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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WAY-272077
catalog no : M29013
cas no: 1415662-57-5
WAY-272077 is a sphingosine kinase inhibitor with anti-inflammatory, antitumor and hemostatic effects. -
4-Deoxypyridoxine hydrochloride
catalog no : M28170
cas no: 148-51-6
4-Deoxypyridoxine (hydrochloride) inhibits the degradation of intracellular S1P by inhibiting S1P lyase (SPL) activity, minimized the chemically induced apoptosis of insulinoma cell lines as S1P did. -
CS 2100
catalog no : M27618
cas no: 913827-99-3
CS 2100 is an S1P1 agonist. -
ML-031
catalog no : M27506
cas no: 852230-33-2
ML-031 activated S1P2 with an EC50 value of 1 μM in an S1P reporter assay. -
MP-A08
catalog no : M26761
cas no: 219832-49-2
MP-A08 is a highly selective ATP competitive inhibitor of sphingosine kinase (SPHK1) that targets both SphK1 and SphK2 (Ki: 6.9 ± 0.8 μM and 27 ± 3 μM, respectively).