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Sphingosine-1-phosphate receptor 5

S1P5, Edg-8
G protein-coupled receptor for the lysolipid phosphoric acid mediator sphingosine 1-phosphate [RGD, Feb 2006] (from NCBI)
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Top mentioned proteins: S1P1, S1P3, S1P2, S1P4, ACID
Papers on S1P5
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.
Sarris et al., Worcester, United States. In J Med Chem, Jan 2016
S1P5 is one of 5 receptors for sphingosine-1-phosphate and is highly expressed on endothelial cells within the blood-brain barrier, where it maintains barrier integrity in in vitro models ( J. Neuroinflamm.
Sphingosine-1-phosphate receptor antagonism enhances proliferation and migration of engrafted neural progenitor cells in a model of viral-induced demyelination.
Lane et al., Salt Lake City, United States. In Am J Pathol, Oct 2015
The oral drug FTY720 affects sphingosine-1-phosphate (S1P) signaling on targeted cells that bear the S1P receptors S1P1, S1P3, S1P4, and S1P5.
Sphingosine 1-Phosphate Receptor 3-Deficient Dendritic Cells Modulate Splenic Responses to Ischemia-Reperfusion Injury.
Okusa et al., Charlottesville, United States. In J Am Soc Nephrol, Sep 2015
Sphingosine 1-phosphate (S1P) is a sphingolipid and the natural ligand for five G protein-coupled receptors (S1P1, S1P2, S1P3, S1P4, and S1P5), and S1PR agonists reduce kidney ischemia-reperfusion injury (IRI) in mice.
Transforming growth factor β2 (TGF-β2)-induced connective tissue growth factor (CTGF) expression requires sphingosine 1-phosphate receptor 5 (S1P5) in human mesangial cells.
Pfeilschifter et al., Frankfurt am Main, Germany. In Biochim Biophys Acta, May 2015
The present study demonstrates that TGF-β2 enhances sphingosine 1-phosphate receptor 5 (S1P5) mRNA and protein expression in a time and concentration dependent manner.
Synthesis and evaluation of fluorinated fingolimod (FTY720) analogues for sphingosine-1-phosphate receptor molecular imaging by positron emission tomography.
Haufe et al., Münster, Germany. In J Med Chem, May 2015
Sphingosine-1-phosphate (S1P) is a lysophospholipid that evokes a variety of biological responses via stimulation of a set of cognate G-protein coupled receptors (GPCRs): S1P1-S1P5.
Sphingosine 1-phosphate signaling pathway in inner ear biology. New therapeutic strategies for hearing loss?
Bruni et al., Florence, Italy. In Front Aging Neurosci, 2014
Interestingly S1P, by acting as intracellular mediator or as ligand of a family of five distinct S1P receptors (S1P1-S1P5), is a very powerful bioactive sphingolipid, capable of triggering also other diverse cellular responses such as cell migration, proliferation and differentiation, and is critically involved in the development and homeostasis of several organs and tissues.
Acid sphingomyelinase is activated in sickle cell erythrocytes and contributes to inflammatory microparticle generation in SCD.
Botchwey et al., Atlanta, United States. In Blood, 2014
One of these intermediates, sphingosine 1-phosphate (S1P), is stored at high concentrations (1 μM) in red blood cells (RBCs) and directs a wide array of cellular processes mediated by 5 known G-protein coupled receptors (S1P1-S1P5).
The role of sphingosine kinase isoforms and receptors S1P1, S1P2, S1P3, and S1P5 in primary, secondary, and recurrent glioblastomas.
Kolodziej et al., Marburg an der Lahn, Germany. In Tumour Biol, 2014
Sphingosine-1-phosphate (S1P), the corresponding kinases SphK1-2, and receptors S1P1-3 and S1P5 are involved in cell survival and growth.
Lysophospholipid receptor nomenclature review: IUPHAR Review 8.
Chun et al., Los Angeles, United States. In Br J Pharmacol, 2014
There are five sphingosine 1-phosphate (S1P) receptors: protein names S1P1 -S1P5 and italicized gene names S1PR1-S1PR5 (human) and S1pr1-S1pr5 (non-human).
