S1P Receptor
In vertebrates, S1P is found in the extracellular milieu and interacts with cell-surface receptors to regulate an array of cellular responses, including cell migration, differentiation and survival. S1P plays fundamental roles in morphogenetic mechanisms, such as collective cell migration, tissue inductive events and biomechanical signalling. S1P receptors exhibit unique as well as common G-proteincoupling properties. For example, S1P1 couples exclusively to the Gi/o family, whereas S1P2 is capable of coupling to Gi/o, to G12/13 as well as to the Gq family. This coupling results in the activation of small GTPases such as Rho, Rac and Ras. Further downstream effectors of S1P receptors include adenylate cylase, PI-3-kinase, phospholipase C, protein kinase C and intracellular calcium. S1P2 receptor activation results in Rho, Rho kinase and PTEN signalling, which disrupts adherens junctions. This receptor also inhibits cell migration induced by growth factors, such as platelet-derived growth factor (PDGF) and insulin-like growth factor (IGF), and chemokines, such as stromal-derived factor 1 (SDF1, CXCL12), C5a and CCL2. S1P signalling affects the collective behaviour of cells by regulating cell-matrix and cell-cell adhesion, as well as alterations to the cytoskeleton. As this signalling system is involved in human diseases, and given that therapeutic modulation of S1P receptors has just begun in the treatment of neuroinflammatory diseases, developmental insights may be useful in further application to human therapeutics.
References
1.Mendelson K,et al. Development. 2014;141(1):5–9.
References
1.Mendelson K,et al. Development. 2014;141(1):5–9.
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S1P Receptor
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Amgen-23
catalog no : M35699
cas no: 1448706-15-7
Amgen-23 is a selective and highly potent sphingosine kinase 1 (SPHK1) inhibitor that inhibits SPHK2 and can be used in anticancer research. -
Ozanimod hydrochloride
catalog no : M35654
cas no: 1618636-37-5
Ozanimod hydrochloride (RPC-1063 hydrochloride) is an orally available, selective and potent sphingosine 1-phosphate (S1P) receptor modulator that shows high affinity for S1P1 and S1P5. -
W140 HBr
catalog no : M35378
cas no: 1246817-25-3
[(3S)-3-amino-4-(3-hexylanilino)-4-oxobutyl]phosphonic acid;hydrobromide is a S1P1 antagonist with Ki of 2.84 μM. -
Vibozilimod
catalog no : M35071
cas no: 1403232-33-6
Vibozilimod (SCD-044) is S1P receptor-1 (S1PR1) agonist . -
AMG-369
catalog no : M34499
cas no: 1202073-26-4
AMG-369 (AMG 247) is an S1P1/S1P5 dual agonist that delays the onset of experimental autoimmune encephalomyelitis in rats. encephalomyelitis in rats.