雄激素受體

雄激素受體（英語：androgen receptor，簡稱為AR），亦被稱為NR3C4（核受體亞家族3，C組，成員4）是一類核受體^[6]，當雄性激素睪酮或二氫睪酮^[7]在細胞質中與之結合後會使之激活繼而轉運進核內。雄激素受體與孕酮受體之間的關係很密切，高劑量的黃體製劑可阻斷雄激素受體^[8][9]。

雄激素受體
雄激素受體（彩虹卡通圖）結合配體的結構域正與睪酮（白色棍狀）結合的晶體結構[1]。
有效結構 PDB 直系同源檢索：PDBe, RCSB PDB查詢代碼列表 1E3G, 1GS4, 1T5Z, 1T63, 1T65, 1XJ7, 1XOW, 1XQ3, 1Z95, 2AM9, 2AMA, 2AMB, 2AO6, 2AX6, 2AX7, 2AX8, 2AX9, 2AXA, 2HVC, 2OZ7, 2PIO, 2PIP, 2PIQ, 2PIR, 2PIT, 2PIU, 2PIV, 2PIW, 2PIX, 2PKL, 2PNU, 2Q7I, 2Q7J, 2Q7K, 2Q7L, 2YHD, 2YLO, 2YLP, 2YLQ, 2Z4J, 3B5R, 3B65, 3B66, 3B67, 3B68, 3BTR, 3L3X, 3L3Z, 3RLJ, 3RLL, 3V49, 3V4A, 3ZQT, 4HLW
標識
代號	AR; AIS; DHTR; HUMARA; HYSP1; KD; NR3C4; SBMA; SMAX1; TFM
擴展標識	遺傳學：313700 鼠基因：88064 同源基因：28 IUPHAR:   ChEMBL: 1871 GeneCards: AR Gene
基因本體論描述 分子功能 · RNA polymerase II transcription factor binding · DNA binding · chromatin binding · sequence-specific DNA binding transcription factor activity · ligand-activated sequence-specific DNA binding RNA polymerase II transcription factor activity · androgen receptor activity · receptor binding · androgen binding · protein binding · beta-catenin binding · transcription factor binding · zinc ion binding · enzyme binding · sequence-specific DNA binding · transcription regulatory region DNA binding · protein dimerization activity · androgen receptor binding · POU domain binding 細胞成分 · nuclear chromatin · nucleus · nucleoplasm · cytoplasm · plasma membrane · axon · dendrite · protein complex 生物過程 · in utero embryonic development · regulation of systemic arterial blood pressure · transcription, DNA-dependent · transcription initiation from RNA polymerase II promoter · transport · signal transduction · cell-cell signaling · sex differentiation · cell death · cell proliferation · positive regulation of cell proliferation · male gonad development · gene expression · cell growth · male somatic sex determination · androgen receptor signaling pathway · intracellular receptor signaling pathway · prostate gland development · response to insulin stimulus · positive regulation of intracellular estrogen receptor signaling pathway · positive regulation of phosphorylation · negative regulation of apoptotic process · positive regulation of MAPK cascade · positive regulation of insulin-like growth factor receptor signaling pathway · negative regulation of integrin biosynthetic process · positive regulation of integrin biosynthetic process · positive regulation of transcription, DNA-dependent · positive regulation of transcription from RNA polymerase II promoter · positive regulation of transcription from RNA polymerase III promoter · regulation of developmental growth · organ formation · male genitalia morphogenesis · negative regulation of epithelial cell proliferation · regulation of catalytic activity · positive regulation of NF-kappaB transcription factor activity · protein oligomerization · activation of prostate induction by androgen receptor signaling pathway · morphogenesis of an epithelial fold · lateral sprouting involved in mammary gland duct morphogenesis · regulation of prostatic bud formation · prostate gland growth · prostate gland epithelium morphogenesis · epithelial cell differentiation involved in prostate gland development · tertiary branching involved in mammary gland duct morphogenesis · mammary gland alveolus development · regulation of establishment of protein localization to plasma membrane Sources: Amigo / QuickGO
RNA表達模式
更多表達數據
直系同源體
物種	人類	小鼠
Entrez	367	11835
Ensembl	ENSG00000169083	ENSMUSG00000046532
UniProt	P10275	P19091
mRNA序列	NM_000044	NM_013476
蛋白序列	NP_000035	NP_038504
基因位置	Chr X: 66.76 – 66.95 Mb	Chr X: 98.15 – 98.32 Mb
PubMed查詢	[1]	[2]
閱 論 編

雄激素受體
人類雄激素受體結合配體的結構域正與雄激素結合的晶體結構，受體NH2-端肽鏈、ar20-30及r1881
鑑定
標誌	Androgen_recep
Pfam	PF02166（舊版）
InterPro（英語：InterPro）	IPR001103
現有可用的蛋白結構： Pfam 結構（舊版） / ECOD PDB RCSB PDB; PDBe; PDBj PDBsum（英語：PDBsum） 結構概要

雄激素受體的正常功能。如果細胞中存在5α-還原酶，睪酮（T）進入細胞後就會被轉化為二氫睪酮（DHT）。雄激素受體（AR）一旦與甾體結合後就會發生構象改變並釋放一些熱休克蛋白（hsps）。在甾體結合之前或之後會發生磷酸化（P）。AR轉運到細胞核中，在那裡會相互之間形成二聚體、與DNA結合併招募共激活因子。靶基因被轉錄（mRNA）繼而被翻譯為蛋白質^[2][3][4][5]。

