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; [11]) are activated by the endogenous lipid S1P (S1P) and with lower apparent affinity, SPC (SPC). Originally cloned as orphan members of the endothelial differentiation gene (edg) family, deorphanisation as lysophospholipid receptors for S1P was based on sequence homology to LPA receptors. Current gene names have been codified as 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], and awaits precise definition. Previously-proposed SPC (or lysophophosphatidylcholine) receptors – G2A, TDAG8, OGR1 and GPR4 – continue to lack confirmation of these roles [7]. 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 [9]. The FDA-approved drug for relapsing forms of multiple sclerosis, known as fingolimod (FTY720, Gilenya), is an S1P receptor modulator.

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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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation:

Lysophospholipid (S1P) receptors. Accessed on 18/12/2014. 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.