雄激素受体

雄激素受体（英语：androgen receptor，简称为AR），亦被称为NR3C4（核受体亚家族3，C组，成员4）是一类核受体^[6]，当雄性激素睾酮或二氢睾酮^[7]在细胞质中与之结合后会使之激活继而转运进核内。雄激素受体与孕酮受体之间的关系很密切，高剂量的黄体制剂可阻断雄激素受体^[8][9]。

雄激素受体
雄激素受体（彩虹卡通图）结合配体的结构域正与睾酮（白色棍状）结合的晶体结构[1]。
有效结构 PDB 直系同源检索：PDBe, RCSB PDB查询代码列表 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
标识
代号	AR; AIS; DHTR; HUMARA; HYSP1; KD; NR3C4; SBMA; SMAX1; TFM
扩展标识	遗传学：313700 鼠基因：88064 同源基因：28 IUPHAR:   ChEMBL: 1871 GeneCards: AR Gene
基因本体论描述 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 细胞成分 · nuclear chromatin · nucleus · nucleoplasm · cytoplasm · plasma membrane · axon · dendrite · protein complex 生物过程 · 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表达模式
更多表达数据
直系同源体
物种	人类	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查询	[1]	[2]
查 论 编

雄激素受体
人类雄激素受体结合配体的结构域正与雄激素结合的晶体结构，受体NH2-端肽链、ar20-30及r1881
鉴定
标志	Androgen_recep
Pfam	PF02166（旧版）
InterPro（英语：InterPro）	IPR001103
现有可用的蛋白结构： Pfam 结构（旧版） / ECOD PDB RCSB PDB; PDBe; PDBj PDBsum（英语：PDBsum） 结构概要

雄激素受体的正常功能。如果细胞中存在5α-还原酶，睾酮（T）进入细胞后就会被转化为二氢睾酮（DHT）。雄激素受体（AR）一旦与甾体结合后就会发生构象改变并释放一些热休克蛋白（hsps）。在甾体结合之前或之后会发生磷酸化（P）。AR转运到细胞核中，在那里会相互之间形成二聚体、与DNA结合并招募共激活因子。靶基因被转录（mRNA）继而被翻译为蛋白质^[2][3][4][5]。

雄激素受体的主要功能是作为调控基因表达的一种结合DNA的转录因子^[10]；然而雄激素受体也有其它方面的功能^[11]。受雄激素调控的基因在男性性表型的发育及维持中起到重要作用。

另见

• 雄激素
• 抗雄激素的发现及发展

参考文献

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.^{[永久失效链接]}
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.

外部链接

• GeneReviews/NCBI/NIH/UW entry on Androgen Insensitivity Syndrome （页面存档备份，存于互联网档案馆）
• 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 （页面存档备份，存于互联网档案馆）
• OMIM entries on Spinal and Bulbar Muscular Atrophy, Kennedy's Disease, SBMA, X-Linked Spinal and Bulbar Muscular Atrophy
• 医学主题词表（MeSH）：Androgen+Receptors
• Brinkmann AO. Androgen physiology: receptor and metabolic disorders (PDF). Robert McLachlan, editor (编). Endocrinology of Male Reproduction. Endotext.org. [2008-04-29]. （原始内容 (PDF)存档于2012-02-22）.
• Gottlieb B. The Androgen Receptor Gene Mutations Database Server. McGill University. 2007-07-24 [2008-04-29]. （原始内容存档于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]. （原始内容 (PDF)存档于2008-04-06）.