GPER1: A GPCR Protein with Multiple Domains for Drug Development and Biomarker Potential
GPER1: A GPCR Protein with Multiple Domains for Drug Development and Biomarker Potential
GPER1, also known as Leucine rich protein in GPR30 3'UTR, is a protein that is expressed in various tissues throughout the body. It is a member of the G protein-coupled receptor (GPCR) family, which is a large superfamily of transmembrane proteins that play a crucial role in cellular signaling. GPER1 is one of the many GPCR proteins that have been identified as potential drug targets or biomarkers due to its unique structure and function.
GPER1 is a 190-kDa protein that is expressed in the brain, heart, skeletal muscles, and various other tissues. It is highly conserved across species, with similar sequences observed in humans, mice, and other experimental organisms. GPER1 is localized to the cytoplasm and has been shown to interact with various cellular signaling pathways.
One of the key features of GPER1 is its ability to interact with G proteins. G proteins are a family of transmembrane proteins that play a central role in cellular signaling. They are composed of a catalytic active alpha-helices, a transmembrane segment, and an optional cytoplasmic tail. GPER1 contains a catalytic active alpha-helix that is similar to other GPCR proteins, as well as a transmembrane segment and a cytoplasmic tail.
GPER1 has been shown to interact with several different G proteins. For example, GPER1 has been shown to interact with the G protein-coupled receptor (GPCR) kinase 2 (GK2), which is a protein that is involved in the regulation of cellular signaling pathways. GK2 is a non-catalytic GPCR kinase that is activated by GPER1, which in turn activates the downstream GPCR signaling pathway.
Another example is GPER1's interaction with the G protein-coupled receptor (GPCR) agonist receptor, this interaction is involved in the regulation of neurotransmitter signaling in the brain.
GPER1 has also been shown to interact with several other G proteins, including the GPCR adapter protein, Pyh, and the GPCR intracellular signaling kinase, Pak. These interactions suggest that GPER1 may play a role in the regulation of various cellular signaling pathways, including those involved in neurotransmission, muscle contractions, and cellular signaling.
GPER1 is also a potential biomarker for certain diseases. For example, GPER1 has been shown to be expressed in the brains of individuals with Alzheimer's disease, which is a neurodegenerative disorder that is characterized by the progressive loss of brain cells. Additionally, GPER1 has been shown to be involved in the regulation of neurotransmitter signaling in the brain, which may be altered in individuals with Alzheimer's disease. Therefore, GPER1 may be a useful biomarker for the diagnosis and treatment of Alzheimer's disease.
In addition to its potential role as a drug target or biomarker, GPER1 is also of interest due to its unique structure and function. GPER1 is a large protein that contains multiple distinct domains, including an extracellular domain, a transmembrane segment, and an intracellular segment . The extracellular domain is involved in the protein's ability to interact with various cellular signaling pathways, while the transmembrane and intracellular segments are involved in the protein's localization and interactions with other cellular components.
GPER1's unique structure and function also make it a good candidate for drug development. The protein's large size and multiple domains make it difficult to target specific regions of the protein, which may limit its effectiveness as a drug. However, the protein's ability to interact with Various cellular signaling pathways also makes it a potential target for small molecules that can modulate these pathways.
