Abstract：
:There is considerable evidence that sphingosine kinases play a key role in cancer progression, which might involve positive selection of cancer cells that have been provided with a survival and growth advantage as a consequence of overexpression of the enzyme. Therefore, inhibitors of sphingosine kinase represent a novel class of compounds that have potential as anticancer agents. Poor inhibitor potency is a major issue that has precluded successful translation of these compounds into the clinic. However, recent discoveries have shown that sphingosine kinase 1 is an allosteric enzyme and that some inhibitors offer improved effectiveness by inducing proteasomal degradation of the enzyme or having nanomolar potency. Herein, we provide a perspective about these recent developments and highlight the importance of translating basic pharmacologic and biochemical findings on sphingosine kinase into new drug discovery programs for treatment of cancer.
journal_name
Cancer Resjournal_title
Cancer researchauthors
Pyne S,Bittman R,Pyne NJdoi
10.1158/0008-5472.CAN-11-2364subject
Has Abstractpub_date
2011-11-01 00:00:00pages
6576-82issue
21eissn
0008-5472issn
1538-7445pii
0008-5472.CAN-11-2364journal_volume
71pub_type
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