Androgen receptor

AR
Available structures
PDBOrtholog search: PDBe RCSB
Identifiers
AliasesAR, AIS, AR8, DHTR, HUMARA, HYSP1, KD, NR3C4, SBMA, SMAX1, TFM, androgen receptor
External IDsOMIM: 313700; MGI: 88064; HomoloGene: 28; GeneCards: AR; OMA:AR - orthologs
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_001011645
NM_000044
NM_001348061
NM_001348063
NM_001348064

NM_013476

RefSeq (protein)

NP_038504

Location (UCSC)Chr X: 67.54 – 67.73 MbChr X: 97.19 – 97.37 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse
Androgen_recep
crystal structure of the human androgen receptor ligand binding domain bound with an androgen receptor nh2-terminal peptide, ar20-30, and r1881
Identifiers
SymbolAndrogen_recep
PfamPF02166
InterProIPR001103
Available protein structures:
Pfam  structures / ECOD  
PDBRCSB PDB; PDBe; PDBj
PDBsumstructure summary
Normal function of the androgen receptor. Testosterone (T) enters the cell and, if 5-alpha-reductase is present, is converted into dihydrotestosterone (DHT). Upon steroid binding, the androgen receptor (AR) undergoes a conformational change and releases heat-shock proteins (hsps). Phosphorylation (P) occurs before or after steroid binding. The AR translocates to the nucleus where dimerization, DNA binding, and the recruitment of coactivators occur. Target genes are transcribed (mRNA) and translated into proteins.[5][6][7][8]

The androgen receptor (AR), also known as NR3C4 (nuclear receptor subfamily 3, group C, member 4), is a type of nuclear receptor[9] that is activated by binding any of the androgenic hormones, including testosterone and dihydrotestosterone,[10] in the cytoplasm and then translocating into the nucleus. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor.[11][12]

The main function of the androgen receptor is as a DNA-binding transcription factor that regulates gene expression;[13] however, the androgen receptor has other functions as well.[14] Androgen-regulated genes are critical for the development and maintenance of the male sexual phenotype.

  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000169083Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000046532Ensembl, May 2017
  3. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^ Quigley CA, De Bellis A, Marschke KB, el-Awady MK, Wilson EM, French FS (June 1995). "Androgen receptor defects: historical, clinical, and molecular perspectives". Endocrine Reviews. 16 (3): 271–321. doi:10.1210/edrv-16-3-271. PMID 7671849.
  6. ^ Gottlieb B, Lombroso R, Beitel LK, Trifiro MA (January 2005). "Molecular pathology of the androgen receptor in male (in)fertility". Reproductive Biomedicine Online. 10 (1): 42–8. doi:10.1016/S1472-6483(10)60802-4. PMID 15705293.
  7. ^ Choong CS, Wilson EM (December 1998). "Trinucleotide repeats in the human androgen receptor: a molecular basis for disease". Journal of Molecular Endocrinology. 21 (3): 235–57. doi:10.1677/jme.0.0210235. PMID 9845666.
  8. ^ Meehan KL, Sadar MD (May 2003). "Androgens and androgen receptor in prostate and ovarian malignancies". Frontiers in Bioscience. 8 (1–3): d780–800. doi:10.2741/1063. PMID 12700055.
  9. ^ Lu NZ, Wardell SE, Burnstein KL, Defranco D, Fuller PJ, Giguere V, et al. (December 2006). "International Union of Pharmacology. LXV. The pharmacology and classification of the nuclear receptor superfamily: glucocorticoid, mineralocorticoid, progesterone, and androgen receptors". Pharmacological Reviews. 58 (4): 782–97. doi:10.1124/pr.58.4.9. PMID 17132855. S2CID 28626145.
  10. ^ Roy AK, Lavrovsky Y, Song CS, Chen S, Jung MH, Velu NK, et al. (1999). Regulation of androgen action. Vitamins & Hormones. Vol. 55. Elsevier. pp. 309–52. doi:10.1016/S0083-6729(08)60938-3. ISBN 978-0-12-709855-5. PMID 9949684.
  11. ^ Bardin CW, Brown T, Isomaa VV, Jänne OA (1983). "Progestins can mimic, inhibit and potentiate the actions of androgens". Pharmacology & Therapeutics. 23 (3): 443–59. doi:10.1016/0163-7258(83)90023-2. PMID 6371845.
  12. ^ Raudrant D, Rabe T (2003). "Progestogens with antiandrogenic properties". Drugs. 63 (5): 463–92. doi:10.2165/00003495-200363050-00003. PMID 12600226. S2CID 28436828.
  13. ^ Mooradian AD, Morley JE, Korenman SG (February 1987). "Biological actions of androgens". Endocrine Reviews. 8 (1): 1–28. doi:10.1210/edrv-8-1-1. PMID 3549275.
  14. ^ Heinlein CA, Chang C (October 2002). "The roles of androgen receptors and androgen-binding proteins in nongenomic androgen actions". Molecular Endocrinology. 16 (10): 2181–7. doi:10.1210/me.2002-0070. PMID 12351684.