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|Title:||Synthesis and evaluation of sphingosine analogues as inhibitors of sphingosine kinases|
|Source:||Wong, L., Tan, S.S.L., Lam, Y., Melendez, A.J. (2009-06-25). Synthesis and evaluation of sphingosine analogues as inhibitors of sphingosine kinases. Journal of Medicinal Chemistry 52 (12) : 3618-3626. ScholarBank@NUS Repository. https://doi.org/10.1021/jm900121d|
|Abstract:||Sphingolipid-metabolizing enzymes control the critical balance of the cellular levels of sphingolipids, including the apoptotic inducing ceramide (Cer) and the proliferative inducing sphingosine 1-phosphate (S1P). The production of S1P, catalyzed by the action of sphingosine kinases (SPHKs), is known to be critical for many cellular processes. However, it is suggested that SPHK, and/or its catalytic product S1P, plays critical roles in various diseases including autoimmune diseases, cancer, and allergies. However, there is a great limitation of specific pharmacological inhibitors for SPHKs. In this paper, we describe a novel and stereoselective method of synthesizing SPHKs inhibitors. We generated a number of novel compounds and identified a number of specific inhibitors of human SPHKs. These compounds demonstrated inhibition of SPHKs at micromolar concentrations, making them more potent than dimethylsphingosine (DMS), a wellknown inhibitor of SPHKs. In particular, one of the inhibitors was found to be selective toward a particular isoform of SPHK. © 2009 American Chemical Society.|
|Source Title:||Journal of Medicinal Chemistry|
|Appears in Collections:||Staff Publications|
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