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Structural and functional evidence that GPR30 is not a direct estrogen receptor.GPR30并非直接雌激素受体的结构和功能证据。
Cell Res. 2024 Jul;34(7):530-533. doi: 10.1038/s41422-024-00963-y. Epub 2024 May 14.
2
G protein-coupled receptor 30 (GPR30) forms a plasma membrane complex with membrane-associated guanylate kinases (MAGUKs) and protein kinase A-anchoring protein 5 (AKAP5) that constitutively inhibits cAMP production.G蛋白偶联受体30（GPR30）与膜相关鸟苷酸激酶（MAGUKs）和蛋白激酶A锚定蛋白5（AKAP5）形成一种质膜复合物，该复合物可组成性抑制环磷酸腺苷（cAMP）的产生。
J Biol Chem. 2014 Aug 8;289(32):22117-27. doi: 10.1074/jbc.M114.566893. Epub 2014 Jun 24.
3
G protein-coupled estrogen receptor 1 (GPER1)/GPR30 increases ERK1/2 activity through PDZ motif-dependent and -independent mechanisms.G蛋白偶联雌激素受体1（GPER1）/GPR30通过依赖和不依赖PDZ基序的机制增加ERK1/2活性。
J Biol Chem. 2017 Jun 16;292(24):9932-9943. doi: 10.1074/jbc.M116.765875. Epub 2017 Apr 27.
4
G protein-coupled estrogen receptor (GPER)/GPR30 forms a complex with the β-adrenergic receptor, a membrane-associated guanylate kinase (MAGUK) scaffold protein, and protein kinase A anchoring protein (AKAP) 5 in MCF7 breast cancer cells.G 蛋白偶联雌激素受体（GPER）/GPR30 在 MCF7 乳腺癌细胞中与β-肾上腺素能受体、膜相关鸟苷酸激酶（MAGUK）支架蛋白和蛋白激酶 A 锚定蛋白（AKAP）5 形成复合物。
Arch Biochem Biophys. 2024 Feb;752:109882. doi: 10.1016/j.abb.2024.109882. Epub 2024 Jan 10.
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Hetero-oligomeric Complex between the G Protein-coupled Estrogen Receptor 1 and the Plasma Membrane Ca2+-ATPase 4b.G蛋白偶联雌激素受体1与质膜Ca2+-ATP酶4b之间的异源寡聚复合物
J Biol Chem. 2015 May 22;290(21):13293-307. doi: 10.1074/jbc.M114.628743. Epub 2015 Apr 6.
6
Expression and function of the nonclassical estrogen receptor, GPR30, in human cartilage and chondrocytes.人软骨和软骨细胞中非经典雌激素受体 GPR30 的表达和功能。
J Cell Physiol. 2020 Nov;235(11):8486-8494. doi: 10.1002/jcp.29691. Epub 2020 Apr 23.
7
GPR30: A G protein-coupled receptor for estrogen.GPR30：一种雌激素的G蛋白偶联受体。
Mol Cell Endocrinol. 2007 Feb;265-266:138-42. doi: 10.1016/j.mce.2006.12.010. Epub 2007 Jan 11.
8
Ligand-Independent G Protein-Coupled Estrogen Receptor/G Protein-Coupled Receptor 30 Activity: Lack of Receptor-Dependent Effects of G-1 and 17-Estradiol.非配体依赖性G蛋白偶联雌激素受体/G蛋白偶联受体30活性：G-1和17-β-雌二醇缺乏受体依赖性效应
Mol Pharmacol. 2021 Sep;100(3):271-282. doi: 10.1124/molpharm.121.000259. Epub 2021 Jul 30.
9
Plasma membrane expression of G protein-coupled estrogen receptor (GPER)/G protein-coupled receptor 30 (GPR30) is associated with worse outcome in metachronous contralateral breast cancer.G 蛋白偶联雌激素受体（GPER）/G 蛋白偶联受体 30（GPR30）在血浆膜中的表达与对侧乳腺癌的异时性更差的结果相关。
PLoS One. 2020 Apr 17;15(4):e0231786. doi: 10.1371/journal.pone.0231786. eCollection 2020.
10
Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells.人乳腺癌细胞中与G蛋白偶联的雌激素膜受体的鉴定
Endocrinology. 2005 Feb;146(2):624-32. doi: 10.1210/en.2004-1064. Epub 2004 Nov 11.

