Sphingosine-1-phosphate receptor 1 (S1P receptor 1 or S1P1), also known as endothelial differentiation gene 1 (EDG1) is a protein encoded by the S1PR1 gene in humans. It is a bioactive sphingolipid present at high concentrations in plasma and lymphatic fluid. S1P plays a critical role in regulating lymphocyte trafficking mainly through sphingosine-1-phosphate receptor 1 (S1PR1). It is a blood-borne lysosphingolipid that acts to promote endothelial cell (EC) barrier function. In plasma, it is associated with both high density lipoproteins (HDL) and albumin.
Immunogen
synthetic peptide (approximately 2.5 kDa) derived from the C-terminal region of the EDG-1/S1P1 receptor.
Application
Anti-S1P1, C-Terminal antibody produced in rabbit is suitable for western blotting at a working concentration of 5 to 10 μg/ml using RH7777 cells transfected with full-length EDG-1 receptor.
Biochem/physiol Actions
Sphingosine-1-phosphate (SPP) activates the heterotrimeric guanine nucleotide binding protein (G protein)-coupled orphan receptor EDG-1. EDG-1 is a high-affinity receptor for the bioactive lipid mediator SPP. It binds to SPP with high affinity and specificity. Overexpression of EDG-1 induces exaggerated cell-cell aggregation, enhances expression of cadherins and formation of well-developed adherens junctions. It is essential for lymphocyte egress from secondary lymphoid organs and acts as a validated drug target for the treatment of autoimmune diseases. Activated EDG-1 induces an immediate increase in intracellular calcium and is able to increase S1P1 phosphorylation.
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Biochimica et biophysica acta, 1843(2), 327-334 (2013-11-19)
The role of protein kinase C (PKC) isozymes in phorbol myristate acetate (PMA)-induced sphingosine 1-phosphate (S1P) receptor 1 (S1P1) phosphorylation was studied. Activation of S1P1 receptors induced an immediate increase in intracellular calcium, which was blocked by preincubation with PMA.
Molecular biology of the cell, 10(4), 1179-1190 (1999-04-10)
The endothelial-derived G-protein-coupled receptor EDG-1 is a high-affinity receptor for the bioactive lipid mediator sphingosine-1-phosphate (SPP). In the present study, we constructed the EDG-1-green fluorescent protein (GFP) chimera to examine the dynamics and subcellular localization of SPP-EDG-1 interaction. SPP binds
Development of a selective S1P1 receptor agonist, Syl930, as a potential therapeutic agent for autoimmune encephalitis.
Laboratory investigation; a journal of technical methods and pathology, 93(4), 462-471 (2013-02-20)
Classical Hodgkin lymphoma (CHL), a neoplasm of abnormal B lymphocytes (Hodgkin-Reed-Sternberg (HRS) cells), has been described to have a typical pattern of clinical presentation and dissemination often involving functionally contiguous lymph nodes. Despite the progress made in understanding CHL pathophysiology
The Journal of biological chemistry, 287(53), 44645-44653 (2012-11-09)
Sphingosine 1-phosphate (S1P) is a blood-borne lysosphingolipid that acts to promote endothelial cell (EC) barrier function. In plasma, S1P is associated with both high density lipoproteins (HDL) and albumin, but it is not known whether the carriers impart different effects
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