Abstract
Sphingosine kinase (SPHK), which catalyzes the phosphorylation of sphingosine to generate sphingosine 1-phosphate, has two mammalian isotypes, SPHK1 and SPHK2. Both isozymes are promising anti-cancer therapeutic targets. In this report, we found that SG-12, a synthetic analogue of sphingosine that acts as a SPHK2 inhibitor, induces apoptosis via phosphorylation by SPHK2. The present results revealed the novel anti-cancer potential of a sphingosine analogue in the pathological setting where SPHK2 is upregulated.
Copyright © 2013 Elsevier Ltd. All rights reserved.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Antineoplastic Agents / chemical synthesis
-
Antineoplastic Agents / chemistry
-
Antineoplastic Agents / pharmacology*
-
Apoptosis / drug effects*
-
Cell Line, Tumor
-
Dose-Response Relationship, Drug
-
Drug Screening Assays, Antitumor
-
Mice
-
Phosphorylation / drug effects
-
Phosphotransferases (Alcohol Group Acceptor) / antagonists & inhibitors*
-
Phosphotransferases (Alcohol Group Acceptor) / metabolism
-
Protein Kinase Inhibitors / chemical synthesis
-
Protein Kinase Inhibitors / chemistry
-
Protein Kinase Inhibitors / pharmacology*
-
Sphingosine / analogs & derivatives*
-
Sphingosine / chemical synthesis
-
Sphingosine / chemistry
-
Sphingosine / pharmacology
-
Structure-Activity Relationship
Substances
-
Antineoplastic Agents
-
Protein Kinase Inhibitors
-
SG-12 compound
-
Phosphotransferases (Alcohol Group Acceptor)
-
sphingosine kinase
-
Sphingosine