Structural determinants of sphingosine‐1‐phosphate receptor selectivity [PDF]
AbstractFingolimod, the prodrug of fingolimod‐1‐phosphate (F1P), was the first sphingosine‐1‐phosphate receptor (S1PR) modulator approved for multiple sclerosis. F1P unselectively targets all five S1PR subtypes. While agonism (functional antagonism via receptor internalization) at S1PR1 leads to the desired immune modulatory effects, agonism at S1PR3 ...
Friederike Wunsch +3 more
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Fingolimod modulates microglial activation to augment markers of remyelination [PDF]
Introduction Microglial activation in multiple sclerosis has been postulated to contribute to long-term neurodegeneration during disease. Fingolimod has been shown to impact on the relapsing remitting phase of disease by modulating autoreactive T-cell ...
Baker David +2 more
doaj +2 more sources
Epilepsy is one of the common chronic neurological diseases, affecting more than 70 million people worldwide. The brains of people with epilepsy exhibit a pathological and persistent propensity for recurrent seizures.
Lin Wang +4 more
doaj +3 more sources
Impaired Sphingosine-1-Phosphate Synthesis Induces Preeclampsia by Deactivating Trophoblastic YAP (Yes-Associated Protein) Through S1PR2 (Sphingosine-1-Phosphate Receptor-2)-Induced Actin Polymerizations [PDF]
Incomplete spiral artery remodeling, caused by impaired extravillous trophoblast invasion, is a fundamental pathogenic process associated with malplacentation and the development of preeclampsia.
Yue Wu (1262184) +19 more
core +8 more sources
Intracellular S1P generation is essential for S1P-induced motility of human lung endothelial cells : role of sphingosine kinase 1 and S1P lyase [PDF]
Earlier we have shown that extracellular sphingosine-1-phosphate (S1P) induces migration of human pulmonary artery endothelial cells (HPAECs) through the activation of S1P(1) receptor, PKCε, and PLD2-PKCζ-Rac1 signaling cascade.
Gorshkova, Irina +9 more
core +4 more sources
Sphingosine-1-phosphate receptor 2 [PDF]
Sphingosine-1-phosphate (S1P) is a potent bioactive sphingolipid involved in cell proliferation, angiogenesis, inflammation and malignant transformation among other functions. S1P acts either directly on intracellular targets or activates G protein-coupled receptors, specifically five S1P receptors (S1PRs).
Mohamad, Adada +3 more
openaire +2 more sources
Interaction of microRNAs with sphingosine kinases, sphingosine-1 phosphate, and sphingosine-1 phosphate receptors in cancer [PDF]
AbstractSphingosine-1-phosphate (S1P), a pleiotropic lipid mediator, participates in various cellular processes during tumorigenesis, including cell proliferation, survival, drug resistance, metastasis, and angiogenesis. S1P is formed by two sphingosine kinases (SphKs), SphK1 and SphK2. The intracellularly produced S1P is delivered to the extracellular
Guangmeng Xu +4 more
openaire +3 more sources
Structural Insights into Sphingosine-1-phosphate Receptor Activation [PDF]
Abstract As a critical sphingolipid metabolite, sphingosine-1-phosphate (S1P) plays an essential role in immune and vascular systems. There are five S1P receptors, designated as S1PR1-5, encoded in the human genome, and their activities are governed by endogenous S1P, lipid-like S1P mimics, or non-lipid-like ...
Leiye Yu +9 more
openaire +2 more sources
Sphingosine-1-phosphate receptor signalling in the heart [PDF]
The five known members of the sphingosine-1-phosphate (S1P) receptor family exhibit diverse tissue expression profiles and couple to distinct G-protein-mediated signalling pathways. S1P1, S1P2, and S1P3 receptors are all present in the heart, but the ratio of these subtypes differs for various cardiac cells. The goal of this review is to summarize data
Christopher K, Means, Joan Heller, Brown
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Structure of the First Sphingosine 1-Phosphate Receptor [PDF]
The lipid sphingosine 1-phosphate may laterally diffuse through the membrane to bind a receptor.
Abby L, Parrill +2 more
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