糖皮质激素受体：修订间差异

糖皮質激素受體
已知的結構
PDB	直系同源搜索: PDBe RCSB
PDBID列表
	1M2Z、1NHZ、1P93、3BQD、3CLD、3E7C、3H52、3K22、3K23、4CSJ、4HN5、4HN6、4LSJ、4MDD、4P6W、4P6X、5CBY、5CBX、4UDC、4UDD、5CBZ、5CC1、5EMQ、5EMC、5EMP
識別號
别名	NR3C1；, GCCR, GCR, GCRST, GR, GRL, nuclear receptor subfamily 3 group C member 1, Glucocorticoid Receptor
外部ID	OMIM：138040 MGI：95824 HomoloGene：30960 GeneCards：NR3C1
相關疾病
	glucocorticoid resistance
為以下藥物的標靶
	莫米松、去炎松、泼尼松龙
	布地奈德、環索奈德、丙酸氯倍他索、皮質醇、11-脱氧皮质酮、去羥米松、地塞米松、difluprednate、氟轻松、氟欣諾能、fluorometholone、氟替卡松、丙酸氟替卡松、甲泼尼龙、泼尼松龙、强的松、RU28362、去炎松、曲安奈德、倍他米松、美服培酮
基因位置（人类）
染色体	5號染色體
终止	143,435,512 bp
基因位置（小鼠）
染色体	小鼠18号染色体
终止	39,652,474 bp
RNA表达模式
	; ; ; ;
	查阅更多表达数据
基因本體
分子功能	• steroid hormone binding; • DNA结合; • sequence-specific DNA binding; • DNA结合转录因子活性; • 鋅離子結合; • DNA-binding transcription activator activity, RNA polymerase II-specific; • glucocorticoid receptor activity; • nuclear receptor activity; • 金屬離子結合; • RNA polymerase II cis-regulatory region sequence-specific DNA binding; • steroid hormone receptor activity; • steroid binding; • 血浆蛋白结合; • lipid binding; • RNA binding; • SUMO binding; • Hsp90 protein binding; • DNA-binding transcription factor activity, RNA polymerase II-specific; • protein kinase binding;
細胞組分	• 細胞質; • 核质; • 线粒体基质; • 線粒體; • 细胞核; • 细胞骨架; • 纺锤体; • 微管组织中心; • 细胞质基质; • nuclear speck; • 大分子复合体;
生物學過程	• cellular response to steroid hormone stimulus; • regulation of transcription, DNA-templated; • glucocorticoid mediated signaling pathway; • transcription by RNA polymerase II; • transcription initiation from RNA polymerase II promoter; • glucocorticoid receptor signaling pathway; • 訊息傳遞; • steroid hormone mediated signaling pathway; • 細胞週期; • 細胞分裂; • 细胞凋亡; • 染色体分离; • negative regulation of transcription by RNA polymerase II; • transcription, DNA-templated; • cellular response to dexamethasone stimulus; • cellular response to transforming growth factor beta stimulus; • positive regulation of transcription by RNA polymerase II; • cellular response to glucocorticoid stimulus; • chromatin organization; • positive regulation of pri-miRNA transcription by RNA polymerase II;
	Sources:Amigo / QuickGO
直系同源
	2908
	14815
	ENSG00000113580
	ENSMUSG00000024431
	P04150; Q3MSN4
	P06537
NM_000176; NM_001018074; NM_001018075; NM_001018076; NM_001018077;
	NM_001020825; NM_001024094; NM_001204258; NM_001204259; NM_001204260; NM_001204261; NM_001204262; NM_001204263; NM_001204264; NM_001204265; NM_001364180; NM_001364181; NM_001364182; NM_001364183; NM_001364184; NM_001364185
	NM_008173; NM_001361209; NM_001361210; NM_001361211; NM_001361212
NP_000167; NP_001018084; NP_001018085; NP_001018086; NP_001018087;
	NP_001018661; NP_001019265; NP_001191187; NP_001191188; NP_001191189; NP_001191190; NP_001191191; NP_001191192; NP_001191193; NP_001191194; NP_001351109; NP_001351110; NP_001351111; NP_001351112; NP_001351113; NP_001351114; NP_000167.1; NP_001018084.1; NP_001018085.1; NP_001018086.1; NP_001018087.1; NP_001018661.1; NP_001019265.1; NP_001191187.1; NP_001191188.1; NP_001191189.1; NP_001191190.1; NP_001191191.1; NP_001191192.1; NP_001191193.1
	NP_001348138; NP_001348139; NP_001348140; NP_001348141; NP_032199
	維基數據
檢視/編輯人類	檢視/編輯小鼠

