Selectivity and specificity of sphingosine 1-phosphate receptor ligands: "off-targets" or complex pharmacology?

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Abstract

A recent perspective published in Frontiers of Pharmacology by Salomone and Waeber (2011) discussed the selectivity and specificity of sphingosine 1-phosphate (S1P) receptor ligands. This perspective surveyed the use of various S1P receptor ligands and attempted to reconcile a number of inconsistencies in the predicted biological outcomes: these were interpreted as "off-target" effects. Therefore the perspective cautioned against the use of these S1P receptor ligands. Here we highlight the complex pharmacology of S1P receptors, which along with "inside-out" signaling might provide an alternative explanation for "off-target" effects.
LanguageEnglish
Article number26
Number of pages5
JournalFrontiers in Pharmacology
Volume2
DOIs
Publication statusPublished - 31 May 2011

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Lysosphingolipid Receptors
Pharmacology
Ligands

Keywords

  • sphingosine 1-phosphate
  • S1P
  • receptor ligands
  • pharmacology
  • biological outcomes
  • signalling

Cite this

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title = "Selectivity and specificity of sphingosine 1-phosphate receptor ligands: {"}off-targets{"} or complex pharmacology?",
abstract = "A recent perspective published in Frontiers of Pharmacology by Salomone and Waeber (2011) discussed the selectivity and specificity of sphingosine 1-phosphate (S1P) receptor ligands. This perspective surveyed the use of various S1P receptor ligands and attempted to reconcile a number of inconsistencies in the predicted biological outcomes: these were interpreted as {"}off-target{"} effects. Therefore the perspective cautioned against the use of these S1P receptor ligands. Here we highlight the complex pharmacology of S1P receptors, which along with {"}inside-out{"} signaling might provide an alternative explanation for {"}off-target{"} effects.",
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