S1PR1
Description
The S1PR1 (sphingosine-1-phosphate receptor 1) is a protein-coding gene located on chromosome 1.
S1PR1 (Sphingosine-1-phosphate receptor 1), also known as EDG1 (Endothelial Differentiation Gene 1), is a protein encoded by the S1PR1 gene in humans. It belongs to a family of five S1P receptors (S1PR1-5) and is a G-protein coupled receptor that binds S1P, a bioactive signaling molecule. S1PR1 is primarily expressed in endothelial cells and plays a critical role in regulating endothelial cell structure, migration, capillary network formation, and vascular maturation. S1PR1 signaling is also crucial in regulating lymphocyte maturation, migration, and trafficking. S1PR1, like other GPCRs, is composed of seven transmembrane helices arranged in a conserved bundle. It has a unique structure with a helical cap at the N terminus that limits ligand access to the binding pocket. The ligand, S1P, likely reaches the binding pocket from within the cell membrane, rather than the extracellular space, through an opening between helices I and VII.
S1PR1 is a G-protein coupled receptor (GPCR) for the signaling molecule sphingosine 1-phosphate (S1P), primarily coupled to the G(i) subclass of heteromeric G proteins. Activation of S1PR1 leads to the activation of several downstream signaling molecules including RAC1, SRC, PTK2/FAK1, and MAP kinases. S1PR1 plays a key role in cell migration, likely through its involvement in reorganizing the actin cytoskeleton and forming lamellipodia in response to stimuli that increase sphingosine kinase SPHK1 activity. It is crucial for normal chemotaxis towards S1P. S1PR1 is essential for normal embryonic heart development and cardiac morphogenesis. It also plays a significant role in the regulation of sprouting angiogenesis and vascular maturation, acting as an inhibitor of excessive sprouting during blood vessel development. S1PR1 is required for the normal egress of mature T-cells from the thymus into the bloodstream and peripheral lymphoid organs. It contributes to the migration of osteoclast precursor cells, and the regulation of bone mineralization and homeostasis. S1PR1 is involved in responses to oxidized 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine by pulmonary endothelial cells, and provides protection against ventilator-induced lung injury.
S1PR1 is also known as CD363, CHEDG1, D1S3362, ECGF1, EDG-1, EDG1, S1P1.