Abstract
| Original language | English |
|---|---|
| Pages (from-to) | 6576-6582 |
| Number of pages | 7 |
| Journal | Cancer Research |
| Volume | 71 |
| Issue number | 21 |
| Early online date | 22 Sep 2011 |
| DOIs | |
| Publication status | Published - 2011 |
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Keywords
- sphingosine kinase inhibitors
- cancer
- hercules
- golden sword
Cite this
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Sphingosine kinase inhibitors and cancer : seeking the golden sword of Hercules. / Pyne, Susan; Bittman, Robert; Pyne, Nigel.
In: Cancer Research, Vol. 71, No. 21, 2011, p. 6576-6582.Research output: Contribution to journal › Article
TY - JOUR
T1 - Sphingosine kinase inhibitors and cancer
T2 - seeking the golden sword of Hercules
AU - Pyne, Susan
AU - Bittman, Robert
AU - Pyne, Nigel
PY - 2011
Y1 - 2011
N2 - 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.
AB - 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.
KW - sphingosine kinase inhibitors
KW - cancer
KW - hercules
KW - golden sword
UR - http://www.scopus.com/inward/record.url?scp=80155127315&partnerID=8YFLogxK
U2 - 10.1158/0008-5472.CAN-11-2364
DO - 10.1158/0008-5472.CAN-11-2364
M3 - Article
VL - 71
SP - 6576
EP - 6582
JO - Cancer Research
JF - Cancer Research
SN - 0008-5472
IS - 21
ER -