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Showing 1 to 20 of 31 for “"Sphingosine Kinase"”.
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Design, synthesis, and biological evaluation of selective sphingosine kinase inhibitors
Sphingosine kinase (SphK) has emerged as an attractive target for cancer therapeutics due to its role in cell proliferation. SphK phosphorylates sphingosine to form sphingosine-1-phosphate (S1P) which has been implicated as a major player in cancer growth and survival. SphK exists as two different …
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Structure Activity Relationship Studies on Isoform Selective Sphingosine Kinase Inhibitors
… have been associated with elevated levels of sphingosine-1-phosphate (S1P). S1P, a pleiotropic lipid mediator involved in a broad range of cellular processes, is synthesized solely by the phosphorylation of sphingosine (Sph) and is catalyzed by the two isoforms of sphingosine kinase (SphK1 and …
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The Role of Sphingosine Kinase 2 in Cell Growth and Apoptosis
Two isoforms of sphingosine kinase (SphK) catalyze the formation of sphingosine-1-phosphate (SIP). Whereas, SphKl stimulates cell growth and survival, it was found that when overexpressed in mouse NIH 3T3 fibroblasts SphK2 enhances caspase-dependent apoptosis in response to serum deprivation, …
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Design and Synthesis of Orally Bioavailable Sphingosine Kinase 2 Selective Inhibitors
… synthetic pathway of one prominent sphingolipid, sphingosine 1-phosphate (S1P), has been implicated in a variety of disease states such as cancer, sickle cell disease, multiple sclerosis, and renal fibrosis. Formation of S1P is facilitated from the ATP dependent phosphorylation of sphingosine …
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Structure-Activity Relationship Studies of Sphingosine Kinase Inhibitors and Mitochondrial Uncouplers
Sphingosine 1-phosphate (S1P) is a cellular signaling molecule that has been implicated in a variety of diseases including cancer, fibrosis, Alzheimer's, and sickle cell disease. It is formed from the phosphorylation of sphingosine (Sph) by sphingosine kinase (SphK) and SphK exists as two …
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Design, Synthesis, and Structure-Activity Relationship Investigation of Selective Sphingosine Kinase Inhibitors
Sphingosine kinase 1 (SphK1) is the key enzyme catalyzing the formation of sphingosine-1-phosphate (S1P), which is an important signaling molecule that regulates multiple biological process including inflammatory responses. Elevated SphK1 activity as well as upregulated S1P levels is linked to …
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Structure-activity relationship studies and biological evaluation of selective sphingosine kinase inhibitors
Sphingosine 1-phosphate (S1P) has become a prevalent drug discovery target due to studies implicating it to several disease pathologies such as fibrosis, sickle cell disease, inflammation, diabetes, and cancer. S1P functions to induce cell proliferation and migration. S1P signaling occurs through …
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Regulation of sphingosine kinase 1 oncogenic signalling by calcium and integrin binding proteins
Sphingosine kinase 1 (SK1) is one of the key enzymes that regulate the cellular balance of pro-apoptotic and pro-survival sphingolipids. By catalysing formation of the versatile signalling molecule sphingosine 1-phosphate (S1P), SK1 has clear roles in a wide range of cellular processes. The …
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Sphingosine Kinase 1 Regulates Fascin Expression to Promote Metastasis In Triple Negative Breast Cancer
… for repurposed intervention. Here, I found that sphingosine kinase 1 (SPHK1) was expressed at higher levels in TNBCs patients samples than in other breast cancer subtypes and high SPHK1 expression is associated with poor survival in TNBC patients. Also, TNBC cell lines have relatively higher …
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Intracellular sphingosine kinase activity as a regulator of endothelial cell inflammatory and angiogenic potential.
