Discovery of novel sphingosine kinase 1 inhibitors |
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Authors: | Yibin Xiang Gary Asmussen Michael Booker Bradford Hirth John L Kane Junkai Liao Kevin D Noson Christopher Yee |
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Institution: | Drug and Biomaterial R&D, Genzyme Corporation, 153 Second Avenue, Waltham, MA 02451, USA |
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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. |
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