Development of amidine-based sphingosine kinase 1 nanomolar inhibitors and reduction of sphingosine 1-phosphate in human leukemia cells

AJ Kennedy, TP Mathews, Y Kharel…

文献索引：Kennedy, Andrew J.; Mathews, Thomas P.; Kharel, Yugesh; Field, Saundra D.; Moyer, Morgan L.; East, James E.; Houck, Joseph D.; Lynch, Kevin R.; MacDonald, Timothy L. Journal of Medicinal Chemistry, 2011 , vol. 54, # 10 p. 3524 - 3548

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被引用次数: 53

摘要

Sphingosine 1-phosphate (S1P) is a bioactive lipid that has been identified as an accelerant of cancer progression. The sphingosine kinases (SphKs) are the sole producers of S1P, and thus, SphK inhibitors may prove effective in cancer mitigation and chemosensitization. Of the two SphKs, SphK1 overexpression has been observed in a myriad of cancer cell lines and tissues and has been recognized as the presumptive target over that of the poorly ...