GPER1 Membrane Protein Introduction

Introduction of GPER1

GPER1 is a kind of G protein-coupled receptor analog GPCR-Br cDNA obtained from human breast cancer cells by subtractive hybridization in the late 1990s. It was confirmed by comparing its cDNA and gene library to a new G protein. The full-length gene is 2 604 bp and is located on chromosome 7p22, including a non-coding region of 504 bp on the 5' end, a non-coding region of 972 bp on the 3' terminus, and an 1128 bp long encoding region. It has 375 amino acids, an open reading frame of a protein with a molecular mass of approximately 4227 u.

Basic Information of GPER1
Protein Name	G-protein coupled estrogen receptor 1
Gene Name	GPER1
Aliases	FEG-1, GPCR-Br, LYGPR, mER, CEPR, CMKRL2, DRY12, GPER
Organism	Homo sapiens (Human)
UniProt ID	Q99527
Transmembrane Times	7
Length (aa)	375
Sequence	MDVTSQARGVGLEMYPGTAQPAAPNTTSPELNLSHPLLGTALANGTGELSEHQQYVIGLFLSCL YTIFLFPIGFVGNILILVVNISFREKMTIPDLYFINLAVADLILVADSLIEVFNLHERYYDIAV LCTFMSLFLQVNMYSSVFFLTWMSFDRYIALARAMRCSLFRTKHHARLSCGLIWMASVSATLVP FTAVHLQHTDEACFCFADVREVQWLEVTLGFIVPFAIIGLCYSLIVRVLVRAHRHRGLRPRRQK ALRMILAVVLVFFVCWLPENVFISVHLLQRTQPGAAPCKQSFRHAHPLTGHIVNLAAFSNSCLN PLIYSFLGETFRDKLRLYIEQKTNLPALNRFCHAALKAVIPDSTEQSDVRFSSAV

Function of GPER1 Membrane Protein

GPER1 is widely distributed in many tissues, such as the female reproductive system, central hippocampal tissue, cardiovascular system, and various cancer tissues including breast cancer, prostate cancer, endometrial cancer, and ovarian cancer. Moreover, a number of studies have shown that the expression level is related to the tissue type, development level, and pathological state. GPER1 also plays a role in the slow gene effect, which is mainly manifested by the rapid non-gene effect mediating a series of other protein changes and regulating the expression of genes in the nucleus. However, the GPER1 response element has not yet been found, and GPER1 has not been found as classic.

GPER1 Membrane Protein Introduction Fig.1 The signaling pathway initiated by estrogen in MCF-7 cells. (Ji, 2016)

Application of GPER1 Membrane Protein in Literature

Elizabeth M., et al. G-Protein-Coupled Estrogen Receptor 1 Is Anatomically Positioned to Modulate Synaptic Plasticity in the Mouse Hippocampus. J Neurosci. 2015, 35(6): 2384-2397. PubMed ID: 25673833

This article reports that interaction with synaptic scaffold proteins (such as SAP97) is a prerequisite for the action of GPER1 in synapses, and estrogen may accumulate on the same synaptic element due to the action of GPER1.
Kastenberger I., et al. GPER1 (GPR30) knockout mice display reduced anxiety and altered stress response in a sex and paradigm dependent manner. Horm Behav. 2014, 66(4): 628-636. PubMed ID: 25236887

This article investigates that GPER1 is involved in the control of anxiety and stress, and its effect is more effective in male mice.
Johanna L., et al. Diverse Synaptic Distributions of G Protein-coupled Estrogen Receptor 1 in Monkey Prefrontal Cortex with Aging and Menopause. Cereb Cortex. 2017, 27(3): 2022-2033. PubMed ID: 26941383

The article reveals that age and menopausal-related damage in working memory in humans and non-human primates is mediated by the dorsolateral prefrontal cortex (diPFC), and the key to synaptic plasticity in monkey diPFC multifunction is GPER1.
Nilsson B., et al. G protein-coupled oestrogen receptor 1 (GPER1)/GPR30: a new player in cardiovascular and metabolic oestrogenic signalling. Br J Pharmacol. 2011, 163(6): 1131-1139. PubMed ID: 21250980

This article shows that GPER1 is becoming a candidate therapeutic target for cardiovascular and metabolic diseases due to its beneficial effects in the cardiovascular system.
Charlotte M., et al. 17β-estradiol inhibits spreading of metastatic cells from granulosa cell tumors through a non-genomic mechanism involving GPER1. Carcinogenesis. 2015, 36(5): 564-573, PubMed ID: 25823895

This article evaluates that E2 action was mediated by GPER1 signaling pathway by using pharmacological and RNA silencing approaches and demonstrates that GPER1 can be a possible target in this disease.

GPER1 Preparation Options

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Reference

Yanlei Ji, et al. (2016). Ultrasound-targeted microbubble destruction of calcium channel subunit α 1D siRNA inhibits breast cancer via G protein-coupled receptor 30. Oncology Reports.

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