GPER1 - G Protein Coupled Estrogen Receptor 1 | Elisa - Clia - Antibody - Protein

Background:

G Protein-Coupled Estrogen Receptor 1 (GPER1), also known as G protein-coupled receptor 30 (GPR30), is a transmembrane receptor that is activated by the hormone estrogen. GPER1 was discovered relatively recently compared to other estrogen receptors. It was identified in the late 1990s and early 2000s through molecular cloning techniques.GPER1 is found in various tissues throughout the body, including the reproductive organs, cardiovascular system, central nervous system, and gastrointestinal tract. GPER1 is primarily activated by estrogen, particularly the estrogen metabolites 17β-estradiol (E2) and estrone. Apart from estrogen, GPER1 can also be activated by selective agonists such as G-1 (a synthetic compound) and some phytoestrogens.

Structural Features:

• Transmembrane Protein: GPER1 is a seven-transmembrane protein, typical of G protein-coupled receptors (GPCRs).
• Topology: It consists of an extracellular N-terminus, seven transmembrane helices connected by intracellular and extracellular loops, and an intracellular C-terminus.
• Ligand Binding Site: The binding pocket for estrogen is located within the transmembrane domain.

Subtypes and Classification:

• GPER1 is classified as a member of the G protein-coupled receptor superfamily.
• While it was initially considered a unique estrogen receptor subtype, recent research suggests that it may also have structural similarities with other GPCRs, indicating its potential to interact with a broader range of ligands and signaling pathways.

Physiological Functions:

• Cell Proliferation and Survival: GPER1 activation has been linked to the regulation of cell proliferation and survival in various tissues, including breast, endometrial, and ovarian tissues.
• Cardiovascular Effects: GPER1 plays a role in cardiovascular physiology, influencing vascular tone, endothelial function, and cardiac contractility.
• Neurological Effects: There is evidence suggesting that GPER1 activation may affect synaptic plasticity, cognition, and mood regulation.
• Metabolic Regulation: GPER1 has been implicated in the regulation of energy metabolism, adipogenesis, and glucose homeostasis.

Clinical Implications:

Cancer: GPER1 expression has been observed in various cancers, including breast, ovarian, and endometrial cancers. Its activation has been associated with tumor growth, metastasis, and resistance to therapy.

Cardiovascular Disease: Dysregulation of GPER1 signaling has been implicated in cardiovascular diseases such as hypertension, atherosclerosis, and heart failure.

Neurological Disorders: Some studies suggest a potential role for GPER1 in neurodegenerative diseases and mood disorders, although further research is needed to elucidate its precise involvement.

Endocrine Disorders: GPER1 may play a role in endocrine disorders such as polycystic ovary syndrome (PCOS) and osteoporosis.

Therapeutic Potential:

• Cancer Therapy: GPER1 antagonists are being investigated as potential therapeutics for estrogen-dependent cancers, either as standalone treatments or in combination with other therapies.
• Cardiovascular Drugs: Modulators of GPER1 signaling may hold promise for the treatment of cardiovascular diseases, although more research is needed to develop safe and effective drugs targeting this receptor.
• Neurological and Metabolic Disorders: The potential therapeutic applications of GPER1 modulation in neurological and metabolic disorders are still in the early stages of investigation.