Discovery of novel sphingosine kinase 1 inhibitors

Potent and novel sphingosine kinase 1 (SK1) inhibitor (12aa) have been discovered through a series of modifications of sphingosine, the substrate of this enzyme. Sphingosine kinase 1 (SK1) is an important enzyme that regulates the balance between ceramide and sphingosine-1-phosphate (S1P). Potent an...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-11, Vol.19 (21), p.6119-6121
Main Authors: Xiang, Yibin, Asmussen, Gary, Booker, Michael, Hirth, Bradford, Kane, John L., Liao, Junkai, Noson, Kevin D., Yee, Christopher
Format: Article
Language:English
Subjects:
3-Hydroxyproline
Aminobutyrates - chemical synthesis
Aminobutyrates - chemistry
Aminobutyrates - pharmacology
Analytical, structural and metabolic biochemistry
Biological and medical sciences
Cell Line, Tumor
Drug Design
Enzyme
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Enzymes and enzyme inhibitors
Fundamental and applied biological sciences. Psychology
Homoserine - analogs & derivatives
Homoserine - chemical synthesis
Homoserine - chemistry
Homoserine - pharmacology
Humans
Inhibitor
Lysophospholipids - chemistry
Lysophospholipids - metabolism
Medical sciences
Miscellaneous
Pharmacology. Drug treatments
Phosphotransferases (Alcohol Group Acceptor) - antagonists & inhibitors
Phosphotransferases (Alcohol Group Acceptor) - metabolism
Proline - analogs & derivatives
Proline - chemical synthesis
Proline - chemistry
Proline - pharmacology
SK1
Sphingosine - analogs & derivatives
Sphingosine - chemistry
Sphingosine - metabolism
Sphingosine kinase
Transferases
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Summary:Potent and novel sphingosine kinase 1 (SK1) inhibitor (12aa) have been discovered through a series of modifications of sphingosine, the substrate of this enzyme. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.09.022