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2022年7月11日 (一) 01:26的版本

糖皮质激素受体，也称为NR3C1（核受体亚家族3，C组，成员1），是皮质醇和其他糖皮质激素结合的受体。^[8]

结构

与其他类固醇受体一样，^[9]糖皮质激素受体在结构上是模块化的，^[10]并包含以下结构域（标记为A - F）：

A/B - N端调控域
C - DNA结合域（DBD）
D - 铰链区
E - 配体结合域（LBD）
F - C端结构域

配体结合和反应

在没有激素的情况下，糖皮质激素受体位于与多种蛋白质复合的细胞质中，包括热休克蛋白90（Hsp90）、热休克蛋白70（Hsp70）和蛋白FKBP4（FK506结合蛋白4）。^[11]内源性糖皮质激素皮质醇通过细胞膜扩散到细胞质中并与糖皮质激素受体结合，导致热休克蛋白释放。所得的活化形式GR具有两种主要的作用机制，反式激活和反式阻遏，^[12]^[13]如下所述。

参考文献

^ 與糖皮質激素受體相關的疾病；在維基數據上查看/編輯參考.
^ 對Glucocorticoid receptor起作用的藥物；在維基數據上查看/編輯參考.
^ 對Nuclear receptor subfamily 3 group C member 1起作用的藥物；在維基數據上查看/編輯參考.
^ ^4.0 ^4.1 ^4.2 GRCh38: Ensembl release 89: ENSG00000113580 - Ensembl, May 2017
^ ^5.0 ^5.1 ^5.2 GRCm38: Ensembl release 89: ENSMUSG00000024431 - Ensembl, May 2017
^ Human PubMed Reference:. National Center for Biotechnology Information, U.S. National Library of Medicine.
^ Mouse PubMed Reference:. National Center for Biotechnology Information, U.S. National Library of Medicine.
^ Nicolaides, Nicolas C.; Chrousos, George; Kino, Tomoshige. Glucocorticoid Receptor. Feingold, Kenneth R. (编). Endotext. South Dartmouth (MA): MDText.com, Inc. 2000. PMID 25905394.
^ Kumar, R.; Thompson, E. B. The structure of the nuclear hormone receptors. Steroids. 1999-05, 64 (5). ISSN 0039-128X. PMID 10406480. doi:10.1016/s0039-128x(99)00014-8.
^ Kumar, Raj; Thompson, E. Brad. Gene regulation by the glucocorticoid receptor: structure:function relationship. The Journal of Steroid Biochemistry and Molecular Biology. 2005-04, 94 (5). ISSN 0960-0760. PMID 15876404. doi:10.1016/j.jsbmb.2004.12.046.
^ Pratt, W. B.; Morishima, Y.; Murphy, M.; Harrell, M. Chaperoning of glucocorticoid receptors. Handbook of Experimental Pharmacology. 2006, (172). ISSN 0171-2004. PMID 16610357. doi:10.1007/3-540-29717-0_5.
^ Buckingham, Julia C. Glucocorticoids: exemplars of multi-tasking. British Journal of Pharmacology. 2006-01,. 147 Suppl 1. ISSN 0007-1188. PMC 1760726 . PMID 16402112. doi:10.1038/sj.bjp.0706456.
^ Hayashi, Ryuji; Wada, Hiroo; Ito, Kazuhiro; Adcock, Ian M. Effects of glucocorticoids on gene transcription. European Journal of Pharmacology. 2004-10-01, 500 (1-3). ISSN 0014-2999. PMID 15464020. doi:10.1016/j.ejphar.2004.07.011.

[1] 與糖皮質激素受體相關的疾病；在維基數據上查看/編輯參考.

[2] 對Glucocorticoid receptor起作用的藥物；在維基數據上查看/編輯參考.

[3] 對Nuclear receptor subfamily 3 group C member 1起作用的藥物；在維基數據上查看/編輯參考.