ASP4058, a novel agonist for sphingosine 1-phosphate receptors 1 and 5, ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.
Morokata et al., Tsukuba, Japan. In Plos One, 2013
Sphingosine-1-phosphate (S1P) is a biologically active sphingolipid that acts through the members of a family of five G protein-coupled receptors (S1P1-S1P5).
Sphingosine 1-phosphate receptor agonists: a patent review (2010-2012).
Rosen et al., Los Angeles, United States. In Expert Opin Ther Pat, 2013
EXPERT OPINION: Limited progress has been made on agonists at S1P(4,5)-R subtypes, with some families of S1P5-R agonists showing promising results in animal models of age-related cognitive disorders.
Sequential desensitization of CXCR4 and S1P5 controls natural killer cell trafficking.
Walzer et al., Lyon, France. In Blood, 2011
Coordinated changes in CXCR4 and S1P5 responsiveness govern NK-cell trafficking.
Probe Development Efforts for an Allosteric Agonist of the Sphingosine 1-phosphate Receptor 3 (S1P3)
Rosen et al., Bethesda, United States. In Unknown Journal, 2011
ML249 activates S1P3 receptor with an EC50 of 72.3 nM–132 nM, and is inactive as an agonist against other members of the receptor family S1P1 (EC50 >10 μM), S1P2 (EC50 >50 μM), S1P4 (EC50 >50 μM), and S1P5 (EC50 >25 μM).
Discovery of AMG 369, a Thiazolo[5,4-b]pyridine Agonist of S1P1 and S1P5.
Bürli et al., Thousand Oaks, United States. In Acs Med Chem Lett, 2011
These efforts resulted in the discovery of 1-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo-[5,4-b]pyridin-2-yl)benzyl)azetidine-3-carboxylic acid (5d, AMG 369), a potent dual S1P1/S1P5 agonist with limited activity at S1P3 and no activity at S1P2/S1P4.
Sphingosine 1-phosphate regulation of extracellular signal-regulated kinase-1/2 in embryonic stem cells.
Pyne et al., Glasgow, United Kingdom. In Stem Cells Dev, 2009
Fndings suggest that S1P(5) may mediate the effects of S1P in terms of regulating ERK-1/2 signaling in ES cells.
T-bet-dependent S1P5 expression in NK cells promotes egress from lymph nodes and bone marrow.
Chun et al., San Francisco, United States. In J Exp Med, 2009
These findings identify S1P5 as a T-bet-induced gene that is required for natural killer cell egress from lymph nodes and bone marrow.
S1P(5) is required for sphingosine 1-phosphate-induced autophagy in human prostate cancer PC-3 cells.
Lee et al., Taipei, Taiwan. In Am J Physiol Cell Physiol, 2009
Results suggest that, under serum-starved conditions, sphingosine 1-phosphate (S1P) further upregulates autophagic activity through S1P(5)-dependent pathways in PC-3 cells.
The sphingosine 1-phosphate receptor 5 and sphingosine kinases 1 and 2 are localised in centrosomes: possible role in regulating cell division.
Pyne et al., Glasgow, United Kingdom. In Cell Signal, 2009
The centrosomal sphingosine-1-phosphate receptor 5 might function as an intracellular target of sphingosine-1-phosphate linked to regulation of mitosis.
Natural killer cell trafficking in vivo requires a dedicated sphingosine 1-phosphate receptor.
Vivier et al., Marseille, France. In Nat Immunol, 2007
In contrast, S1P5 is detected in the brain and regulates oligodendrocyte migration and survival in vitro.
Identification of a Novel Agonist of the Sphingosine 1-phosphate Receptor 4 (S1P4)
Roberts et al., Bethesda, United States. In Unknown Journal, 0001
ML248 activates S1P4 receptor with a half maximal effective concentration (EC50) of 37.7 nM–79.1 nM, and is inactive as an agonist against other members of the receptor family, with EC50s > 25 μM against S1P1, S1P2, and S1P3 receptors, and an EC50 of 2.1 μM against the S1P5 receptor.
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