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Title: Synthesis and evaluation of sphingosine analogues as inhibitors of sphingosine kinases
Authors: Wong, L.
Tan, S.S.L.
Lam, Y. 
Melendez, A.J.
Issue Date: 25-Jun-2009
Citation: 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.
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
ISSN: 00222623
DOI: 10.1021/jm900121d
Appears in Collections:Staff Publications

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