, ECO:0000269|PubMed:7962294, ECO:0000269|PubMed:7970939, ECO:0000269|PubMed:7981687, ECO:0000269|PubMed:7981689, ECO:0000269|PubMed:7993455, ECO:0000269|PubMed:8040309, ECO:0000269|PubMed:8096390, ECO:0000269|PubMed:8103398, ECO:0000269|PubMed:8162033, ECO:0000269|PubMed:8224266, ECO:0000269|PubMed:8281140, ECO:0000269|PubMed:8325950, ECO:0000269|PubMed:8413310, ECO:0000269|PubMed:8446106, ECO:0000269|PubMed:8626869, ECO:0000269|PubMed:8647313, ECO:0000269|PubMed:8683794, ECO:0000269|PubMed:8723113, ECO:0000269|PubMed:8768864, ECO:0000269|PubMed:8809734, ECO:0000269|PubMed:8830623, ECO:0000269|PubMed:8918984, ECO:0000269|PubMed:8990010, ECO:0000269|PubMed:9001799, ECO:0000269|PubMed:9007482, ECO:0000269|PubMed:9039340, ECO:0000269|PubMed:9106550, ECO:0000269|PubMed:9160185, ECO:0000269|PubMed:9252933, ECO:0000269|PubMed:9255042, ECO:0000269|PubMed:9302173, ECO:0000269|PubMed:9328206, ECO:0000269|PubMed:9544375, ECO:0000269|PubMed:9554754, ECO:0000269|PubMed:9610419, ECO:0000269|PubMed:9627582, ECO:0000269|PubMed:9698822, ECO:0000269|PubMed:9788719, ECO:0000269|PubMed:9851768, ECO:0000269|PubMed:9856504, ECO:0000269|Ref.107, ECO:0000269|Ref.173}. Note=The disease is caused by mutations affecting the gene represented in this entry.
Spinal and bulbar muscular atrophy X-linked 1 (SMAX1) [MIM:313200]: An X-linked recessive form of spinal muscular atrophy. Spinal muscular atrophy refers to a group of neuromuscular disorders characterized by degeneration of the anterior horn cells of the spinal cord, leading to symmetrical muscle weakness and atrophy. SMAX1 occurs only in men. Age at onset is usually in the third to fifth decade of life, but earlier involvement has been reported. It is characterized by slowly progressive limb and bulbar muscle weakness with fasciculations, muscle atrophy, and gynecomastia. The disorder is clinically similar to classic forms of autosomal spinal muscular atrophy. {ECO:0000269|PubMed:15851746}. Note=The disease is caused by mutations affecting the gene represented in this entry. Caused by trinucleotide CAG repeat expansion. In SMAX1 patients the number of Gln ranges from 38 to 62. Longer expansions result in earlier onset and more severe clinical manifestations of the disease.
Note=Defects in AR may play a role in metastatic prostate cancer. The mutated receptor stimulates prostate growth and metastases development despite of androgen ablation. This treatment can reduce primary and metastatic lesions probably by inducing apoptosis of tumor cells when they express the wild-type receptor.
Androgen insensitivity, partial (PAIS) [MIM:312300]: A disorder that is characterized by hypospadias, hypogonadism, gynecomastia, genital ambiguity, normal XY karyotype, and a pedigree pattern consistent with X-linked recessive inheritance. Some patients present azoospermia or severe oligospermia without other clinical manifestations. {ECO:0000269|PubMed:10022458, ECO:0000269|PubMed:10221692, ECO:0000269|PubMed:10470409, ECO:0000269|PubMed:10502786, ECO:0000269|PubMed:10543676, ECO:0000269|PubMed:11587068, ECO:0000269|PubMed:1303262, ECO:0000269|PubMed:1307250, ECO:0000269|PubMed:1316540, ECO:0000269|PubMed:1424203, ECO:0000269|PubMed:1430233, ECO:0000269|PubMed:2010552, ECO:0000269|PubMed:7581399, ECO:0000269|PubMed:7649358, ECO:0000269|PubMed:7671849, ECO:0000269|PubMed:7909256, ECO:0000269|PubMed:7910529, ECO:0000269|PubMed:7929841, ECO:0000269|PubMed:7970939, ECO:0000269|PubMed:7981687, ECO:0000269|PubMed:8033918, ECO:0000269|PubMed:8097257, ECO:0000269|PubMed:8126121, ECO:0000269|PubMed:8205256, ECO:0000269|PubMed:8281139, ECO:0000269|PubMed:8325932, ECO:0000269|PubMed:8325950, ECO:0000269|PubMed:8446106, ECO:0000269|PubMed:8550758, ECO:0000269|PubMed:8809734, ECO:0000269|PubMed:8823308, ECO:0000269|PubMed:8824883, ECO:0000269|PubMed:9039340, ECO:0000269|PubMed:9196614, ECO:0000269|PubMed:9302173, ECO:0000269|PubMed:9329414, ECO:0000269|PubMed:9543136, ECO:0000269|PubMed:9607727, ECO:0000269|PubMed:9768671, ECO:0000269|PubMed:9856504, ECO:0000269|Ref.115}. Note=The disease is caused by mutations affecting the gene represented in this entry.

Schematic diagram of Pfam domains in target sequence plus wiring diagrams of PDB structures containing drug molecules

1z95
2am9
1gs4

Key:    PfamA domain  Secondary structure  Bound drug molecule

Sequence length: 918 a.a.

Approved drugs targeting this protein

The DrugBank database identifies 18 drugs for this target protein:

 

 
Generic name: DB01406 danazol
Formula: C22H27No2
Structure: There are no structures of this molecule in the PDB.
Generic name: DB01128 bicalutamide
198
Formula: C18H14F4N2O4S
Structure: There are 10 PDB structures containing this molecule of which 8 are bound to the above target protein.
 
Generic name: DB00499 flutamide
Formula: C11H11F3N2O3
Structure: There are no structures of this molecule in the PDB.
Generic name: DB00624 testosterone
TES
Formula: C19H28O2
Structure: There are 22 PDB structures containing this molecule of which 11 are bound to the above target protein.
 
Generic name: DB04839 cyproterone
Formula: C22H27Clo3
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB08804 nandrolone decanoate
Formula: C28H44O3
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00858 drostanolone
Formula: C20H32O2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00984 nandrolone phenpropionate
Formula: C27H34O3
Structure: There are no structures of this molecule in the PDB.
Generic name: DB00687 fludrocortisone
ZK5
Formula: C21H29Fo5
Structure: There is one PDB structure containing this molecule and it is bound to the above target protein.
Generic name: DB00421 spironolactone
SNL
Formula: C24H32O4S
Structure: There are 3 PDB structures containing this molecule although none are bound to the above target protein.
 
Generic name: DB00665 nilutamide
Formula: C12H10F3N3O4
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00621 oxandrolone
Formula: C19H30O3
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01185 fluoxymesterone
Formula: C20H29Fo3
Structure: There are no structures of this molecule in the PDB.
Generic name: DB00367 levonorgestrel
NOG
Formula: C21H28O2
Structure: There are 2 PDB structures containing this molecule although none are bound to the above target protein.
 
Generic name: DB08899 enzalutamide
Formula: C21H16F4N4O2S
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB06710 methyltestosterone
Formula: C20H30O2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01420 testosterone propionate
Formula: C22H32O3
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01395 drospirenone
Formula: C24H30O3
Structure: There are no structures of this molecule in the PDB.

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