引用本文的文献

1
AlphaFold3 versus experimental structures: assessment of the accuracy in ligand-bound G protein-coupled receptors.AlphaFold3与实验结构：配体结合型G蛋白偶联受体准确性评估
Acta Pharmacol Sin. 2025 Apr;46(4):1111-1122. doi: 10.1038/s41401-024-01429-y. Epub 2024 Dec 6.

本文引用的文献

1
The G protein-coupled oestrogen receptor GPER in health and disease: an update.G 蛋白偶联雌激素受体 GPER 在健康和疾病中的作用：最新进展。
Nat Rev Endocrinol. 2023 Jul;19(7):407-424. doi: 10.1038/s41574-023-00822-7. Epub 2023 May 16.
2
Multiplex G Protein-Coupled Receptor Screen Reveals Reliably Acting Agonists and a Gq-Phospholipase C Coupling Mode of GPR30/GPER1.多重G蛋白偶联受体筛选揭示了GPR30/GPER1可靠起作用的激动剂和Gq-磷脂酶C偶联模式。
Mol Pharmacol. 2023 Feb;103(2):48-62. doi: 10.1124/molpharm.122.000580. Epub 2022 Nov 18.
3
Role of estrogen receptors in health and disease.雌激素受体在健康和疾病中的作用。
Front Endocrinol (Lausanne). 2022 Aug 18;13:839005. doi: 10.3389/fendo.2022.839005. eCollection 2022.
4
Ligand-Independent G Protein-Coupled Estrogen Receptor/G Protein-Coupled Receptor 30 Activity: Lack of Receptor-Dependent Effects of G-1 and 17-Estradiol.非配体依赖性G蛋白偶联雌激素受体/G蛋白偶联受体30活性：G-1和17-β-雌二醇缺乏受体依赖性效应
Mol Pharmacol. 2021 Sep;100(3):271-282. doi: 10.1124/molpharm.121.000259. Epub 2021 Jul 30.
5
Structures of the glucocorticoid-bound adhesion receptor GPR97-G complex.糖皮质激素结合黏附受体 GPR97-G 复合物的结构。
Nature. 2021 Jan;589(7843):620-626. doi: 10.1038/s41586-020-03083-w. Epub 2021 Jan 6.
6
Does GPER Really Function as a G Protein-Coupled Estrogen Receptor ?GPER 真的是一种 G 蛋白偶联雌激素受体吗？
Front Endocrinol (Lausanne). 2020 Mar 31;11:148. doi: 10.3389/fendo.2020.00148. eCollection 2020.
7
Estrogen receptor signaling mechanisms.雌激素受体信号转导机制。
Adv Protein Chem Struct Biol. 2019;116:135-170. doi: 10.1016/bs.apcsb.2019.01.001. Epub 2019 Feb 4.
8
Structure of the human κ-opioid receptor in complex with JDTic.人κ-阿片受体与 JDTic 复合物的结构。
Nature. 2012 Mar 21;485(7398):327-32. doi: 10.1038/nature10939.
9
Involvement of estrogen receptor variant ER-alpha36, not GPR30, in nongenomic estrogen signaling.非基因组雌激素信号传导中涉及的是雌激素受体变体ER-alpha36，而非GPR30。
Mol Endocrinol. 2010 Apr;24(4):709-21. doi: 10.1210/me.2009-0317. Epub 2010 Mar 2.
10
G protein-coupled receptor 30 localizes to the endoplasmic reticulum and is not activated by estradiol.G蛋白偶联受体30定位于内质网，且不被雌二醇激活。
Endocrinology. 2008 Oct;149(10):4846-56. doi: 10.1210/en.2008-0269. Epub 2008 Jun 19.

Structural and functional evidence that GPR30 is not a direct estrogen receptor.

作者信息

Liu Heng, Guo Shimeng, Dai Antao, Xu Peiyu, Li Xin, Huang Sijie, He Xinheng, Wu Kai, Zhang Xinyue, Yang Dehua, Xie Xin, Xu H Eric

机构信息

The State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.

The State Key Laboratory of Chemical Biology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.

出版信息

Cell Res. 2024 Jul;34(7):530-533. doi: 10.1038/s41422-024-00963-y. Epub 2024 May 14.

DOI:10.1038/s41422-024-00963-y
PMID:38744981
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11217264/
Abstract
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