Page last updated: 2024-08-08 00:11:47

G-protein coupled estrogen receptor 1

A G-protein coupled estrogen receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q99527]

Synonyms

Chemoattractant receptor-like 2;
Flow-induced endothelial G-protein coupled receptor 1;
FEG-1;
G protein-coupled estrogen receptor 1;
G-protein coupled receptor 30;
GPCR-Br;
IL8-related receptor DRY12;
Lymphocyte-derived G-pro

Research

Bioassay Publications (5)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (40.00)29.6817
2010's3 (60.00)24.3611
2020's0 (0.00)2.80

Compounds (1)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta(c)quinolin-8-yl)ethanoneHomo sapiens (human)IC500.011011
1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta(c)quinolin-8-yl)ethanoneHomo sapiens (human)Ki0.009733

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3h-cyclopenta(c)quinolin-8-yl)ethanoneHomo sapiens (human)EC500.484733

Enables

This protein enables 7 target(s):

TargetCategoryDefinition
chromatin bindingmolecular functionBinding to chromatin, the network of fibers of DNA, protein, and sometimes RNA, that make up the chromosomes of the eukaryotic nucleus during interphase. [GOC:jl, ISBN:0198506732, PMID:20404130]
G protein-coupled receptor activitymolecular functionCombining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR]
steroid bindingmolecular functionBinding to a steroid, any of a large group of substances that have in common a ring system based on 1,2-cyclopentanoperhydrophenanthrene. [GOC:jl, ISBN:0198506732]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
nuclear estrogen receptor activitymolecular functionCombining with estrogen and transmitting the signal within the cell to trigger a change in cell activity or function. [GOC:signaling, PMID:17615392]
G protein-coupled estrogen receptor activitymolecular functionCombining with estrogen and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:signaling, PMID:17379646, PMID:20960099]
steroid hormone bindingmolecular functionBinding to a steroid hormone. [GOC:ln]

Located In

This protein is located in 29 target(s):

