雄激素受体

维基百科,自由的百科全书
跳转至: 导航搜索
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
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
RNA表达模式
PBB GE AR 211110 s at.png
PBB GE AR 211621 at.png
更多表达数据
直系同源体
物种 人类 鼠类
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]
雄激素受体
PDB 1xow EBI.jpg
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(蛋白家族查询站) PF02166
InterPro(蛋白数据整合站) IPR001103
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]

雄激素受体英语androgen receptor,简称为AR),亦被称为NR3C4(核受体亚家族3,家族C,成员4)是一类核受体[6],当雄性激素睾酮二氢睾酮[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[编辑]

参考文献[编辑]

  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. doi:10.1110/ps.051905906. PMC 2242507. PMID 16641486. 
  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. doi:10.1210/edrv-16-3-271. PMID 7671849. 
  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. doi:10.1016/S1472-6483(10)60802-4. PMID 15705293. 
  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. doi:10.1677/jme.0.0210235. PMID 9845666. 
  5. ^ Meehan KL, Sadar MD. Androgens and androgen receptor in prostate and ovarian malignancies. Front. Biosci. May 2003, 8: d780–800. doi:10.2741/1063. PMID 12700055. 
  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. doi:10.1124/pr.58.4.9. PMID 17132855. 
  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. doi:10.1016/S0083-6729(08)60938-3. ISBN 978-0-12-709855-5. PMID 9949684. 
  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. doi:10.1016/0163-7258(83)90023-2. PMID 6371845. 
  9. ^ Raudrant D, Rabe T. Progestogens with antiandrogenic properties. Drugs. 2003, 63 (5): 463–92. doi:10.2165/00003495-200363050-00003. PMID 12600226. 
  10. ^ Mooradian AD, Morley JE, Korenman SG. Biological actions of androgens. Endocr. Rev. 1987, 8 (1): 1–28. doi:10.1210/edrv-8-1-1. PMID 3549275. 
  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. doi:10.1210/me.2002-0070. PMID 12351684. 

外部链接[编辑]