雄激素受體的主要功能是作為調控基因表達的一種結合DNA的轉錄因子^[10]；然而雄激素受體也有其它方面的功能^[11]。受雄激素調控的基因在男性性表型的發育及維持中起到重要作用。

另見

• 雄激素
• 抗雄激素的發現及發展

參考文獻

1. PDB 2AM9; Pereira de Jésus-Tran K, Côté PL, Cantin L, Blanchet J, Labrie F, Breton R. Comparison of crystal structures of human androgen receptor ligand-binding domain complexed with various agonists reveals molecular determinants responsible for binding affinity. Protein Sci. May 2006, 15 (5): 987–99. PMC 2242507 . PMID 16641486. doi:10.1110/ps.051905906.
2. Quigley CA, De Bellis A, Marschke KB, el-Awady MK, Wilson EM, French FS. Androgen receptor defects: historical, clinical, and molecular perspectives. Endocr. Rev. June 1995, 16 (3): 271–321. PMID 7671849. doi:10.1210/edrv-16-3-271.
3. Gottlieb B, Lombroso R, Beitel LK, Trifiro MA. Molecular pathology of the androgen receptor in male (in)fertility. Reprod. Biomed. Online. January 2005, 10 (1): 42–8. PMID 15705293. doi:10.1016/S1472-6483(10)60802-4.
4. Choong CS, Wilson EM. Trinucleotide repeats in the human androgen receptor: a molecular basis for disease. J. Mol. Endocrinol. December 1998, 21 (3): 235–57. PMID 9845666. doi:10.1677/jme.0.0210235.
5. Meehan KL, Sadar MD. Androgens and androgen receptor in prostate and ovarian malignancies. Front. Biosci. May 2003, 8: d780–800. PMID 12700055. doi:10.2741/1063.
6. Lu NZ, Wardell SE, Burnstein KL, Defranco D, Fuller PJ, Giguere V, Hochberg RB, McKay L, Renoir JM, Weigel NL, Wilson EM, McDonnell DP, Cidlowski JA. International Union of Pharmacology. LXV. The pharmacology and classification of the nuclear receptor superfamily: glucocorticoid, mineralocorticoid, progesterone, and androgen receptors. Pharmacol. Rev. December 2006, 58 (4): 782–97. PMID 17132855. doi:10.1124/pr.58.4.9.
7. Roy AK, Lavrovsky Y, Song CS, Chen S, Jung MH, Velu NK, Bi BY, Chatterjee B. Regulation of androgen action. Vitam. Horm. Vitamins & Hormones. 1999, 55: 309–52. ISBN 978-0-12-709855-5. PMID 9949684. doi:10.1016/S0083-6729(08)60938-3.
8. Bardin CW, Brown T, Isomaa VV, Jänne OA. Progestins can mimic, inhibit and potentiate the actions of androgens. Pharmacol. Ther. 1983, 23 (3): 443–59. PMID 6371845. doi:10.1016/0163-7258(83)90023-2.
9. Raudrant D, Rabe T. Progestogens with antiandrogenic properties. Drugs. 2003, 63 (5): 463–92. PMID 12600226. doi:10.2165/00003495-200363050-00003.^{[永久失效連結]}
10. Mooradian AD, Morley JE, Korenman SG. Biological actions of androgens. Endocr. Rev. 1987, 8 (1): 1–28. PMID 3549275. doi:10.1210/edrv-8-1-1.
11. Heinlein CA, Chang C. The roles of androgen receptors and androgen-binding proteins in nongenomic androgen actions. Mol. Endocrinol. 2002, 16 (10): 2181–7. PMID 12351684. doi:10.1210/me.2002-0070.

外部連結

• GeneReviews/NCBI/NIH/UW entry on Androgen Insensitivity Syndrome （頁面存檔備份，存於網際網路檔案館）
• OMIM entries on Androgen Insensitivity Syndrome
• GeneReviews/NIH/NCBI/UW entry on Spinal and Bulbar Muscular Atrophy, Kennedy's Disease, SBMA, X-Linked Spinal and Bulbar Muscular Atrophy （頁面存檔備份，存於網際網路檔案館）
• OMIM entries on Spinal and Bulbar Muscular Atrophy, Kennedy's Disease, SBMA, X-Linked Spinal and Bulbar Muscular Atrophy
• 醫學主題詞表（MeSH）：Androgen+Receptors
• Brinkmann AO. Androgen physiology: receptor and metabolic disorders (PDF). Robert McLachlan, editor (編). Endocrinology of Male Reproduction. Endotext.org. [2008-04-29]. （原始內容 (PDF)存檔於2012-02-22）.
• Gottlieb B. The Androgen Receptor Gene Mutations Database Server. McGill University. 2007-07-24 [2008-04-29]. （原始內容存檔於2008-04-22）.
• Thompson J. Molecular Mechanisms of Androgen Receptor Interactions (PDF). Helsinki University Biomedical Dissertations No. 80. University of Helsinki. 2006-09-30 [2008-04-29]. （原始內容 (PDF)存檔於2008-04-06）.