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Lysophospholipid (S1P) receptors C

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).


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Sphingosine 1-phosphate (S1P) receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Lysophospholipid receptors [18]) are activated by the endogenous lipid sphingosine 1-phosphate (S1P) and with lower apparent affinity, sphingosylphosphorylcholine (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 S1P1R, 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 [33], and awaits precise definition. Previously-proposed SPC (or lysophophosphatidylcholine) receptors- G2A, TDAG8, OGR1 and GPR4- continue to lack 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 (e.g [21]). 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 been described [15].
The S1P receptor modulator, fingolimod (FTY720, Gilenya), has received world-wide approval as the first oral therapy for relapsing forms of multiple sclerosis. This drug has a novel mechanism of action involving modulation of S1P receptors in both the immune and nervous systems [6-7,13], although the precise nature of its interaction requires clarification.


S1P1 receptor C Show summary » More detailed page

S1P2 receptor C Show summary » More detailed page

S1P3 receptor C Show summary » More detailed page

S1P4 receptor C Show summary » More detailed page

S1P5 receptor C Show summary » More detailed page


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Further reading

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation:

Jerold Chun, Victoria Blaho, Yasuyuki Kihara, Hirotaka Mizuno, Chido Mpamhanga, Sarah Spiegel. Lysophospholipid (S1P) receptors. Accessed on 20/03/2019. IUPHAR/BPS Guide to PHARMACOLOGY,

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Marrion NV, Peters JA, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2017) The Concise Guide to PHARMACOLOGY 2017/18: G protein-coupled receptors. Br J Pharmacol. 174 Suppl 1: S17-S129.