GPER-L1

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Introduction

GPER-L1 (G Protein-Coupled Estrogen Receptor 1) is a G protein-coupled receptor (GPCR) that is activated by estrogen. It is also known as GPR30. GPER-L1 is distinct from the classical nuclear estrogen receptors, ERα and ERβ, and is involved in rapid non-genomic signaling pathways.

Structure

GPER-L1 is a member of the GPCR family, which is characterized by seven transmembrane domains. These receptors are integral membrane proteins that transduce extracellular signals through the activation of intracellular G proteins. The structure of GPER-L1 allows it to interact with various ligands, including estrogen, and initiate signaling cascades within the cell.

Function

GPER-L1 mediates a variety of physiological processes through its ability to bind estrogen and activate downstream signaling pathways. These pathways include the activation of adenylyl cyclase, leading to increased levels of cyclic AMP (cAMP), and the activation of phosphatidylinositol 3-kinase (PI3K) and mitogen-activated protein kinase (MAPK) pathways. These signaling events can result in diverse cellular responses, such as cell proliferation, apoptosis, and migration.

Role in Cardiovascular System

In the cardiovascular system, GPER-L1 has been shown to mediate vasodilation and protect against vascular injury. It is involved in the regulation of blood pressure and has potential implications in the treatment of hypertension.

Role in Cancer

GPER-L1 is implicated in the progression of certain types of cancer, including breast cancer and ovarian cancer. It can influence cancer cell proliferation and survival, making it a potential target for therapeutic intervention.

Clinical Significance

The discovery of GPER-L1 has expanded the understanding of estrogen signaling beyond the classical nuclear receptors. It offers new insights into the mechanisms of estrogen action in various tissues and has potential implications for the development of novel therapeutic agents targeting estrogen-related diseases.

Research and Development

Ongoing research is focused on elucidating the precise mechanisms of GPER-L1 signaling and its role in health and disease. The development of selective GPER-L1 agonists and antagonists is an area of active investigation, with the aim of modulating its activity for therapeutic benefit.

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Contributors: Prab R. Tumpati, MD