雄激素受体

雄激素受体（英語：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]
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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
鑑定
標誌	Androgen_recep
Pfam	PF02166（旧版）
InterPro（英语：InterPro）	IPR001103
現有可用的蛋白結構： Pfam 結構（旧版） / ECOD PDB RCSB PDB; PDBe; PDBj PDBsum（英语：PDBsum） 結構概要

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