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Vol. 54, Issue 2, 265-270, June 2002
Merck Research Laboratories, La Jolla, California (J.C.);
Department of Medicine, University of California, San Francisco,
California (E.J.G.); Department of Physiology, University of
Connecticut, Farmington, Connecticut (T.L.H.); Department of
Biomembrane and Biofunctional Chemisty, Hokkaido University, Sapporo,
Japan (Y.I.); Department of Pharmacology, University of Virginia,
Charlottesville, Virginia (K.R.L.); Division of Cellular Biochemistry,
Netherlands Cancer Institute, Amsterdam, The Netherlands (W.M.);
Department of Physiology and Pharmacology, University of Strathclyde,
Glasgow, Scotland (S.P.); and Department of Physiology, University of
Tennessee, Memphis, Tennessee (G.T.)
I. Introduction
II. Discovery of Lysophospholipid Receptors
III. Receptor Nomenclature
IV. Nonhuman Lysophospholipid Receptors
V. Lysophospholipid Receptor Ligands
VI. Lysophospholipid Receptor Gene Knockouts
VII. Lysophospholipid Receptor Expression
VIII. Conclusion
References
The lysophospholipids, lysophosphatidic acid (LPA) and sphingosine 1-phosphate (S1P), are now recognized as important extracellular signaling molecules. These lipid mediators are pleiotropic; among the most common cellular responses are mitogenesis, cell survival (anti-apoptosis), inhibition of adenylyl cyclase and calcium mobilization. Physiologic events associated with these mediators include platelet aggregation, vasopressor activity, wound healing, immune modulation, and angiogenesis. Many of the actions of LPA and S1P are mediated through a set of eight G protein-coupled receptors. Five of these are S1P-prefering while the remaining three are LPA receptors. These receptors are expressed widely and in aggregate signal through a variety of heterotrimeric G proteins. The lysophospholipid receptor family is referred to commonly as the "Edg" group (e.g., Edg-1, Edg-2, etc.). Herein, the molecular pharmacology of the lysophospholipid receptors is reviewed briefly, and a rational nomenclature for LPA and S1P receptors that is consistent with the International Union of Pharmacology guidelines is proposed.
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