… that the intracellular levels and activity of Sphingosine Kinase (SK) regulate the inflammatory potential of the endothelium and are also an important determinant of the ability of the endothelium to undergo angiogenesis. Moderate (three to fivefold) elevations in SK activity in human umbilical …
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Suppression and activation of lipid signalling in cancer : tumour suppressor PTEN and oncogenic sphingosine kinase
… and anti-apoptotic phosphatidylinositol 3-kinase (PI3K)/AKT signalling pathway to modulate cell proliferation, cell cycle progression and cell survival. Sphingosine kinase 1 (SphK1), a known tumour promoter/oncogene, has been shown to activate the PI3K/Akt pathway to enhance resistance to …
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Design, synthesis and biological evaluation of sphingosine kinase inhibitors for the treatment of prostate cancer
Sphingosine is phosphorylated via the action of the enzymes sphingosine kinase 1 (SK1) and sphingosine kinase 2 (SK2) to produce the bioactive signalling molecule sphingosine 1-phosphate (S1P). S1P drives cancer cell proliferation and migration whilst also promoting cell survival. Many studies have …
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Metabolomic and metabolomic flux studies of the effects of sphingosine kinase inhibitors on prostate cancer cells using high-resolution mass spectrometry as an analytical technique
There is evidence of the involvement of sphingosine kinases (two isoforms termed SK1and SK2), which catalyse the formation of the bioactive lipid, sphingosine 1-phosphate(S1P), in various diseases including cancer. Over the last few years, metabolomics has become an increasingly critical part in …
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The role of a monomer/dimer equilibrium and the C-terminal tail in regulating translocation of sphingosine kinase 1 to the plasma membrane of breast cancer cells
Sphingosine kinase-1 (SK1) is able to translocate from the cytoplasm to the plasma membrane (PM) to catalyse the formation of sphingosine 1-phosphate (S1P) from sphingosine and adenosine triphosphate (ATP). It is known that both the expression and activity of SK1 is increased in many tumour types …
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The role of sphingosine kinases and dihydroceramide desaturase in regulating senescence in prostate cancer cells
Sphingosine kinase 1 and Sphingosine kinase 2 (SK1 and SK2) are lipid kinases which form the bioactive lipid sphingosine-1-phosphate (S1P). SKs have been widely implicated in human cancers and inflammation. This has been demonstrated to be a consequence of the actions of S1P, which acts as a ligand …
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The role of sphingosine kinases in pulmonary fibrosis
… growth factors that regulate this transition. Sphingosine kinases (SK) are promising new targets for pulmonary fibrosis as they regulate the balance between the proapototic ceramides and prosurvival sphingosine 1-phosphate. Sphingosine kinase 1 has a profibrotic role whilst the role of …
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Is there an association between S1P signaling and the transcription factor Nrf2?
… cancers to drugs, chemotherapy or radiotherapy. Sphingosine 1-phosphate is a biological lipid mediator that serves a pivotal function in physiological functions and pathophysiological conditions. Synthesized by sphingosine kinase, S1P regulates several cellular events through five sphingosine …
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Synthesis Of Natural Product-Based Sphingosine Derivatives
… sphingolipids and their metabolites, especially sphingosine-1-phosphate (S1P). S1P plays an important role in cell differentiation, survival, proliferation and the immune response. The enzyme sphingosine kinase (SK) is critical for the phosphorylation of sphingosine to S1P and has been examined …
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Investigating the use of omega three fish oils as protective agents against cytokine-induced skeletal muscle damage
… Proliferator-Activated Receptor-y(PPARv) and the sphingosine kinase pathway. ERA and DMA effects on cytokinereceptors were assessed by flow cytometry.ResultsERA and DMA prevented decreases in myogenesis induced by all three cytokinesthat reduced the myotube diameter and myogenic index of …
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The role of sphingolipids in autosomal dominant polycystic kidney disease (ADPKD)
… these cellular processes. Two isoforms of sphingosine kinase (SK1 and SK2) catalyse the formation of the bioactive lipid sphingosine-1-phosphate (S1P) from sphingosine.;We sought to determine the effects of modulating these enzymes, either separately or together, on the signalling pathways …
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