TargetCategoryDefinition
Golgi membranecellular componentThe lipid bilayer surrounding any of the compartments of the Golgi apparatus. [GOC:mah]
nucleuscellular componentA membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators]
nuclear envelopecellular componentThe double lipid bilayer enclosing the nucleus and separating its contents from the rest of the cytoplasm; includes the intermembrane space, a gap of width 20-40 nm (also called the perinuclear space). [ISBN:0198547684]
nucleoplasmcellular componentThat part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653]
nucleoluscellular componentA small, dense body one or more of which are present in the nucleus of eukaryotic cells. It is rich in RNA and protein, is not bounded by a limiting membrane, and is not seen during mitosis. Its prime function is the transcription of the nucleolar DNA into 45S ribosomal-precursor RNA, the processing of this RNA into 5.8S, 18S, and 28S components of ribosomal RNA, and the association of these components with 5S RNA and proteins synthesized outside the nucleolus. This association results in the formation of ribonucleoprotein precursors; these pass into the cytoplasm and mature into the 40S and 60S subunits of the ribosome. [ISBN:0198506732]
cytoplasmcellular componentThe contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]
early endosomecellular componentA membrane-bounded organelle that receives incoming material from primary endocytic vesicles that have been generated by clathrin-dependent and clathrin-independent endocytosis; vesicles fuse with the early endosome to deliver cargo for sorting into recycling or degradation pathways. [GOC:mah, NIF_Subcellular:nlx_subcell_20090701, PMID:19696797]
endoplasmic reticulumcellular componentThe irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732]
endoplasmic reticulum membranecellular componentThe lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah]
Golgi apparatuscellular componentA membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732]
trans-Golgi networkcellular componentThe network of interconnected tubular and cisternal structures located within the Golgi apparatus on the side distal to the endoplasmic reticulum, from which secretory vesicles emerge. The trans-Golgi network is important in the later stages of protein secretion where it is thought to play a key role in the sorting and targeting of secreted proteins to the correct destination. [GOC:vw, ISBN:0815316194]
cytosolcellular componentThe part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl]
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
postsynaptic densitycellular componentAn electron dense network of proteins within and adjacent to the postsynaptic membrane of an asymmetric, neuron-neuron synapse. Its major components include neurotransmitter receptors and the proteins that spatially and functionally organize them such as anchoring and scaffolding molecules, signaling enzymes and cytoskeletal components. [GOC:BHF, GOC:dos, GOC:ef, GOC:jid, GOC:pr, GOC:sjp, http://molneuro.kaist.ac.kr/psd, PMID:14532281, Wikipedia:Postsynaptic_density]
axoncellular componentThe long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732]
dendritecellular componentA neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732]
cytoplasmic vesicle membranecellular componentThe lipid bilayer surrounding a cytoplasmic vesicle. [GOC:mah]
mitochondrial membranecellular componentEither of the lipid bilayers that surround the mitochondrion and form the mitochondrial envelope. [GOC:mah, NIF_Subcellular:sao1045389829]
dendritic spine membranecellular componentThe portion of the plasma membrane surrounding a dendritic spine. [GOC:mah]
presynaptic membranecellular componentA specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194]
dendritic shaftcellular componentCylindric portion of the dendrite, directly stemming from the perikaryon, and carrying the dendritic spines. [GOC:nln]
intracellular membrane-bounded organellecellular componentOrganized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators]
axon terminuscellular componentTerminal inflated portion of the axon, containing the specialized apparatus necessary to release neurotransmitters. The axon terminus is considered to be the whole region of thickening and the terminal button is a specialized region of it. [GOC:dph, GOC:jl]
dendritic spine headcellular componentDistal part of the dendritic spine, that carries the post-synaptic density. [GOC:BHF, GOC:nln, GOC:rl]
keratin filamentcellular componentA filament composed of acidic and basic keratins (types I and II), typically expressed in epithelial cells. The keratins are the most diverse classes of IF proteins, with a large number of keratin isoforms being expressed. Each type of epithelium always expresses a characteristic combination of type I and type II keratins. [ISBN:0716731363]
perinuclear region of cytoplasmcellular componentCytoplasm situated near, or occurring around, the nucleus. [GOC:jid]
presynaptic active zonecellular componentA specialized region of the plasma membrane and cell cortex of a presynaptic neuron; encompasses a region of the plasma membrane where synaptic vesicles dock and fuse, and a specialized cortical cytoskeletal matrix. [GOC:dh, GOC:dl, GOC:ef, GOC:jid, GOC:pr, PMID:3152289]
recycling endosomecellular componentAn organelle consisting of a network of tubules that functions in targeting molecules, such as receptors transporters and lipids, to the plasma membrane. [GOC:dph, GOC:jid, GOC:kmv, GOC:rph, PMID:10930469, PMID:15601896, PMID:16246101, PMID:21556374, PMID:21562044]
hippocampal mossy fiber to CA3 synapsecellular componentOne of the giant synapses that form between the mossy fiber axons of dentate gyrus granule cells and the large complex spines of CA3 pyramidal cells. It consists of a giant bouton known as the mossy fiber expansion, synapsed to the complex, multiheaded spine (thorny excresence) of a CA3 pyramidal cell. [DOI:10.1002/1096-9861, PMID:13869693, PMID:23264762]

Active In

This protein is active in 1 target(s):

TargetCategoryDefinition
Golgi apparatuscellular componentA membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732]

Involved In

This protein is involved in 52 target(s):