In conclusion, GPER1 is a unique and highly conserved protein that is expressed in various tissues throughout the body. It is a member of the G protein-coupled receptor
Protein Name: G Protein-coupled Estrogen Receptor 1
Functions: G-protein coupled estrogen receptor that binds to 17-beta-estradiol (E2) with high affinity, leading to rapid and transient activation of numerous intracellular signaling pathways. Stimulates cAMP production, calcium mobilization and tyrosine kinase Src inducing the release of heparin-bound epidermal growth factor (HB-EGF) and subsequent transactivation of the epidermal growth factor receptor (EGFR), activating downstream signaling pathways such as PI3K/Akt and ERK/MAPK. Mediates pleiotropic functions among others in the cardiovascular, endocrine, reproductive, immune and central nervous systems. Has a role in cardioprotection by reducing cardiac hypertrophy and perivascular fibrosis in a RAMP3-dependent manner. Regulates arterial blood pressure by stimulating vasodilation and reducing vascular smooth muscle and microvascular endothelial cell proliferation. Plays a role in blood glucose homeostasis contributing to the insulin secretion response by pancreatic beta cells. Triggers mitochondrial apoptosis during pachytene spermatocyte differentiation. Stimulates uterine epithelial cell proliferation. Enhances uterine contractility in response to oxytocin. Contributes to thymic atrophy by inducing apoptosis. Attenuates TNF-mediated endothelial expression of leukocyte adhesion molecules. Promotes neuritogenesis in developing hippocampal neurons. Plays a role in acute neuroprotection against NMDA-induced excitotoxic neuronal death. Increases firing activity and intracellular calcium oscillations in luteinizing hormone-releasing hormone (LHRH) neurons. Inhibits early osteoblast proliferation at growth plate during skeletal development. Inhibits mature adipocyte differentiation and lipid accumulation. Involved in the recruitment of beta-arrestin 2 ARRB2 at the plasma membrane in epithelial cells. Functions also as a receptor for aldosterone mediating rapid regulation of vascular contractibility through the PI3K/ERK signaling pathway. Involved in cancer progression regulation. Stimulates cancer-associated fibroblast (CAF) proliferation by a rapid genomic response through the EGFR/ERK transduction pathway. Associated with EGFR, may act as a transcription factor activating growth regulatory genes (c-fos, cyclin D1). Promotes integrin alpha-5/beta-1 and fibronectin (FN) matrix assembly in breast cancer cells
The "GPER1 Target / Biomarker Review Report" is a customizable review of hundreds up to thousends of related scientific research literature by AI technology, covering specific information about GPER1 comprehensively, including but not limited to:
• general information;
• protein structure and compound binding;
• protein biological mechanisms;
• its importance;
• the target screening and validation;
• expression level;
• disease relevance;
• drug resistance;
• related combination drugs;
• pharmacochemistry experiments;
• related patent analysis;
• advantages and risks of development, etc.
The report is helpful for project application, drug molecule design, research progress updates, publication of research papers, patent applications, etc. If you are interested to get a full version of this report, please feel free to contact us at BD@silexon.ai
More Common Targets
GPHA2 | GPHB5 | GPHN | GPI | GPI transamidase complex | GPI-GlcNAc transferase complex | GPIHBP1 | GPKOW | GPLD1 | GPM6A | GPM6B | GPN1 | GPN2 | GPN3 | GPNMB | GPR101 | GPR107 | GPR108 | GPR119 | GPR12 | GPR132 | GPR135 | GPR137 | GPR137B | GPR137C | GPR139 | GPR141 | GPR142 | GPR143 | GPR146 | GPR148 | GPR149 | GPR15 | GPR150 | GPR151 | GPR152 | GPR153 | GPR155 | GPR156 | GPR157 | GPR158 | GPR158-AS1 | GPR15LG | GPR160 | GPR161 | GPR162 | GPR17 | GPR171 | GPR173 | GPR174 | GPR176 | GPR179 | GPR18 | GPR180 | GPR182 | GPR183 | GPR19 | GPR199P | GPR20 | GPR21 | GPR22 | GPR25 | GPR26 | GPR27 | GPR3 | GPR31 | GPR32 | GPR33 | GPR34 | GPR35 | GPR37 | GPR37L1 | GPR39 | GPR4 | GPR42 | GPR45 | GPR50 | GPR52 | GPR55 | GPR6 | GPR61 | GPR62 | GPR63 | GPR65 | GPR68 | GPR75 | GPR75-ASB3 | GPR78 | GPR79 | GPR82 | GPR83 | GPR84 | GPR84-AS1 | GPR85 | GPR87 | GPR88 | GPR89A | GPR89B | GPRACR | GPRASP1
