Lysophospholipid (S1P) receptors

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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Sphingosine 1-phosphate (S1P) receptors (nomenclature as agreed by NC-IUPHAR Subcommittee on Lysophospholipid receptors; [6]) are activated by the endogenous lipid derivatives sphingosine 1-phosphate (S1P) and with lower apparent affinity, sphingosylphosphorylcholine (SPC). Originally identified as members of the endothelial differentiation gene (edg) family along with lysophosphatidic acid receptors, the gene names have been updated to S1PR1, etc. to reflect the receptor function of these proteins. Most cellular phenomena ascribed to S1P can be explained by receptor-mediated mechanisms; S1P has also been described to act at intracellular sites [20], still awaiting precise definition. Previously-proposed SPC (or lysophophosphatidylcholine) receptors – G2A, TDAG8, OGR1 and GPR4 – are lacking confirmation of these roles [8]. The relationship between recombinant and endogenously expressed receptors is unclear. Radioligand binding has been conducted in heterologous expression systems using [32P]S1P (e.g [15]). In native systems, analysis of binding data is complicated by metabolism and high levels of nonspecific binding. Targeted deletion of several S1P receptors and key enzymes involved in S1P biosynthesis or degradation has clarified signalling pathways and physiological roles. A crystal structure of an S1P1-T4 fusion protein has recently been described [10].

Receptors

S1P1 receptor Show summary » More detailed page

S1P2 receptor Show summary » More detailed page

S1P3 receptor Show summary » More detailed page

S1P4 receptor Show summary » More detailed page

S1P5 receptor Show summary » More detailed page

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References

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation:

Lysophospholipid (S1P) receptors. Accessed on 29/07/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=135.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Spedding M, Peters JA and Harmar AJ, CGTP Collaborators. (2013) The Concise Guide to PHARMACOLOGY 2013/14: G Protein-Coupled Receptors. Br J Pharmacol. 170: 1459–1581.