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维基百科

雄激素受体

十二月 29, 2023

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
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
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]
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
PfamPF02166（旧版）
InterPro（英语：InterPro）IPR001103
現有可用的蛋白結構：
Pfam結構（旧版） / ECOD
PDBRCSB 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 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. 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. 

外部链接 编辑

  • 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
  • 醫學主題詞表（MeSH）：Androgen+Receptors
  • Brinkmann AO. (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]. （原始内容于2008-04-22）. 
  • Thompson J. (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）. 

十二月 29, 2023
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, 当雄性激素睾酮或二氢睾酮, 在细胞质中与之结合后会使之激活继而转运进核内, 与孕酮受体之间的关系很密切, 高剂量的黄体制剂可阻断, 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, 有效结构pdb, 直系同源检索, pdbe, rcsbpdb查询代码列表1e3g, 1gs4, 1t5z, 1t63, 1t65, 1xj7, 1xow, 1xq3,. 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 RCSBPDB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 membraneSources Amigo QuickGORNA表达模式更多表达数据直系同源体物种人类小鼠Entrez36711835EnsemblENSG00000169083ENSMUSG00000046532UniProtP10275P19091mRNA序列NM 000044NM 013476蛋白序列NP 000035NP 038504基因位置Chr X 66 76 66 95 MbChr X 98 15 98 32 MbPubMed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鑑定標誌Androgen recepPfamPF02166 旧版 InterPro 英语 InterPro IPR001103現有可用的蛋白結構 Pfam結構 旧版 ECODPDBRCSB PDB PDBe PDBjPDBsum 英语 PDBsum 結構概要雄激素受体的正常功能 如果细胞中存在5a 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 编辑雄激素 抗雄激素的发现及发展参考文献 编辑 PDB 2AM9 Pereira de Jesus Tran K Cote 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 nbsp PMID 16641486 doi 10 1110 ps 051905906 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 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 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 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 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 Roy AK Lavrovsky Y Song CS Chen S Jung MH Velu NK Bi BY Chatterjee B Regulation of androgen action Vitam Horm Vitamins amp Hormones 1999 55 309 52 ISBN 978 0 12 709855 5 PMID 9949684 doi 10 1016 S0083 6729 08 60938 3 Bardin CW Brown T Isomaa VV Janne 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 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 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 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 编辑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 醫學主題詞表 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 取自 https zh wikipedia org w index php title 雄激素受体 amp oldid 70154493, 维基百科，wiki，书籍，书籍，图书馆，

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