Abstract
Sphingosine kinase 1 (SK1) is an important enzyme that regulates the balance between ceramide and sphingosine-1-phosphate (S1P). Potent and novel SK1 inhibitors (6ag, 9ab and 12aa) have been discovered through a series of modifications of sphingosine (1), the substrate of this enzyme.
MeSH terms
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Aminobutyrates / chemical synthesis
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Aminobutyrates / chemistry*
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Aminobutyrates / pharmacology
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Cell Line, Tumor
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Drug Design
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology
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Homoserine / analogs & derivatives*
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Homoserine / chemical synthesis
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Homoserine / chemistry
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Homoserine / pharmacology
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Humans
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Lysophospholipids / chemistry
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Lysophospholipids / metabolism
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Phosphotransferases (Alcohol Group Acceptor) / antagonists & inhibitors*
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Phosphotransferases (Alcohol Group Acceptor) / metabolism
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Proline / analogs & derivatives*
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Proline / chemical synthesis
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Proline / chemistry
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Proline / pharmacology
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Sphingosine / analogs & derivatives
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Sphingosine / chemistry
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Sphingosine / metabolism
Substances
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Aminobutyrates
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Enzyme Inhibitors
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Lysophospholipids
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sphingosine 1-phosphate
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Homoserine
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Proline
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Phosphotransferases (Alcohol Group Acceptor)
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sphingosine kinase
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Sphingosine