TargetCategoryDefinition
positive regulation of protein phosphorylationbiological processAny process that activates or increases the frequency, rate or extent of addition of phosphate groups to amino acids within a protein. [GOC:hjd]
positive regulation of neurotransmitter secretionbiological processAny process that activates or increases the frequency, rate or extent of the regulated release of a neurotransmitter. [GOC:hjd]
negative regulation of leukocyte activationbiological processAny process that stops, prevents, or reduces the frequency, rate, or extent of leukocyte activation. [GOC:add]
inflammatory responsebiological processThe immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732]
G protein-coupled receptor signaling pathwaybiological processThe series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor]
adenylate cyclase-activating G protein-coupled receptor signaling pathwaybiological processA G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of adenylyl cyclase activity which results in an increase in the intracellular concentration of cyclic AMP (cAMP). This pathway is negatively regulated by phosphodiesterase, which cleaves cAMP and terminates the signaling. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194]
positive regulation of cytosolic calcium ion concentrationbiological processAny process that increases the concentration of calcium ions in the cytosol. [GOC:ai]
nervous system developmentbiological processThe process whose specific outcome is the progression of nervous tissue over time, from its formation to its mature state. [GOC:dgh]
positive regulation of cell population proliferationbiological processAny process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators]
negative regulation of cell population proliferationbiological processAny process that stops, prevents or reduces the rate or extent of cell proliferation. [GOC:go_curators]
positive regulation of gene expressionbiological processAny process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018]
negative regulation of gene expressionbiological processAny process that decreases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018]
negative regulation of cell cycle processbiological processAny process that decreases the rate, frequency or extent of a cellular process that is involved in the progression of biochemical and morphological phases and events that occur in a cell during successive cell replication or nuclear replication events. [GOC:dph, GOC:tb]
neuronal action potentialbiological processAn action potential that occurs in a neuron. [GOC:dph, GOC:isa_complete, GOC:tb]
cell differentiationbiological processThe cellular developmental process in which a relatively unspecialized cell, e.g. embryonic or regenerative cell, acquires specialized structural and/or functional features that characterize a specific cell. Differentiation includes the processes involved in commitment of a cell to a specific fate and its subsequent development to the mature state. [ISBN:0198506732]
apoptotic chromosome condensationbiological processThe compaction of chromatin during apoptosis. [GOC:mah]
nuclear fragmentation involved in apoptotic nuclear changebiological processThe breakdown of the nucleus into small membrane-bounded compartments, or blebs, each of which contain compacted DNA. [GOC:dph, GOC:mah, GOC:mtg_apoptosis, GOC:tb, ISBN:0721639976]
positive regulation of cell migrationbiological processAny process that activates or increases the frequency, rate or extent of cell migration. [GOC:go_curators]
intracellular steroid hormone receptor signaling pathwaybiological processThe series of molecular signals initiated by a steroid binding to an intracellular steroid hormone receptor. [GOC:mah, GOC:signaling]
positive regulation of insulin secretionbiological processAny process that activates or increases the frequency, rate or extent of the regulated release of insulin. [GOC:mah]
positive regulation of inositol trisphosphate biosynthetic processbiological processAny process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of inositol trisphosphate. [GOC:mah]
positive regulation of apoptotic processbiological processAny process that activates or increases the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis]
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processbiological processAny process that activates or increases the activity of a cysteine-type endopeptidase involved in the apoptotic process. [GOC:jl, GOC:mtg_apoptosis]
steroid hormone mediated signaling pathwaybiological processThe series of molecular signals mediated by a steroid hormone binding to a receptor. [PMID:12606724]
positive regulation of MAPK cascadebiological processAny process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators]
innate immune responsebiological processInnate immune responses are defense responses mediated by germline encoded components that directly recognize components of potential pathogens. [GO_REF:0000022, GOC:add, GOC:ebc, GOC:mtg_sensu]
negative regulation of fat cell differentiationbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of adipocyte differentiation. [GOC:go_curators]
