Emerging medicinal roles for lysophospholipid signaling

Trends Mol Med. 2006 Feb;12(2):65-75. doi: 10.1016/j.molmed.2005.12.001. Epub 2006 Jan 10.


The two lysophospholipids (LPs) lysophosphatidic acid and sphingosine 1-phosphate (S1P) regulate diverse biological processes. Over the past decade, it has become clear that medically relevant LP activities are mediated by specific G protein-coupled receptors, implicating them in the etiology of a growing number of disorders. A new class of LP agonists shows promise for drug therapy: the experimental drug FTY720 is phosphorylated in vivo to produce a potent S1P receptor agonist (FTY720-P) and is currently in Phase III clinical trials for kidney transplantation and Phase II for multiple sclerosis. Recent genetic and pharmacological studies on LP signaling in animal disease models have identified new areas in which interventions in LP signaling might provide novel therapeutic approaches for the treatment of human diseases.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Autoimmune Diseases / drug therapy*
  • Autoimmune Diseases / immunology
  • Cardiovascular Diseases / drug therapy
  • Cardiovascular Diseases / immunology
  • Humans
  • Lysophospholipids / physiology*
  • Neoplasms / drug therapy
  • Neoplasms / immunology
  • Obesity / drug therapy
  • Obesity / immunology
  • Phosphorylation
  • Receptors, G-Protein-Coupled / drug effects
  • Receptors, Lysophosphatidic Acid / agonists
  • Receptors, Lysophosphatidic Acid / antagonists & inhibitors
  • Receptors, Lysophosphatidic Acid / drug effects*
  • Receptors, Lysosphingolipid / agonists
  • Receptors, Lysosphingolipid / antagonists & inhibitors
  • Receptors, Lysosphingolipid / drug effects*
  • Signal Transduction*
  • Sphingosine / analogs & derivatives
  • Sphingosine / physiology
  • Transplantation Immunology


  • Lysophospholipids
  • Receptors, G-Protein-Coupled
  • Receptors, Lysophosphatidic Acid
  • Receptors, Lysosphingolipid
  • sphingosine 1-phosphate
  • Sphingosine
  • lysophosphatidic acid