[refGRCh38Ensembl-4] 4.0 ^4.1 ^4.2 GRCh38: Ensembl release 89: ENSG00000113580 - Ensembl, May 2017

[refGRCm38Ensembl-5] 5.0 ^5.1 ^5.2 GRCm38: Ensembl release 89: ENSMUSG00000024431 - Ensembl, May 2017

[6] Human PubMed Reference:. National Center for Biotechnology Information, U.S. National Library of Medicine.

[7] Mouse PubMed Reference:. National Center for Biotechnology Information, U.S. National Library of Medicine.

[endotext-8] Nicolaides, Nicolas C.; Chrousos, George; Kino, Tomoshige. Glucocorticoid Receptor. Feingold, Kenneth R. (编). Endotext. South Dartmouth (MA): MDText.com, Inc. 2000. PMID 25905394.

[9] Kumar, R.; Thompson, E. B. The structure of the nuclear hormone receptors. Steroids. 1999-05, 64 (5). ISSN 0039-128X. PMID 10406480. doi:10.1016/s0039-128x(99)00014-8.

[10] Kumar, Raj; Thompson, E. Brad. Gene regulation by the glucocorticoid receptor: structure:function relationship. The Journal of Steroid Biochemistry and Molecular Biology. 2005-04, 94 (5). ISSN 0960-0760. PMID 15876404. doi:10.1016/j.jsbmb.2004.12.046.

[11] Pratt, W. B.; Morishima, Y.; Murphy, M.; Harrell, M. Chaperoning of glucocorticoid receptors. Handbook of Experimental Pharmacology. 2006, (172). ISSN 0171-2004. PMID 16610357. doi:10.1007/3-540-29717-0_5.

[12] Buckingham, Julia C. Glucocorticoids: exemplars of multi-tasking. British Journal of Pharmacology. 2006-01,. 147 Suppl 1. ISSN 0007-1188. PMC 1760726 . PMID 16402112. doi:10.1038/sj.bjp.0706456.

[13] Hayashi, Ryuji; Wada, Hiroo; Ito, Kazuhiro; Adcock, Ian M. Effects of glucocorticoids on gene transcription. European Journal of Pharmacology. 2004-10-01, 500 (1-3). ISSN 0014-2999. PMID 15464020. doi:10.1016/j.ejphar.2004.07.011.

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@@ 第9行： / 第9行： @@
 * '''E''' - 配体结合域（LBD）
 * '''F''' - [[C端]]结构域
+== 配体结合和反应 ==
+在没有激素的情况下，糖皮质激素受体位于与多种蛋白质复合的细胞质中，包括[[热休克蛋白]]90（[[Hsp90]]）、热休克蛋白70（[[Hsp70]]）和蛋白[[FKBP4]]（[[FK506]]结合蛋白4）。<ref>{{Cite journal |last=Pratt |first=W. B. |last2=Morishima |first2=Y. |last3=Murphy |first3=M. |last4=Harrell |first4=M. |date=2006 |title=Chaperoning of glucocorticoid receptors |url=https://link.springer.com/chapter/10.1007/3-540-29717-0_5 |journal=Handbook of Experimental Pharmacology |issue=172 |doi=10.1007/3-540-29717-0_5 |issn=0171-2004 |pmid=16610357}}</ref>内源性糖皮质激素[[皮质醇]]通过[[细胞膜]]扩散到[[细胞质]]中并与糖皮质激素受体结合，导致热休克蛋白释放。所得的活化形式GR具有两种主要的作用机制，反式激活和反式阻遏，<ref>{{Cite journal |last=Buckingham |first=Julia C. |date=2006-01 |title=Glucocorticoids: exemplars of multi-tasking |url=https://bpspubs.onlinelibrary.wiley.com/doi/full/10.1038/sj.bjp.0706456 |journal=British Journal of Pharmacology |volume=147 Suppl 1 |doi=10.1038/sj.bjp.0706456 |issn=0007-1188 |pmc=1760726 |pmid=16402112}}</ref><ref>{{Cite journal |last=Hayashi |first=Ryuji |last2=Wada |first2=Hiroo |last3=Ito |first3=Kazuhiro |last4=Adcock |first4=Ian M. |date=2004-10-01 |title=Effects of glucocorticoids on gene transcription |url=https://www.sciencedirect.com/science/article/abs/pii/S0014299904007204 |journal=European Journal of Pharmacology |volume=500 |issue=1-3 |doi=10.1016/j.ejphar.2004.07.011 |issn=0014-2999 |pmid=15464020}}</ref>如下所述。
 == 参考文献 ==