positive regulation of epidermal growth factor receptor signaling pathwaybiological processAny process that activates or increases the frequency, rate or extent of epidermal growth factor receptor signaling pathway activity. [GOC:go_curators]
positive regulation of G protein-coupled receptor signaling pathwaybiological processAny process that activates or increases the frequency, rate or extent of G protein-coupled receptor signaling pathway activity. [GOC:go_curators]
positive regulation of transcription by RNA polymerase IIbiological processAny process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH]
negative regulation of inflammatory responsebiological processAny process that stops, prevents, or reduces the frequency, rate or extent of the inflammatory response. [GOC:ai]
positive regulation of neurogenesisbiological processAny process that activates or increases the frequency, rate or extent of neurogenesis, the generation of cells within the nervous system. [GOC:ai]
negative regulation of lipid biosynthetic processbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of lipids. [GOC:ai]
positive regulation of release of sequestered calcium ion into cytosolbiological processAny process that activates or increases the frequency, rate or extent of the release into the cytosolic compartment of calcium ions sequestered in the endoplasmic reticulum or mitochondria. [GOC:ai]
regulation of cytosolic calcium ion concentrationbiological processAny process involved in the maintenance of an internal steady state of calcium ions within the cytosol of a cell or between the cytosol and its surroundings. [GOC:ai, GOC:mah, GOC:rph]
regulation of cell cyclebiological processAny process that modulates the rate or extent of progression through the cell cycle. [GOC:ai, GOC:dph, GOC:tb]
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionbiological processAny process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai]
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai]
negative regulation of ERK1 and ERK2 cascadebiological processAny process that stops, prevents, or reduces the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:add, ISBN:0121245462, ISBN:0896039986]
positive regulation of ERK1 and ERK2 cascadebiological processAny process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah]
positive regulation of uterine smooth muscle contractionbiological processAny process that increases the frequency, rate or extent of uterine smooth muscle contraction. [GOC:go_curators]
cellular response to glucose stimulusbiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a glucose stimulus. [GOC:mah]
cellular response to tumor necrosis factorbiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a tumor necrosis factor stimulus. [GOC:mah]
cellular response to peptide hormone stimulusbiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a peptide hormone stimulus. A peptide hormone is any of a class of peptides that are secreted into the blood stream and have endocrine functions in living animals. [GOC:mah]
cellular response to mineralocorticoid stimulusbiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a mineralocorticoid stimulus. Mineralocorticoids are hormonal C21 corticosteroids synthesized from cholesterol and characterized by their similarity to aldosterone. Mineralocorticoids act primarily on water and electrolyte balance. [GOC:mah]
cellular response to estradiol stimulusbiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [GOC:mah]
positive regulation of release of cytochrome c from mitochondriabiological processAny process that increases the rate, frequency or extent of release of cytochrome c from mitochondria, the process in which cytochrome c is enabled to move from the mitochondrial intermembrane space into the cytosol, which is an early step in apoptosis and leads to caspase activation. [GOC:BHF, GOC:dph, GOC:mtg_apoptosis, GOC:tb]
positive regulation of protein localization to plasma membranebiological processAny process that activates or increases the frequency, rate or extent of protein localization to plasma membrane. [GO_REF:0000058, GOC:BHF, GOC:rl, GOC:TermGenie, PMID:11602640]
negative regulation of vascular associated smooth muscle cell proliferationbiological processAny process that stops, prevents or reduces the frequency, rate or extent of vascular smooth muscle cell proliferation. [GO_REF:0000058, GOC:TermGenie, PMID:23246467]
positive regulation of endothelial cell apoptotic processbiological processAny process that activates or increases the frequency, rate or extent of endothelial cell apoptotic process. [GOC:BHF, GOC:mah, GOC:mtg_apoptosis]
positive regulation of cardiac vascular smooth muscle cell differentiationbiological processAny process that activates or increases the frequency, rate or extent of cardiac vascular smooth muscle cell differentiation. [GOC:BHF]
positive regulation of extrinsic apoptotic signaling pathwaybiological processAny process that activates or increases the frequency, rate or extent of extrinsic apoptotic signaling pathway. [GOC:mtg_apoptosis]